Professor Susan Charman - Researcher Profile

Susan Charman

Address

Faculty of Pharmacy and Pharmaceutical Sciences
381 Royal Parade, Parkville

Contact Details

Tel: +61 3 990 39626

Fax: +61 3 9903 9627

Email: Susan.Charman@monash.edu

Web: http://www.monash.edu/pharm/research/


Biography

Position: Professor of Pharmaceutics Faculty of Pharmacy and Pharmaceutical Sciences.

Director of the Centre for Drug Candidate Optimisation Monash Institute of Pharmaceutical Sciences.

Understanding the relationships between basic physicochemical properties of drug candidates and their absorption, distribution, metabolism and elimination characteristics can help to guide medicinal chemistry and ensure that drug candidates have the necessary pharmacokinetic properties to deliver the desired pharmacodynamic effect.

Susan Charman is Professor and Director of the Centre for Drug Candidate Optimisation (CDCO), a collaborative research centre established in 2003 and based within the Monash Institute of Pharmaceutical Sciences. Professor Charman's group collaborates with chemists and biologists, providing expertise in physicochemical properties, metabolism and pharmacokinetics with the aim of improving the properties of prospective drug candidates. This involves integrating an understanding of pharmaceutical properties with medicinal chemistry and biology to design and identify drug candidates with the highest potential for rapid and successful development.Susan says it's often one of the most challenging aspects of drug discovery.

'We look at the chemical properties of a drug molecule and try and relate these to its absorption, distribution, and elimination profile,' Susan says. 'These properties define the time course of a drug in the body. It sounds simple, but if the drug can't reach the target site of action, and if concentrations in the body are not maintained for long enough, it won't have the desired effect.'

'We work with drug discovery scientists to design and identify the best drug candidate to take forward into clinical trials. If we do the groundwork properly during drug discovery and 'fix' potential liabilities in a drug candidate by modifying its structure, there is a far better chance of success during clinical development, and that means better drugs can get to patients in a shorter period of time,' she says.

Susan says drug discovery is a long term, high risk, multidisciplinary process. Her group has made significant contributions to the discovery, optimisation and characterisation of drug candidates targeted to treat infectious diseases, cancer and CNS disorders and her group has contributed to the progression of more than 18 new drug candidates into clinical trials. Their success in identifying new drug candidates for malaria highlights the potential impact of this work.

'We work with a number of international groups to identify new drug candidates for neglected diseases, with a particular emphasis on malaria. In collaboration with the Medicines for Malaria Venture, and chemists and biologists around the world, our work has led to one new antimalarial being approved in India, two new antimalarials currently in clinical trials, and 4 candidates undergoing preclinical toxicology testing in preparation for Phase I trials.'

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Research & Supervision Interests

    Drug Discovery and DevelopmentDrug Metabolism and PharmacokineticsOral Drug DeliveryDrug Discovery for Neglected Diseases

Keywords

Drug development, Drug discovery, Pharmaceutics, Pharmacokinetics; Drug Metabolism

Qualifications

DOCTOR OF PHILOSOPHY DEGREE IN PHARMACEUTICAL SCIE
Institution: University of Florida
Year awarded: 1987

Publications

Book Chapters

Tilley, L., Charman, S.A., Vennerstrom, J., 2012, Semisynthetic artemisinin and synthetic peroxide antimalarials, in Neglected Diseases and Drug Discovery, eds Michael Palmer and Timothy Wells, RSC Publishing, Cambridge UK, pp. 33-64.

Charman, W.N., Charman, S.A., Porter, C.J.H., 2006, Contemporary bioequivalence issues for poorly water soluble drugs, in International Bioequivalence Standards: A New Era, eds Gordon Amidon; Lawrence Lesko; Kamal Midha; Vinod Shah; John Hilfinger, TSRL Inc., Ann Arbor, USA, pp. 201-222.

Charman, W.N., Charman, S.A., Porter, C.J.H., 2006, Lipid-based systems, drug exposure and lead optimization, in Optimizing the 'Drug-like' Properties of Leads in Drug Discovery, eds Ronald T Borchardt, Edward H. Kerns, Michael J. Hageman, Dhiren R Thakker and James L. Stevens, Springer Science+Business Media, New York USA, pp. 131-150.

Charman, S.A., Charman, W.N., 2003, Oral modified-release delivery systems, in Modified-Release Drug Delivery Technology, eds Michael J Rathbone, Jonathan Hadgraft, Michael S Roberts, Marcel Dekker, Inc, USA, pp. 1-10.

Baines, P.J., Charman, S.A., Clarke, G.M., Roman, R.S., Walters, S.M., 1997, Overseas Trials, in Drug Products for Clinical Trials : An International Guide to Formulation-Production-Quality Control, Marcel Dekker, New York NY USA, pp. 301-330.

Journal Articles

Drinkwater, N., Vinh, N.B., Mistry, S.N., Bamert, R.S., Ruggeri, C., Holleran, J.P., Loganathan, S., Paiardini, A., Charman, S.A., Powell, A.K., Avery, V.M., McGowan, S., Scammells, P.J., 2016, Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions, European Journal of Medicinal Chemistry [P], vol 110, Elsevier Masson, France, pp. 43-64.

Rahmani, R.S., Ban, K., Jones, A.J., Ferrins, L., Ganame, D., Sykes, M.L., Avery, V.M., White, K.L., Ryan, E., Kaiser, M., Charman, S.A., Baell, J.B., 2015, 6-Arylpyrazine-2-carboxamides: a new core for Trypanosoma brucei inhibitors, Journal of Medicinal Chemistry [P], vol 58, issue 17, ACS Publications, Washington DC USA, pp. 6753-6765.

Phillips, M.A., Lotharius, J., Marsh, K., White, J., Dayan, A., White, K.L., Njoroge, J.W., El Mazouni, F., Lao, Y., Kokkonda, S., Tomchick, D.R., Deng, X., Laird, T., Bhatia, S.N., March-Riera, S., Ng, C.L., Fidock, D.A., Wittlin, S., Lafuente, M.J., Gamo-Benito, F.J., Sanz, L.M., Martinez, M.S., Jimenez-Diaz, M., Ferrer, S.B., Angulo-Barturen, I., Haselden, J.N., Louttit, J., Cui, Y., Sridhar, A., Zeeman, A., Kocken, C.H.M., Sauerwein, R.W., Dechering, K.J., Avery, V.M., Duffy, S., Delves, M.J., Sinden, R.E., Ruecker, A., Wickham, K.S., Rochford, R., Gahagen, J., Iyer, L., Riccio, E.S., Mirsalis, J.C., Bathhurst, I., Rueckle, T., Ding, X.C., Campo, B., Leroy, D., Charman, S.A., 2015, A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria, Science Translational Medicine [P], vol 7, issue 296, American Association for the Advancement of Science (A A A S), Washington DC USA, pp. 1-12.

Baragana, B., Hallyburton, I., Lee, M.C.S., Norcross, N.R., Grimaldi, R., Otto, T.D., Proto, W.R., Blagborough, A.M., Meister, S., Wirjanata, G., Ruecker, A., Upton, L.M., Abraham, T.S., Justino de Almeida, M., Pradhan, A., Porzelle, A., Martinez, M.S., Bolscher, J.M., Woodland, A., Norval, S., Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P.M., Churcher, T.S., Sala, K.A., Zakutansky, S.E., Jimenez-Diaz, M., Sanz, L.M., Riley, J., Basak, R., Campbell, M., Avery, V.M., Sauerwein, R.W., Dechering, K.J., Noviyanti, R., Campo, B., Frearson, J.A., Angulo-Barturen, I., Ferrer, S.B., Gamo, F., Wyatt, P.G., Leroy, D., Siegl, P., Delves, M.J., Kyle, D.E., Wittlin, S., Charman, S.A., 2015, A novel multiple-stage antimalarial agent that inhibits protein synthesis, Nature [P], vol 522, issue 7556, Macmillan Publishers, London UK, pp. 315-320.

Miley, G.P., Pou, S., Winter, R.W., Nilsen, A., Li, Y., Kelly, J.X., Stickles, A.M., Mather, M.W., Forquer, I.P., Pershing, A.M., White, K.L., Shackleford, D., Saunders, J.A., Chen, G., Ting, L., Kim, K., Zakharov, L.N., Donini, C., Burrows, J., Valdya, A.B., Charman, S.A., Riscoe, M.K., 2015, ELQ-300 prodrugs for enhanced delivery and single-dose cure of malaria, Antimicrobial Agents And Chemotherapy [P], vol 59, issue 9, American Society for Microbiology, Washington DC USA, pp. 5555-5560.

Moraes, C.B., White, K.L., Braillard, S., Perez, C., Goo, J., Gaspar, L., Shackleford, D., Cordeiro-da-Silva, A., Thompson, R.C.A., Freitas-Junior, L.H., Charman, S.A., Chatelain, E., 2015, Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties, Antimicrobial Agents and Chemotherapy [P], vol 59, issue 6, American Society for Microbiology, Washington DC USA, pp. 3645-3647.

Ryan, E., Morrow, B.J., Hemley, C.F., Pinson, J., Charman, S.A., Chiu, F.C.K., Foitzik, R., 2015, Evidence for the in vitro bioactivation of aminopyrazole derivatives: trapping reactive aminopyrazole intermediates using glutathione ethyl ester in human liver microsomes, Chemical Research In Toxicology [P], vol 28, issue 9, ACS Publications, Washington DC USA, pp. 1747-1752.

Witschel, M.C., Rottmann, M., Schwab, A., Leartsakulpanich, U., Chitnumsub, P., Seet, M., Tonazzi, S., Schwertz, G., Stelzer, F., Mietzner, T., McNamara, C.W., Thater, F., Freymond, C., Jaruwat, A., Pinthong, C., Riangrungroj, P., Oufir, M., Hamburger, M., Maser, P., Sanz, L.M., Charman, S.A., Wittlin, S., Yuthavong, Y., Chaiyen, P., Diederich, F., 2015, Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities, Journal of Medicinal Chemistry [P], vol 58, issue 7, ACS Publications, Washington DC USA, pp. 3117-3130.

Schwartz, B.D., Skinner-Adams, T.S., Andrews, K.T., Coster, M., Edstein, M.D., MacKenzie, D., Charman, S.A., Koltun, M., Blundell, S., Campbell, A., Pouwer, R.H., Quinn, R.J., Beattie, K.D., Healy, P.C., Davis, R.A., 2015, Synthesis and antimalarial evaluation of amide and urea derivatives based on the thiaplakortone A natural product scaffold, Organic & Biomolecular Chemistry [P], vol 13, issue 5, RSC Publishing, Cambridge UK, pp. 1558-1570.

Sahbaz, Y., Williams, H.D., Nguyen, T., Saunders, J.A., Ford, L., Charman, S.A., Scammells, P.J., Porter, C.J., 2015, Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations, Molecular Pharmaceutics [P], vol 12, issue 6, ACS Publications, Washington DC USA, pp. 1980-1991.

Lauterwasser, E.M.W., Fontaine, S.D., Li, H., Gut, J., Katneni, K., Charman, S.A., Rosenthal, P.J., Bogyo, M., Renslo, A.R., 2015, Trioxolane-mediated delivery of mefloquine limits brain exposure in a mouse model of malaria, A C S Medicinal Chemistry Letters [E], vol 6, issue 11, ACS Publications, Washington DC USA, pp. 1145-1149.

Jimenez-Diaz, M., Ebert, D., Salinas, Y., Pradhan, A., Lehane, A.M., Myrand-Lapierre, M., O'Loughlin, K.G., Shackleford, D., Justino de Almeida, M., Carrillo, A., Clark, J.A., Dennis, A.S.M., Diep, J., Deng, X., Duffy, S., Endsley, A.N., Fedewa, G., Guiguemde, W.A., Gomez, M.G., Holbrook, G., Horst, J.A., Kim, C.C., Liu, J., Lee, M.C.S., Matheny, A., Martinez, M.S., Miller, G.E., Rodriguez-Alejandre, A., Sanz, L.M., Sigal, M., Spillman, N.J., Stein, P.D., Wang, Z., Zhu, F., Waterson, D., Knapp, S., Shelat, A.A., Avery, V.M., Fidock, D.A., Gamo, F., Charman, S.A., Mirsalis, J.C., Ma, H., Ferrer, S.B., Kirk, K., Angulo-Barturen, I., Kyle, D.E., de Risi, J.L., Floyd, D.M., Guy, R.K., 2014, (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium, Proceedings Of The National Academy Of Sciences Of The United States Of America [P], vol 111, issue 50, National Academy of Sciences, Washington DC USA, pp. e5455-e5462.

Cabrera, D.G., Le Manach, C., Douelle, F., Younis, Y., Feng, T., Paquet, T., Nchinda, A.T., Street, L.J., Taylor, D., de Kock, C., Wiesner, L., Duffy, S., White, K.L., Zabiulla, M.K., Sambandan, Y., Bashyam, S., Waterson, D., Witty, M.J., Charman, S.A., Avery, V.M., Wittlin, S., Chibale, K., 2014, 2,4-Diaminothienopyrimidines as orally active antimalarial agents, Journal of Medicinal Chemistry [P], vol 57, issue 3, American Chemical Society, Washington DC USA, pp. 1014-1022.

Bahia, M.T., Nascimento, A.F.S., Mazzeti, A.L., Marques, L.F., Goncalves, K.R., Mota, L.W.R., Diniz, L.d.F., Caldas, I.S., Talvani, A., Shackleford, D., Koltun, M., Saunders, J., White, K.L., Scandale, I., Charman, S.A., Chatelain, E., 2014, Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates for Chagas disease, Antimicrobial Agents And Chemotherapy [P], vol 58, issue 8, American Society for Microbiology, Washington DC USA, pp. 4362-4370.

Sundriyal, S., Malmquist, N.A., Caron, J., Blundell, S., Liu, F., Chen, X., Srimongkolpithak, N., Jin, J., Charman, S.A., Scherf, A., Fuchter, M.J., 2014, Development of diaminoquinazoline histone lysine methyltransferase inhibitors as potent blood-stage antimalarial compounds, Chemmedchem [P], vol 9, issue 10, Wiley - V C H Verlag GmbH & Co. KGaA, Weinheim Germany, pp. 2360-2373.

Nilsen, A., Miley, G.P., Forquer, I.P., Mather, M.W., Katneni, K., Li, Y., Pou, S., Pershing, A.M., Stickles, A.M., Ryan, E., Kelly, J.X., Doggett, J.S., White, K.L., Hinrichs, D.J., Winter, R.W., Charman, S.A., Zakharov, L.N., Bathurst, I.C., Burrows, J., Vaidya, A.B., Riscoe, M.K., 2014, Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers, Journal of Medicinal Chemistry [P], vol 57, issue 9, American Chemical Society, Washington DC USA, pp. 3818-3834.

Deng, X., Kokkonda, S., El Mazouni, F., White, J., Burrows, J., Kaminsky, W., Charman, S.A., Matthews, D., Rathod, P.K., Phillips, M.A., 2014, Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors, Journal of Medicinal Chemistry [P], vol 57, issue 12, American Chemical Society, Washington DC USA, pp. 5381-5394.

Le Manach, C., Cabrera, D.G., Douelle, F., Nchinda, A.T., Younis, Y., Taylor, D., Wiesner, L., White, K.L., Ryan, E., March, C., Duffy, S., Avery, V.M., Waterson, D., Witty, M.J., Wittlin, S., Charman, S.A., Street, L.J., Chibale, K., 2014, Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: Part 1, Journal of Medicinal Chemistry [P], vol 57, issue 6, American Chemical Society, Washington DC USA, pp. 2789-2798.

Cross, M., Flanigan, D.L., Monastyrskyi, A., LaCrue, A.N., Saenz, F.E., Maignan, J.R., Mutka, T.S., White, K.L., Shackleford, D., Bathurst, I.C., Fronczek, F.R., Wojtas, L., Guida, W.C., Charman, S.A., Burrows, J., Kyle, D.E., Manetsch, R., 2014, Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium, Journal of Medicinal Chemistry [P], vol 57, issue 21, American Chemical Society, Washington DC USA, pp. 8860-8879.

Vaidya, A.B., Morrisey, J.M., Zhang, Z., Das, S., Daly, T.M., Otto, T.D., Spillman, N.J., Wyvratt, M., Siegl, P., Marfurt, J., Wirjanata, G., Sebayang, B.F., Price, R.N., Chatterjee, A., Nagle, A.S., Stasiak, M., Charman, S.A., Angulo-Barturen, I., Ferrer, S.B., Jimenez-Diaz, M., Martinez, M.S., Gamo-Benito, F.J., Avery, V.M., Ruecker, A., Delves, M.J., Kirk, K., Berriman, M., Kortagere, S., Burrows, J., Fan, E., Bergman, L.W., 2014, Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum, Nature Communications [E], vol 5, issue 5521, Nature Publishing Group, London UK, pp. 1-10.

Ferrins, L., Gazdik, M., Rahmani, R.S., Varghese, S., Sykes, M.L., Jones, A.J., Avery, V.M., White, K.L., Ryan, E., Charman, S.A., Kaiser, M., Bergstrom, C.A.S., Baell, J.B., 2014, Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, Journal of Medicinal Chemistry [P], vol 57, issue 15, American Chemical Society, Washington DC USA, pp. 6393-6402.

Pouwer, R.H., Deydier, S.M., Le, P.V., Schwartz, B.D., Franken, N.C., Davis, R.A., Coster, M., Charman, S.A., Edstein, M.D., Skinner-Adams, T.S., Andrews, K.T., Jenkins, I.D., Quinn, R.J., 2014, Total synthesis of thiaplakortone A: Derivatives as metabolically stable leads for the treatment of malaria, A C S Medicinal Chemistry Letters [E], vol 5, issue 2, American Chemical Society, Washington DC USA, pp. 178-182.

Ferrins, L., Rahmani, R.S., Sykes, M.L., Jones, A.J., Avery, V.M., Teston, E., Almohaywi, B., Yin, J., Smith, J., Chris, H., White, K.L., Ryan, E., Campbell, M., Charman, S.A., Kaiser, M., Baell, J.B., 2013, 3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis, European Journal of Medicinal Chemistry [P], vol 66, Elsevier, Issy les Moulineaux France, pp. 450-465.

Carroux, C.J., Rankin, G.M., Moeker, J., Bornaghi, L.F., Katneni, K., Morizzi, J., Charman, S.A., Vullo, D., Supuran, C.T., Poulsen, S., 2013, A prodrug approach toward cancer-related carbonic anhydrase inhibition, Journal of Medicinal Chemistry [P], vol 56, issue 23, ACS Publications, Washington DC USA, pp. 9623-9634.

Wang, X., Dong, Y., Wittlin, S., Charman, S.A., Chiu, F.C.K., Chollet, J., Katneni, K., Mannila, J.M., Morizzi, J., Ryan, E., Scheurer, C., Steuten, J.A., Santo Tomas, J., Snyder, C., Vennerstrom, J., 2013, Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres, Journal of Medicinal Chemistry [P], vol 56, issue 6, ACS Publications, Washington DC USA, pp. 2547-2555.

Hargrove, T.Y., Wawrzak, Z., Alexander, P.W., Chaplin, J.H., Keenan, M., Charman, S.A., Perez, C., Waterman, M., Chatelain, E., Lepesheva, G.I., 2013, Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: Structural basis for pathogen selectivity, Journal Of Biological Chemistry [P], vol 288, issue 44, American Society for Biochemistry and Molecular Biology, Bethesda MD USA, pp. 31602-31615.

Keenan, M., Alexander, P.W., Diao, H., Best, W.M., Khong, A., Kerfoot, M., Thompson, R.C.A., White, K.L., Shackleford, D., Ryan, E., Gregg, A.D., Charman, S.A., von Geldern, T.W., Scandale, I., Chatelain, E., 2013, Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi, Bioorganic & Medicinal Chemistry [P], vol 21, issue 7, Pergamon-Elsevier, Oxford UK, pp. 1756-1763.

Murugesan, D., Mital, A., Kaiser, M., Shackleford, D., Morizzi, J., Katneni, K., Campbell, M., Hudson, A., Charman, S.A., Yeates, C., Gilbert, I.H., 2013, Discovery and structure-activity relationships of pyrrolone antimalarials, Journal of Medicinal Chemistry [P], vol 56, issue 7, ACS Publications, Washington DC USA, pp. 2975-2990.

Moehrle, J., Duparc, S., Siethoff, C., van Giersbergen, P.L.M., Craft, C.J., Arbe-Barnes, S., Charman, S.A., Gutierrez, M., Wittlin, S., Vennerstrom, J., 2013, First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials, British Journal Of Clinical Pharmacology [P], vol 75, issue 2, Wiley-Blackwell, Malden USA, pp. 535-548.

Schleiferbock, S., Scheurer, C., Ihara, M., Itoh, I., Bathurst, I.C., Burrows, J., Fantauzzi, P., Lotharius, J., Charman, S.A., Morizzi, J., Shackleford, D., White, K.L., Brun, R., Wittlin, S., 2013, In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models, Drug Design, Development and Therapy [E], vol 7, Dove Medical Press, Auckland New Zealand, pp. 1377-1384.

Nilsen, A., LaCrue, A.N., White, K.L., Forquer, I., Cross, M., Marfurt, J., Mather, M.W., Delves, M.J., Shackleford, D., Saenz, F.E., Morrisey, J.M., Steuten, J.A., Mutka, T., Li, Y., Wirjanata, G., Ryan, E., Duffy, S., Kelly, J.X., Sebayang, B.F., Zeeman, A., Noviyanti, R., Sinden, R.E., Kocken, C.H.M., Price, R.N., Avery, V.M., Angulo-Barturen, I., Jimenez-Diaz, M., Ferrer, S.B., Herreros, E., Sanz, L.M., Gamo, F., Bathurst, I.C., Burrows, J., Siegl, P., Guy, R.K., Winter, R.W., Vaidya, A.B., Charman, S.A., Kyle, D.E., Manetsch, R., Risco, M.K., 2013, Quinolone-3-diarylethers: A new class of antimalarial drug, Science Translational Medicine [P], vol 5, issue 177, American Association for the Advancement of Science, Washington DC USA, pp. 1-13.

Keenan, M., Alexander, P.W., Chaplin, J.H., Abbott, M.J., Diao, H., Wang, S.Z., Best, W.M., Perez, C., Cornwall, S.M., Keatley, S.K., Thompson, R.C.A., Charman, S.A., White, K.L., Ryan, E., Chen, G., Ioset, J.R., von Geldern, T.W., Chatelain, E., 2013, Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi, Future Medicinal Chemistry [P], vol 5, issue 15, Future Science, London UK, pp. 1733-1752.

Williams, H.D., Trevaskis, N., Charman, S.A., Shanker, R., Charman, W.N., Pouton, C.W., Porter, C.J., 2013, Strategies to address low drug solubility in discovery and development, Pharmacological Reviews [P], vol 65, issue 1, American Society for Pharmacology and Experimental Therapeutics, Bethesda MD USA, pp. 315-499.

Murugesan, D., Kaiser, M., White, K.L., Norval, S., Riley, J., Wyatt, P.G., Charman, S.A., Read, K.D., Yeates, C., Gilbert, I.H., 2013, Structure-activity relationship studies of pyrrolone antimalarial agents, Chemmedchem [P], vol 8, issue 9, Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim Germany, pp. 1537-1544.

Younis, Y., Douelle, F., Cabrera, D.G., Le Manach, C., Nchinda, A.T., Paquet, T., Street, L.J., White, K.L., Zabiulla, M.K., Joseph, J.T., Bashyam, S., Waterson, D., Witty, M.J., Wittlin, S., Charman, S.A., Chibale, K., 2013, Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity, Journal of Medicinal Chemistry [P], vol 56, issue 21, ACS Publications, Washington DC USA, pp. 8860-8871.

Carroux, C.J., Moeker, J., Motte, J., Lopez, M., Bornaghi, L.F., Katneni, K., Ryan, E., Morizzi, J., Shackleford, D., Charman, S.A., Poulsen, S., 2013, Synthesis of acylated glycoconjugates as templates to investigate in vitro biopharmaceutical properties, Bioorganic & Medicinal Chemistry Letters [P], vol 23, issue 2, Pergamon-Elsevier, Oxford UK, pp. 455-459.

Keenan, M., Chaplin, J.H., Alexander, P.W., Abbott, M.J., Best, W.M., Khong, A., Botero, A., Perez, C., Cornwall, S., Thompson, R.C.A., White, K.L., Shackleford, D., Koltun, M., Chiu, F.C.K., Morizzi, J., Ryan, E., Campbell, M., von Geldern, T.W., Scandale, I., Chatelain, E., Charman, S.A., 2013, Two analogues of fenarimol show curative activity in an experimental model of chagas disease, Journal of Medicinal Chemistry [P], vol 56, issue 24, ACS Publications, Washington DC USA, pp. 10158-10170.

Younis, Y., Douelle, F., Feng, T., Cabrera, D.G., Le Manach, C., Nchinda, A.T., Duffy, S., White, K.L., Shackleford, D., Morizzi, J., Mannila, J.M., Katneni, K., Bhamidipati, R., Zabiulla, M.K., Joseph, J.T., Bashyam, S., Waterson, D., Witty, M.J., Hardick, D., Wittlin, S., Avery, V.M., Charman, S.A., Chibale, K., 2012, 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential, Journal of Medicinal Chemistry [P], vol 55, issue 7, ACS Publications, Washington DC USA, pp. 3479-3487.

Keenan, M., Abbott, M.J., Alexander, P.W., Armstrong, T., Best, W.M., Berven, B., Botero, A., Chaplin, J.H., Charman, S.A., Chatelain, E., von Geldern, T.W., Kerfoot, M., Khong, A., Nguyen, T.T., McManus, J.D., Morizzi, J., Ryan, E., Scandale, I., Thompson, R.C.A., Wang, S.Z., White, K.L., 2012, Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of chagas disease, Journal of Medicinal Chemistry [P], vol 55, issue 9, ACS Publications, Washington DC USA, pp. 4189-4204.

Davis, R.A., Buchanan, M.S., Duffy, S., Avery, V.M., Charman, S.A., Charman, W.N., White, K.L., Shackleford, D., Edstein, M.D., Andrews, K., Camp, D.G., Quinn, R.J., 2012, Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp., Journal of Medicinal Chemistry [P], vol 55, issue 12, ACS Publications, Washington DC USA, pp. 5851-5858.

Zaloumis, S., Humberstone, A.J., Charman, S.A., Price, R.N., Moehrle, J., Gamo-Benito, J., McCaw, J., Jamsen, K., Smith, K., Simpson, J.A., 2012, Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development, Malaria Journal [P], vol 11, issue 303, BioMed Central, London UK, pp. 1-14.

Marwaha, A., White, J., El Mazouni, F., Creason, S., Kokkonda, S., Buckner, F.S., Charman, S.A., Phillips, M., Rathod, P., 2012, Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase, Journal of Medicinal Chemistry [P], vol 55, issue 17, ACS Publications, Washington DC USA, pp. 7425-7436.

Bergstrom, C.A.S., Charman, S.A., Nicolazzo, J., 2012, Computational prediction of CNS drug exposure based on a novel in vivo dataset, Pharmaceutical Research [P], vol 29, issue 11, Springer, New York USA, pp. 3131-3142.

Doggett, J.S., Nilsen, A., Forquer, I., Wegmann, K.W., Jones-Brando, L., Yolken, R.H., Bordon, C., Charman, S.A., Katneni, K., Schultz, T., Burrows, J., Hinrichs, D.J., Meunier, B., Carruthers, V.B., Risco, M.K., 2012, Endochin-like quinolones are highly efficacious against acute and latent experimental toxoplasmosis, Proceedings Of The National Academy Of Sciences Of The United States Of America [P], vol 109, issue 39, National Academies Press, Washington DC USA, pp. 15936-15941.

Yuthavong, Y., Tarnchompoo, B., Vilaivan, T., Chitnumsub, P., Kamchonwongpaisan, S., Charman, S.A., McLennan, D.N., White, K.L., Vivas, L., Bongard, E., Thongphanchang, C., Taweechai, S., Vanichtanankul, J., Rattanajak, R., Arwon, U., Fantauzzi, P., Yuvaniyama, J., Charman, W.N., Matthews, D., 2012, Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target, Proceedings of the National Academy of Sciences of the United States of America [E], vol 109, issue 42, National Academies Press, Washington DC USA, pp. 16823-16828.

Salmon, A.J., Williams, M.L., Wu, Q.K., Morizzi, J., Gregg, D.J., Charman, S.A., Vullo, D., Supuran, C.T., Poulsen, S., 2012, Metallocene-based inhibitors of cancer-associated carbonic anhydrase enzymes IX and XII, Journal of Medicinal Chemistry [P], vol 55, issue 11, ACS Publications, Washington DC USA, pp. 5506-5517.

Buckner, F.S., Bahia, M.T., Suryadevara, P.K., White, K.L., Shackleford, D., Chennamaneni, N.K., Hulverson, M.A., Laydbak, J.U., Chatelain, E., Scandale, I., Verlinde, C.L.M., Charman, S.A., Lepesheva, G.I., Gelb, M.H., 2012, Pharmacological characterization, structural studies, and in vivo activities of anti-chagas disease lead compounds derived from tipifarnib, Antimicrobial Agents And Chemotherapy [P], vol 56, issue 9, American Society for Microbiology, Washington DC USA, pp. 4914-4921.

Mannila, A.H., Morizzi, J., Nguyen, T.T., Charman, S.A., McIntosh, M.P., Shackleford, D., 2012, Probing a potential in vivo drug-excipient interaction: Temporal effects of a modified beta-cyclodextrin on the intravenous pharmacokinetics of a model high-affinity drug ligand, Journal of Pharmaceutical Sciences [P], vol 101, issue 9, Wiley-Blackwell, Malden, Massachusetts USA, pp. 3381-3389.

Cabrera, D.G., Douelle, F., Younis, Y., Feng, T., Le Manach, C., Nchinda, A.T., Street, L.J., Scheurer, C., Kamber, J., White, K.L., Montagnat, O.D., Ryan, E., Katneni, K., Zabiulla, M.K., Joseph, J.T., Bashyam, S., Waterson, D., Witty, M.J., Charman, S.A., Wittlin, S., Chibale, K., 2012, Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines, Journal of Medicinal Chemistry [P], vol 55, issue 24, ACS Publications, Washington DC, USA, pp. 11022-11030.

Kooijmans, S.A.A., Senyschyn, D., Mezhiselvam, M.M., Morizzi, J., Charman, S.A., Weksler, B., Romero, I., Couraud, P., Nicolazzo, J., 2012, The involvement of a Na+ - and Cl- -dependent transporter in the brain uptake of amantadine and rimantadine, Molecular Pharmaceutics [P], vol 9, ACS Publications, United States, pp. 883-893.

Ndakala, A., Gessner, R., Gitari, P., October, N., White, K., Hudson, A., Fakorede, F., Shackleford, D., Kaiser, M., Yates, C., Charman, S., Chibale, K., 2011, Antimalarial Pyrido[1,2-a]benzimidazoles, Journal of Medicinal Chemistry [P], vol 54, ACS Publications, USA, pp. 4581-4589.

Dow, G., Milner, E., Bathurst, I., Bhonsle, J., Caridha, D., Gardner, S., Gerena, L., Kozar, M., Lanteri, C., Mannila, A., McCalmont, W., Moon, J., Read, K., Norval, S., Roncal, N., Shackleford, D., Sousa, J., Steuten, J., White, K., Zeng, Q., Charman, S., 2011, Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice, Malaria Journal [P], vol 10, issue 150, BioMed Central, United Kingdom, pp. e1-e11.

Flynn, B., Gurmit, G., Grobelny, D., Chaplin, J., Paul, D., Leske, A., Lavranos, T., Chalmers, D., Charman, S., Kostewicz, E., Shackleford, D., Morizzi, J., Hamel, E., Jung, K., Kremmidiotis, G., 2011, Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties, Journal of Medicinal Chemistry [P], vol 54, issue 17, ACS Publications, USA, pp. 6014-6027.

Gujjar, R., El Mazouni, F., White, K., White, J., Creason, S., Shackleford, D., Deng, X., Charman, W., Bathurst, I., Burrows, J., Floyd, D., Matthews, D., Buckner, F., Charman, S., Phillips, M., Rathod, P., 2011, Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice, Journal of Medicinal Chemistry [P], vol 54, ACS Publications, USA, pp. 3935-3949.

Cabera, D., Douelle, F., Feng, T., Nchinda, A., Younis, Y., White, K., Wu, Q., Ryan, E., Burrows, J., Waterson, D., Witty, M., Wittlin, S., Charman, S., Chibale, K., 2011, Novel orally active antimalarial thiazoles, Journal of Medicinal Chemistry [P], vol 54, ACS Publications, USA, pp. 7713-7719.

Coteron, J., Marco, M., Esquivias, J., Deng, X., White, K., White, J., Koltun, M., El Mazouni, F., Kokkonda, S., Katneni, K., Bhamidipati, R., Shackleford, D., Angulo-Barturen, I., Ferrer, S., Jimenez-Diaz, M., Gamo, F., Goldsmith, E., Charman, W., Bathurst, I., Floyd, D., Matthews, D., Burrows, J., Rathod, P., Charman, S., Phillips, M., 2011, Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential, Journal of Medicinal Chemistry [P], vol 54, issue 15, ACS Publications, USA, pp. 5540-5561.

Charman, S., Arbe-Barnes, S., Bathurst, I., Brun, R., Campbell, M., Charman, W., Chiu, F., Chollet, J., Craft, C., Creek, D., Dong, Y., Matile, H., Maurer, M., Morizzi, J., Nguyen, T., Papastogiannidis, P., Scheurer, C., Shackleford, D., Sriraghavan, K., Stingelin, L., Tang, Y., Urwyler, H., Wang, X., White, K., Wittlin, S., Zhou, L., Vennerstrom, J., 2011, Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria, Proceedings Of The National Academy Of Sciences Of The United States Of America [P], vol 108, issue 11, National Academies Press, Washington D.C., USA, pp. 4400-4405.

Nicolazzo, J., Steuten, J.A., Charman, S.A., Taylor, N., Davies, P., Petrou, S., 2010, Brain uptake of diazepam and phenytoin in a genetic animal model of absence epilepsy, Clinical And Experimental Pharmacology And Physiology [P], vol 37, Blackwell's, Australia, pp. 647-649.

Ge, J., Arai, C., Yang, M., Bakar, A., Lu, J., Ismail, N.S.M., Wittlin, S., Kaiser, M., Brun, R., Charman, S.A., Nguyen, T., Morizzi, J., Itoh, I., Ihara, M., 2010, Discovery of novel benzo[ a ]phenoxazine SSJ-183 as a drug candidate for malaria, A C S Medicinal Chemistry Letters [E], vol 1, issue 7, ACS Publications, United States, pp. 360-364.

Koltun, M., Morizzi, J., Katneni, K., Charman, S.A., Shackleford, D., McIntosh, M.P., 2010, Preclinical comparison of intravenous melphalan pharmacokinetics administered in formulations containing either (SBE)7m-beta-cyclodextrin or a co-solvent system, Biopharmaceutics and Drug Disposition [E], vol 31, issue 8-9, John Wiley & Sons, online, pp. 450-454.

Lopez, M., Bornaghi, L.F., Innocenti, A., Vullo, D., Charman, S.A., Supuran, C.T., Poulsen, S., 2010, Sulfonamide linked neoglycoconjugates-A new class of inhibitors for cancer-associated carbonic anhydrases, Journal of Medicinal Chemistry [P], vol 53, ACS Publications, USA, pp. 2913-2926.

Johnstone, K.D., Karoli, T., Liu, L., Dredge, K., Copeman, E., Li, C.P., Davis, K., Hammond, E., Bytheway, I., Kostewicz, E.S., Chiu, F.C.K., Shackleford, D., Charman, S.A., Charman, W.N., Harenberg, J., Gonda, T., Ferro, V., 2010, Synthesis and Biological Evaluation of Polysulfated Oligosaccharide Glycosides as Inhibitors of Angiogenesis and Tumor Growth, Journal of Medicinal Chemistry [P], vol 53, issue 4, ACS Publications, USA, pp. 1686-1699.

Tang, Y., Wittlin, S., Charman, S.A., Chollet, J., Chiu, F.C.K., Morizzi, J., Johnson, L., Santo Tomas, J., Scheurer, C., Snyder, C., Zhou, L., Dong, Y., Charman, W.N., Matile, H., Urwyler, H., Dorn, A., Vennerstrom, J., 2010, The comparative antimalarial properties of weak base and neutral synthetic ozonides, Bioorganic & Medicinal Chemistry Letters [P], vol 20, issue 2, Pergamon, UK, pp. 563-566.

Dong, Y., Wittlin, S., Sriraghavan, K., Chollet, J., Charman, S.A., Charman, W.N., Scheurer, C., Urwyler, H., Santo Tomas, J., Snyder, C., Creek, D.J., Morizzi, J., Koltun, M., Matile, H., Wang, X., Padmanilayam, M., Tang, Y., Dorn, A., Brun, R., Vennerstrom, J., 2010, The structure - activity relationship of the antimalarial ozonide arterolane (OZ277), Journal of Medicinal Chemistry [P], vol 53, ACS Publications, USA, pp. 481-491.

Saltiel, J., Smothers, W.K., Schanze, K.S., Charman, S.A., Bonneau, R., 2009, 2,5-Dimethyl-2,4-hexadiene induced photodechlorination of 9,10-dichloroanthracene, Photochemical & Photobiological Sciences [P], vol 8, issue 6, RSC Publishing, UK, pp. 856-867.

Burns, C., Fantino, E., Phillips, I.D., Su, S., Harte, M., Bukczynska, P.E., Frazzetto, M., Joffe, M., Kruszelnicki, I., Wang, B., Wang, Y., Wilson, N., Dilley, R.J., Wan, S.S., Charman, S.A., Shackleford, D., Fida, R., Malcontenti-Wilson, C., Wilks, A.F., 2009, CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo, Molecular Cancer Therapeutics [P], vol 8, issue 11, American Association for Cancer Research, USA, pp. 3036-3045.

Burns, C., Harte, M., Bu, X., Fantino, E., Joffe, M., Sikanyika, H., Su, S., Tranberg, C., Wilson, N., Charman, S.A., Shackleford, D., Wilks, A.F., 2009, Discovery of CYT997: a structurally novel orally active microtubule targeting agent, Bioorganic & Medicinal Chemistry Letters [P], vol 19, issue 16, Pergamon, UK, pp. 4639-4642.

Gujjar, R., Marwaha, A., El Mazouni, F., White, J., White, K.L., Creason, S., Shackleford, D., Baldwin, J., Charman, W.N., Buckner, F.S., Charman, S.A., Rathod, P., Phillips, M., 2009, Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice, Journal of Medicinal Chemistry [P], vol 52, issue 7, ACS Publications, USA, pp. 1864-1872.

Burns, C., Bourke, D.G., Andrau, L., Bu, X., Charman, S.A., Donohue, A.C., Fantino, E., Farrugia, M., Feutrill, J.T., Joffe, M., Kling, R.M., Kurek M., Nero, T.L., Nguyen, T., Palmer, J.T., Phillips, I.D., Shackleford, D., Sikanyika, H., Styles, M., Su, S., Treutlein, H., Zeng, J., Wilks, A.F., 2009, Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs), Bioorganic & Medicinal Chemistry Letters [P], vol 19, issue 20, Pergamon, UK, pp. 5887-5892.

Bhamidipati, R.K., Morizzi, J., Chiu, F.C.K., Shackleford, D., Charman, S.A., 2009, Simultaneous determination of OZ277, a synthetic 1,2,4-trioxolane antimalarial, and its polar metabolites in rat plasma using hydrophilic interaction chromatography, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences [P], vol 877, issue 27, Elsevier, The Netherlands, pp. 2989-2995.

Wang, X., Creek, D.J., Schiaffo, C.E., Dong, Y., Chollet, J., Scheurer, C., Wittlin, S., Charman, S.A., Dussault, P.H., Wood, J.K., Vennerstrom, J., 2009, Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: Relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity, Bioorganic & Medicinal Chemistry Letters [P], vol 19, issue 16, Elsevier, The Netherlands, pp. 4542-4545.

Creek, D.J., Ryan, E., Charman, W.N., Chiu, F.C.K., Prankerd, R., Vennerstrom, J., Charman, S.A., 2009, Stability of peroxide antimalarials in the presence of human hemoglobin, Antimicrobial Agents And Chemotherapy [P], vol 53, issue 8, American Society for Microbiology, USA, pp. 3496-3500.

Katneni, K., Charman, S.A., Porter, C.J., 2008, An evaluation of the relative roles of the unstirred water layer and receptor sink in limiting the in-vitro intestinal permeability of drug compounds of varying lipophilicity, Journal of Pharmacy and Pharmacology, vol 60, issue 10, Wiley-Blackwell, UK, pp. 1311-1319.

Zhou, L., Alker, A., Ruf, A., Wang, X., Chiu, F.C.K., Morizzi, J., Charman, S.A., Charman, W.N., Scheurer, C., Wittlin, S., Dong, Y., Hunziker, D., Vennerstrom, J., 2008, Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277, Bioorganic and Medicinal Chemistry Letters, vol 18, issue 5, Pergamon, UK, pp. 1555-1558.

Nicolazzo, J., Nguyen, T.T., Katneni, K., Steuten, J.A., Smith, G.D., Jarrott, B., Callaway, J.K., Charman, S.A., 2008, Pharmacokinetics and brain uptake of AM-36, a novel neuroprotective agent, following intravenous administration to rats, Journal of Pharmacy and Pharmacology, vol 60, issue 2, Wiley-Blackwell, UK, pp. 171-178.

Adlard, P.A., Cherny, R.A., Finklestein, D.I., Gautier, E., Robb, E., Cortes, M., Volitakis, I., Liu, X., Smith, J.P., Perez, K., Laughton, K.M., Lin, Q., Charman, S.A., Nicolazzo, J., Wilkins, S.J., Deleva, K., Lynch, T., Kok, G., Ritchie, C.W., Tanzi, R.E., Cappai, R., Masters, C.L., Barnham, K.J., Bush, A.I., 2008, Rapid restoration of cognition in alzheimer's transgenic mice with 8-hydroxy quinoline analogs is associated with decreased interstitial Abeta, Neuron, vol 59, Elsevier, USA, pp. 43-55.

Creek, D.J., Charman, W.N., Chiu, F.C.K., Prankerd, R.J., Dong, Y., Vennerstrom, J., Charman, S.A., 2008, Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials, Antimicrobial Agents and Chemotherapy, vol 52, issue 4, American Society for Microbiology, USA, pp. 1291-1296.

Katneni, K., Charman, S.A., Porter, C.J., 2008, Use of plasma proteins as solubilizing agents in in vitro permeability experiments: correction for unbound drug concentration using the reciprocal permeability approach, Journal of Pharmaceutical Sciences, vol 97, issue 1, John Wiley & Sons, USA, pp. 209-224.

Dong, Y., Creek, D.J., Chollet, J., Matile, H., Charman, S.A., Wittlin, S., Woods, J.H., Vennerstrom, J., 2007, Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers), Antimicrobial Agents and Chemotherapy, vol 51, issue 8, America Society for Microbiology, Unites States, pp. 3033-3035.

Katneni, K., Charman, S.A., Porter, C.J., 2007, Impact of cremophor-El and polysorbate-80 on digoxin permeability across rat jejunum: delineation of thermodynamic and transporter related events using the reciprocal permeability approach, Journal of Pharmaceutical Sciences, vol 96, issue 2, Wiley-Liss Inc, USA, pp. 280-293.

Creek, D.J., Charman, W.N., Chiu, F.C.K., Prankerd, R.J., McCullough, K.J., Dong, Y., Vennerstrom, J., Charman, S.A., 2007, Iron-mediated degradation kinetics of substituted dispiro-1,2,4-trioxolane antimalarials, Journal of Pharmaceutical Sciences, vol 96, issue 11, Wiley-Liss Inc, New Jersey, United States, pp. 2945-2956.

Kota, J., Machavaram, K.K., McLennan, D.N., Edwards, G.A., Porter, C.J., Charman, S.A., 2007, Lymphatic absorption of subcutaneously administered proteins: influence of different injection sites on the absorption of darbepoetin alfa using a sheep model, Drug Metabolism and Disposition, vol 35, issue 12, American Society for Pharmacology and Experimental Therapeutics, US, pp. 2211-2217.

Wang, X., Dong, Y., Wittlin, S., Creek, D., Chollet, J., Charman, S.A., Santo Tomas, J., Scheurer, C., Snyder, C., Vennerstrom, J., 2007, Spiro- and dispiro-1,2-dioxolanes: contribution of iron(II)-mediated one-electron vs two-electron reduction to the activity of antimalarial peroxides, Journal of Medicinal Chemistry, vol 50, issue 23, American Chemical Society, USA, pp. 5840-5847.

Tang, Y., Dong, Y., Wittlin, S., Charman, S.A., Chollet, J., Chiu, F.C.K., Charman, W.N., Matile, H., Urwyler, H., Dorn, A., Bajpai, S., Wang, X., Padmanilayam, M., Karle, J.M., Brun, R., Vennerstrom, J., 2007, Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides, Bioorganic & Medicinal Chemistry Letters, vol 17, issue 5, Elsevier, UK, pp. 1260-1265.

Charman, S.A., Perry, C.S., Chiu, F.C.K., McIntosh, K.A., Prankerd, R.J., Charman, W.N., 2006, Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin, Journal of Pharmaceutical Sciences, vol 95, issue 2, John Wiley & Sons Inc., USA, pp. 256-267.

Padmanilayam, M., Scorneaux, B., Dong, Y., Chollet, J., Matile, H., Charman, S.A., Creek, D.J., Charman, W.N., Santo Tomas, J., Scheurer, C., Wittlin, S., Brun, R., Vennerstrom, J., 2006, Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine, Bioorganic & Medicinal Chemistry Letters, vol 16, issue 21, Pergamon, UK, pp. 5542-5545.

Perry, C.S., Charman, S.A., Prankerd, R.J., Chiu, F.C.K., Dong, Y., Vennerstrom, J.L., Charman, W.N., 2006, Chemical kinetics and aqueous degradation pathways of a new class of synthetic ozonide antimalarials, Journal of Pharmaceutical Sciences, vol 95, issue 4, John Wiley & Sons, Inc., USA, pp. 737-747.

Dong, Y., Tang, Y., Chollet, J., Matile, H., Wittlin, S., Charman, S.A., Charman, W.N., Santo Tomas, J., Scheurer, C., Snyder, C., Scorneaux, B., Bajpai, S., Alexander, S.A., Wang, X., Padmanilayam, M., Cheruku, S.R., Brun, R., Vennerstrom, J.L., 2006, Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes, Bioorganic & Medicinal Chemistry, vol 14, issue 18, Pergamon, UK, pp. 6368-6382.

Maerki, S., Brun, R., Charman, S.A., Dorn, A., Matile, H., Wittlin, S., 2006, In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum, Journal of Antimicrobial Chemotherapy, vol 58, issue 1, Oxford University Press, UK, pp. 52-58.

Nicolazzo, J.A., Charman, S.A., Charman, W.N., 2006, Methods to assess drug permeability across the blood-brain barrier, Journal of Pharmacy and Pharmacology, vol 58, issue 3, Pharmaceutical Press, UK, pp. 281-293.

Katneni, K., Charman, S.A., Porter, C.J.H., 2006, Permeability assessment of poorly water-soluble compounds under solubilizing conditions: the reciprocal permeability approach, Journal of Pharmaceutical Sciences, vol 95, issue 10, John Wiley & Sons, Inc, USA, pp. 2170-2185.

McLennan, D.N., Porter, C.J.H., Edwards, G.A., Heatherington, A.C., Martin, S.W., Charman, S.A., 2006, The absorption of darbepoetin alfa occurs predominantly via the lymphatics following subcutaneous administration to sheep., Pharmaceutical Research, vol 23, issue 9, Springer New York LLC, USA, pp. 2060-2066.

Perry, C.S., Charman, S.A., Prankerd, R.J., Chiu, F.C.K., Scanlon, M.J., Chalmers, D.K., Charman, W.N., 2006, The binding interaction of synthetic ozonide antimalarials with natural and modified beta-cyclodextrins, Journal of Pharmaceutical Sciences, vol 95, issue 1, John Wiley & Sons, Inc., USA, pp. 146-158.

Creek, D.J., Chiu, F.C.K., Prankerd, R.J., Charman, S.A., Charman, W.N., 2005, Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt, Journal of Pharmaceutical Sciences, vol 94, issue 8, John Wiley & Sons, Inc., USA, pp. 1820-1829.

McLennan, D.N., Porter, C.J.H., Edwards, G.A., Martin, S.W., Heatherington, A.C., Charman, S.A., 2005, Lymphatic absorption is the primary contributor to the systemic availability of epoetin alfa following subcutaneous administration to sheep, The Journal of Pharmacology and Experimental Therapeutics, vol 313, issue 1, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 345-351.

Dong, Y., Chollet, J., Matile, H., Charman, S.A., Chiu, F.C.K., Charman, W.N., Scorneaux, B., Urwyler, H., Santo Tomas, J., Scheurer, C., Snyder, C., Dorn, A., Wang, X., Karle, J.M., Tang, Y., Wittlin, S., Brun, R., Vennerstrom, J.L., 2005, Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes, Journal of Medicinal Chemistry, vol 48, issue 15, American Chemical Society, USA, pp. 4953-4961.

McLennan, D.N., Porter, C.J.H., Charman, S.A., 2005, Subcutaneous drug delivery and the role of the lymphatics, Drug Discovery Today: Technologies, vol 2, issue 1, Elsevier Ltd., Trends Journals, The Netherlands, pp. 89-96.

Vennerstrom, J.L., Arbe-Barnes, S., Brun, R., Charman, S.A., Chiu, F.C.K., Chollet, J., Dong, Y., Dorn, A., Hunziker, D., Matile, H., McIntosh, K.A., Padmanilayam, M., Santo Tomas, J., Scheurer, C., Scorneaux, B., Tang, Y., Urwyler, H., Wittlin, S., Charman, W.N., 2004, Identification of an antimalarial synthetic trioxolane drug development candidate, Nature, vol 430, issue 7002, Nature Publishing group, UK, pp. 900-904.

Segrave, A.M., Mager, D.E., Charman, S.A., Edwards, G.A., Porter, C.J.H., 2004, Pharmacokinetics of recombinant human leukemia inhibitory factor in sheep, The Journal of Pharmacology and Experimental Therapeutics, vol 309, issue 3, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 1085-1092.

McLennan, D.N., Porter, C.J.H., Edwards, G.A., Brumm, M., Martin, S.W., Charman, S.A., 2003, Pharmacokinetic model to describe the lymphatic absorption of r-metHu-Leptin after subcutaneous injection to sheep, Pharmaceutical Research, vol 20, issue 8, Kluwer Academic/ Plenum Publishers, USA, pp. 1156-1162.

Vine, D.F., Charman, S.A., Gibson, P.R., Sinclair, A.J., Porter, C., 2002, Effect of dietary fatty acids on the intestinal permeability of marker drug compounds in excised rat jejunum, Journal of Pharmacy and Pharmacology, vol 54, issue 6, Pharmaceutical Press, UK, pp. 809-819.

Vine, D.F., Charman, S.A., Gibson, P.R., Sinclair, A.J., Porter, C.J.H., 2002, Effect of dietary fatty acids on the intestinal permeability of marker drug compounds in excised rat jejunum, Journal of Pharmacy and Pharmacology, vol 54, issue 6, Pharmaceutical Press Royal Pharmaceutical Soc Great Britain, UK, pp. 1-11.

Charman, S.A., McLennan, D.N., Edwards, G.A., Porter, C.J.H., 2001, Lymphatic absorption is a significant contributor to the subcutaneous bioavailability of insulin in a sheep model, Pharmaceutical Research, vol 18, issue 11, Kluwer Academic - Plenum Publishers, USA, pp. 1620-1626.

Porter, C., Edwards, G.A., Charman, S.A., 2001, Lymphatic transport of proteins after s.c. injection: implications of animal model selection, Advanced Drug Delivery Reviews, vol 50, Elsevier Science BV, The Netherlands, pp. 157-171.

Porter, C.J.H., Charman, S.A., 2000, Lymphatic transport of proteins after subcutaneous administration, Journal of Pharmaceutical Sciences, vol 89 issue 3, John Wiley & Sons Inc, New York NY USA, pp. 297-310.

Charman, S.A., Segrave, A., Edwards, G.A., Porter, C.J.H., 2000, Systemic availability and lymphatic transport of human growth hormone administered by subcutaneous injection, Journal of Pharmaceutical Sciences, vol 89 issue 2, John Wiley & Sons Inc, New York NY USA, pp. 168-177.

Krise, J.P., Charman, W.N., Charman, S.A., Stella, V.J., 1999, A novel prodrug approach for tertiary amines.3. In vivo evaluation of two N-phosphonocoxymethyl prodrugs in rats and dogs, Journal of Pharmaceutical Sciences, vol 88 issue 9, ACS & Am Pharm Assoc, Washington USA, pp. 928-932.

Charman, W.N., Chan, H., Finnin, B.C., Charman, S.A., 1999, Drug delivery: A key factor in realising the full therapeutic potential of drugs, Drug Development Research, vol 46 issue 3-4, Wiley-Liss, New York NY USA, pp. 316-327.

Simon, L.D., Stella, V.J., Charman, W.N., Charman, S.A., 1999, Mechanisms controlling diffusion and release of model proteins through and from partially esterified hyaluronic acid membranes, Journal of Controlled Release, vol 61 issue 3, Elsevier Science, Netherlands, pp. 267-279.

Simon, L.D., Stella, V.J., Charman, W.N., Charman, S.A., 1999, Variation in the diffusion and release of ribonuclease through and from esterified hyaluronic acid membranes: Effect of changes in matrix characteristics, Journal of Controlled Release, vol 61 issue 1-2, Elsevier Science, Netherlands, pp. 159-164.

McIntosh, K.A., Charman, S.A., Borgen, L.A., Charman, W.N., 1998, Analytical methods and stability assessment of liquid yeast derived sucrase, Journal of Pharmaceutical and Biomedical Analysis, vol 17, Elsevier Science, USA, pp. 1037-1045.

McCrossin, L.E., Charman, W.N., Charman, S.A., 1998, Degradation of recombinant porcine growth hormone in the presence of guanidine hydrochloride, International Journal of Pharmaceutics, vol 173, Elsevier Science, UK, pp. 157-170.

McIntosh, K.A., Charman, W.N., Charman, S.A., 1998, The application of capillary electrophoresis for monitoring effects of excipients on protein conformation, Journal of Pharmaceutical and Biomedical Analysis, vol 16, Elsevier Science, USA, pp. 1097-1105.

Simon, L.D., Charman, W.N., Charman, S.A., Stella, V.J., 1997, Protein transport across hydrated hyaluronic acid ester membranes: Evaluation of ribonuclease A as a potentially useful model protein, Journal of Controlled Release, vol 45, Elsevier, Ireland, pp. 273-285.

Conference Proceedings

McIntosh, K.A., Charman, W.N., Charman, S.A., 1999, A modified ussing chamber model for the evaluation of rhGH transepithelial absorption, AAPS PharmSci Supplement, 14 November 1999 to 18 November 1999, American Association of Pharmaceutical Sciences, USA, p. S-421.

Thomas, B.J., McIntosh, M.P., Kannar, D., Charman, S.A., Charman, W.N., 1999, In vitro distribution of coenzyme Q10 in plasma lipoproteins, AAPS PharmSci Supplement, 14 November 1999 to 18 November 1999, American Association of Pharmaceutical Sciences, USA, p. S-124.

Smith, G.D., Zhou, J., Marcuccio, S., Robertson, A.D., Charman, W.N., Charman, S.A., 1999, Oral absorptionn of nucleoside analogue prodrugs II.Physio cochemical properties and Invitro intestinal permeabilities, AAPS PharmSci Supplement, 14 November 1999 to 18 November 1999, American Association of Pharmaceutical Sciences, USA, p. S-645.

Smith, G.D., Bloodworth, T., Marcuccio, S., Robertson, A.D., Charman, W.N., Charman, S.A., 1999, Oral asorption of nucleoside analogue prodrus I.Invivo bioavailabiliy assessment, AAPS PharmSci Supplement, 14 November 1999 to 18 November 1999, American Association of Pharmaceutical Sciences, USA, p. S-641.

Zhou, J., Smith, G.D., Charman, S.A., 1999, Relationship between physicochemical properties, in vitro intestinal permeability and oral bioavailability for nucleoside analogue prodrugs, Proceedings of the Australasian Pharmaceutical Science Association, 28 November 1999 to 1 December 1999, Curtin University of Technology, Perth WA Australia, p. 68.

McIntosh, K.A., Charman, W.N., Milstein, S., Charman, S.A., 1998, Development and validation of an in vitro model to measure the intestinal permeability of potential oral formulations of human growth hormone, Proceedings of ASCEPT: Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Australasian Soc of Clinical & Exp Pharm & Toxicol, Sydney NSW Australia, p. 97.

Porter, C.J.H., Segrave, A., Kossena, G., Edwards, G.A., Charman, S.A., 1998, Does lymphatic transport limit the systemic blood availability of human growth hormone (hGH) after S.C. injection?, AAPS PharmSci? Supplement, 15 November 1998 to 19 November 1998, American Association of Pharmaceutical Scientists, Virginia USA, p. S335.

Smith, G.D., Robertson, A.D., Charman, W.N., Charman, S.A., 1998, Plasma pharmacokinetics and brain penetration of AM36, a novel neuroprotective compound in the rat, AAPS PharmSci? Supplement, 15 November 1998 to 19 November 1998, American Association of Pharmaceutical Scientists, Virginia USA, p. S678.

Charman, S.A., Smith, G.D., Robertson, A.D., Bloodworth, T., Marcuccio, S., Charman, W.N., 1998, Prodrugs of nucleoside analogues I: Oral bioavailability in the rat, Proceedings of ASCEPT: Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Australasian Soc of Clinical & Exp Pharm & Toxicol, Sydney NSW Australia, p. 94.

Bawden, A., Smith, G.D., Robertson, A.D., Marcuccio, S., Charman, W.N., Charman, S.A., 1998, Prodrugs of nucleoside analogues II: In vitro permeability in excised rat jejunum, Proceedings of ASCEPT: Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Australasian Soc of Clinical & Exp Pharm & Toxicol, Sydney NSW Australia, p. 95.

Charman, S.A., Hill, J.M., Radford, A.J., 1998, Stability studies for solution formulations of leukemia inhibitory factor (LIF), AAPS PharmSci? Supplement, 15 November 1998 to 19 November 1998, American Association of Pharmaceutical Scientists, Virginia USA, p. S536.

Krise, J.P., Charman, W.N., Charman, S.A., Narisawa, S., Zygmunt, J., Stella, V.J., 1998, Synthesis and evaluation of a novel prodrug for increasing the water solubility of tertiary amine-containing drugs, AAPS PharmSci? Supplement, 15 November 1998 to 19 November 1998, American Association of Pharmaceutical Scientists, Virginia USA, p. S99.

Smith, G.D., Robertson, A.D., Hill, J.M., Charman, W.N., Charman, S.A., 1998, The D log D parameter as a correlate of the brain penetration of a series novel neuroprotective compounds in the rat, Proceedings of ASCEPT: Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Australasian Soc of Clinical & Exp Pharm & Toxicol, Sydney NSW Australia, p. 94.

Hill, J.M., Radford, A.J., Charman, S.A., 1997, Preliminary stability studies for solution formulations of an investigational protein, Australasian Pharmaceutical Science Association 1997 Conference, 26 November 1997 to 28 November 1997, APSA 1997 Organising Committee, Sydney NSW Australia, p. 70.

Krise, J.P., Charman, W.N., Charman, S.A., Stella, V.J., 1997, Synthesis, physiochemical and biological evaluation of a novel prodrug for increasing the water solubility of tertiary amine-containing drug, Australasian Pharmaceutical Science Association 1997 Conference, 26 November 1997 to 28 November 1997, APSA 1997 Organising Committee, Sydney NSW Australia, p. 71.

Other

Charman, W.N., Charman, S.A., McNamara, K.P., 2012, Stabilized growth hormone formulation and method of preparation thereof, Canada.

Tarnchompoo, B., Yuthavong, Y., Vilaivan, T., Chitnumsub, P., Thongpanchang, C., Kamchonwongpaisan, S., Matthews, D., Vivas, L., Yuvaniyama, J., Charman, S.A., Charman, W.N., Babu Katiyar, S., 2009, Antimalarial compounds with flexible side chains, USA.

Phillips, M., Rathod, P., Gujjar, R., Marwaha, A., Charman, S.A., 2009, Dihydrooratate dehydrogenase inhibitors with selective antimalarial activity., USA.

Vennerstrom, J., Dong, Y., Charman, S.A., Wittlin, S., Chollet, J., Creek, D., Wang, X., Sriraghavan, K., Zhou, L., Matile, H., Charman, W.N., 2009, Dispiro 1,2,4-trioxolane antimalarials, USA.

Vennerstrom, J., Dong, Y., Charman, S.A., Wittlin, S., Chollet, J., Wang, X., Spiraghavan, K., Zhou, L., Matile, H., Charman, W.N., 2009, Spiro and dispiro 1,2,4-trioxolane antimalarials, United States of America.

Charman, W., Charman, S., McNamara, M., 2009, Stabilized growth hormone formulation and method of preparation thereof (Japan), Japan.

Charman, S.A., Radford, A.J., 2006, Compositions of Leukemia Inhibitory Factor, USA.

McNamara, M.K., Charman, W.N., Charman, S.A., 2006, Stabilised growth hormone formulation and method of preparation thereof.

McNamara, M.K., Charman, W.N., Charman, S.A., 2003, Stabilized growth hormone formulation and method of preparation thereof, USA.

Activities

Affiliations with research centres

Theme Leader
Centre for Drug Candidate Optimisation
Monash Institute of Pharmaceutical Sciences

Other committees

Member
Pharmaceutical Industry Working Group, Australia

Grants

Title:
Rational design of new drug candidates for the treatment of Trypanosoma cruzi infection.
Investigators:
Charman, S, Thompson, R, Keenan, M, Best, W, Khong, A, Chatelain, E
Funding:
(2011 - 2013). Australian Research Council (ARC) [arc, AUS, ACT]. $245,538.00
(2011 - 2013). Australian Research Council (ARC) [arc, AUS, ACT]. $598,000.00
(2011 - 2013). DNDi Drugs for Neglected Diseases Initiative [dndi, CHE, GE]. $1,164,647.00
(2011 - 2013). Epichem [epichem, AUS, VIC]. $0.00
(2011 - 2013). Murdoch University [murdoch, AUS, WA]. -$358,727.00
Title:
Development of small molecules for the treatment of colon cancer.
Investigators:
Charman, S, Lessene, G, Burgess, A, Baell, J, Walker, F, Garrett, T
Funding:
(2011 - 2013). National Health & Medical Research Council (NHMRC) [nhmrc, AUS, ACT]. $74,006.00
Title:
Inhibition of membrane-bound carbonic anhydrases with small molecules as a novel approach to target a safe and effective treatment for solid tumours.
Investigators:
Charman, S, Poulson, S, Supuran, C, Pouyssegur, J
Funding:
(2011 - 2013). Australian Research Council (ARC) [arc, AUS, ACT]. $45,000.00
Title:
NHMRC Standard Equipment Grant - 2007.
Investigators:
Nation, R, McIntosh, M, Li, J, Charman, S, Nicolazzo, J, Taylor, D, Boyd, B, Broadbear, J
Funding:
(2008). National Health & Medical Research Council (NHMRC) [nhmrc, AUS, ACT]. $72,500.00
Title:
Development of therapeutic agents that target carbonic anhydrase enzymes.
Investigators:
Charman, S, Poulsen, S, Supuran, C, Parsons, P
Funding:
(2009 - 2010). Australian Research Council (ARC) [arc, AUS, ACT]. $22,500.00
Title:
Optimizing Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Malaria.
Investigators:
Charman, S, Charman, W
Funding:
(2007 - 2012). Medicines for Malaria Venture [mmv, CHE, GE]. $1,575,135.21

Postgraduate Research Supervisions

Current Supervision

Program of Study:
(DOCTORATE BY RESEARCH).
Thesis Title:
Systems pharmacology understanding the mechanism of action and resistance for peroxide antimalarials.
Supervisors:
Creek, D (Main), Charman, S (Associate).

Completed Supervision

Student:
Bhamidipati, R.
Program of Study:
Basis for the dose-dependent systemic clearance of a novel 1,2,4-trioxolane antimalarial, OZ277, in rats. (PHD) 2009.
Supervisors:
Charman, S (Main), Charman, W (Associate).
Student:
Creek, D.
Program of Study:
Iron-mediated reactivity of peroxide antimalarials. (PHD) 2007.
Supervisors:
Charman, S (Main), Charman, W (Associate).
Student:
Katneni, K.
Program of Study:
The impact of solubilising agents on the in vitro assessment of intestinal drug permeability and transporter function. (PHD) 2006.
Supervisors:
Charman, S (Joint-Co), Porter, C (Joint).
Student:
Kota, J.
Program of Study:
The impact of injection site and animal model on the lymphatic absorption of subcutaneously administered proteins. (PHD) 2007.
Supervisors:
Charman, S (Joint-Co), Porter, C (Joint).
Student:
Mcintosh, K.
Program of Study:
INTESTINAL ABSORPTION OF HUMAN GROWTH HORMONE IN THE PRESENCE OF A NOVEL CARRIER COMPOUND. (PHD) 2002.
Supervisors:
Charman, S (Main), Charman, W (Associate).
Student:
Mclennan ((Double Id)), D.
Program of Study:
THE CONTRIBUTION OF THE LYMPHATICS TO THE SYSTEMIC AVAILABILITY OF SUBCUTANEOUSLY ADMINISTERED RECOMBINANT PROTEINS. (PHD) 2004.
Supervisors:
Charman, S (Main), Porter, C (Associate).
Student:
Mclennan, D.
Program of Study:
THE CONTRIBUTION OF THE LYMPHATICS TO THE SYSTEMATIC AVAILABILITY OF SUBCUTANEOUSLY ADMINISTERED RECOMBINANT PROTEINS. (PHD) 2004.
Supervisors:
Charman, S (Main), Porter, C (Associate).
Student:
Perry, C.
Program of Study:
Chemical stability and pharmacokinetic studies of a new class of synthetic ozonide antimalarials. (PHD) 2006.
Supervisors:
Charman, W (Joint-Co), Charman, S (Joint).
Student:
Segrave, A.
Program of Study:
AN INVESTIGATION OF THE PHARMACOKINETICS AND LYMPHATIC TRANSPORT OF RECOMBINANT HUMAN LEUKAEMIA INHIBITORY FACTOR. (PHD) 2004.
Supervisors:
Charman, S (Joint-Co), Porter, C (Joint).
Student:
Stingelin, L.
Program of Study:
Structural dependency of iron- and blood-mediated degradation and heme alkylation for a series of novel ozonides. (PHD) 2012.
Supervisors:
Charman, S (Main), Charman, W (Associate).