Prof William Charman - Researcher Profile

Biography

Position

Dean
Faculty of Pharmacy and Pharmaceutical Sciences

Director
Monash Institute of Pharmaceutical Sciences


Shared vision inspires pharmacological breakthroughs

A single-dose oral drug that has the potential to cure malaria is one of the latest collaborative advances in medicine design from the Monash Institute of Pharmaceutical Sciences (MIPS). The development could save millions of lives, particularly in sub-Saharan Africa where 85 per cent of malaria’s victims are children aged under five. MIPS Director Professor Bill Charman is confident there will be many further life-saving and life-enhancing advances emerging from the research being conducted at MIPS.  

 

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Qualifications

DOCTOR OF SCIENCE HONORIS CAUSA

Institution: University of London

Year awarded: 2011

DOCTOR OF PHILOSOPHY

Institution: University of Kansas

Year awarded: 1985

BACHELOR OF PHARMACY

Institution: Monash University

Year awarded: 1981

Publications

Journal Articles

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, American Chemical Society, Washington DC USA, pp. 5851-5858.

Caliph, S.M., Trevaskis, N., Charman, W.N., Porter, C.J., 2012, Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies, Journal of Pharmaceutical Sciences [P], vol 101, issue 9, Wiley-Blackwell, Malden, Massachusetts USA, pp. 3540-3546.

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 Academy of Sciences, Washington DC USA, pp. 16823-16828.

Oliyai, R., Brewster, M.E., Ozeki, T., Rajewski, R.A., Charman, W.N., 2012, Professor Valentino J. Stella: Scientist, mentor, entrepreneur, family man, and giant in pharmaceutical chemistry, Journal of Pharmaceutical Sciences [P], vol 101, issue 9, Wiley-Blackwell, Malden Massachusetts USA, pp. 2989-2995.

Trevaskis, N., Charman, W., Porter, C., 2011, Acute hypertriglyceridemia promotes intestinal lymphatic lipid and drug transport: a positive feedback mechanism in lipid and drug absorption, Molecular Pharmaceutics [P], vol 8, American Chemical Society, USA, pp. 1132-1139.

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, American Chemical Society, USA, pp. 3935-3949.

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, American Chemical Society, 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 Academy of Sciences, Washington D.C., USA, pp. 4400-4405.

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, American Chemical Society, USA, pp. 1686-1699.

Trevaskis, N., Charman, W., Porter, C., 2010, Targeted drug delivery to lymphocytes: a route to site-specific immunomodulation?, Molecular Pharmaceutics [P], vol 7, issue 6, American Chemical Society, United States, pp. 2297-2309.

Tang, Y., wittlin, s., Charman, S.A., Chollet, J., Chiu, F.C.K., Morizzi, J., Johnson, L., Santo Tomas, J., Scheurer, C., Christopher Snyder, 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.

Trevaskis, N., Shanker, R., Charman, W.N., Porter, C.J., 2010, The mechanism of lymphatic access of two cholesteryl ester transfer protein inhibitors (CP524,515 and CP532,623) and evaluation of their impact on lymph lipoprotein profiles, Pharmaceutical Research [P], vol 27, issue 9, Springer, USA, pp. 1949-1964.

Trevaskis, N., McEvoy, C.L., McIntosh, M.P., Edwards, G.A., Shanker, R., Charman, W.N., Porter, C.J., 2010, The role of the intestinal lymphatics in the absorption of two highly lipophilic cholesterol ester transfer protein inhibitors (CP524,515 and CP532,623), Pharmaceutical Research [E], vol 27, Springer Science, USA, pp. 878-893.

Dong, Y., Wittlin, S., Sriraghavan, K., Chollet, J., Charman, S.A., Charman, W.N., Scheurer, C., Urwyler, H., Santo Tomas, J., Christopher Snyder, 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, American Chemical Society, USA, pp. 481-491.

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, American Chemical Society, USA, pp. 1864-1872.

Trevaskis, N., Shackleford, D., Charman, W.N., Edwards, G.A., Gardin, A., Appel-Dingemanse, S., Kretz, O., Galli, B., Porter, C.J., 2009, Intestinal lymphatic transport enhances the post-prandial oral bioavailability of a novel cannabinoid receptor agonist via avoidance of first-pass metabolism, Pharmaceutical Research [P], vol 26, issue 6, Springer New York LLC, USA, pp. 1486-1495.

White, K.L., Nguyen, G., Charman, W.N., Edwards, G.A., Faassen, W.A.(., Porter, C.J., 2009, Lymphatic transport of methylnortestosterone undecanoate (MU) and the bioavailability of methylnortestosterone are highly sensitive to the mass of coadministered lipid after oral administration of MU, Journal Of Pharmacology And Experimental Therapeu..., vol 331, issue 2, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 700-709.

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.

Holloway, G.A., Charman, W.N., Fairlamb, A.H., Brun, R., Kaiser, M., Kostewicz, E.S., Novello, P.M., Parisot, J.P., Richardson, J., Street, I.P., Watson, K.G., Baell, J.B., 2009, Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity, Antimicrobial Agents And Chemotherapy [P], vol 53, issue 7, American Society for Microbiology, USA, pp. 2824-2833.

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.

Porter, C.J., Pouton, C.W., Cuine, J., Charman, W.N., 2008, Enhancing intestinal drug solubilisation using lipid-based delivery systems, Advanced Drug Delivery Reviews, vol 60, issue 6, Elsevier BV, Netherlands, pp. 673-691.

Cuine, J., mcevoy, c., Charman, W.N., Pouton, C.W., Edwards, G.A., Benameur, H., Porter, C.J., 2008, Evaluation of the impact of surfactant digestion on the bioavailability of Danazol after oral administration of lipidic self-emulsifying formulations to dogs, Journal of Pharmaceutical Sciences, vol 97, issue 2, John-Wiley & Sons, USA, pp. 995-1012.

Trevaskis, N., Charman, W.N., Porter, C.J., 2008, Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update, Advanced Drug Delivery Reviews, vol 60, issue 6, Elsevier BV, Netherlands, pp. 702-716.

Marriott, J.L., Nation, R.L., Roller, L., Costelloe, M.T., Galbraith, K.J., Stewart, P.J., Charman, W.N., 2008, Pharmacy Education in the Context of Australian Practice, American Journal of Pharmaceutical Education, vol 72, issue 6, American Association of Colleges of Pharmacy, United States, pp. 1-12.

Creek, D.J., Chalmers, D.K., Charman, W.N., Duke, B.J., 2008, Quantum chemical study of the intermediate complex required for iron-mediated reactivity and antimalarial activity of dispiro-1,2,4-trioxolanes, Journal of Molecular Modelling and Design, vol 27, issue 3, Elsevier Inc., USA, pp. 394-400.

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, The American Society for Microbiology, USA, pp. 1291-1296.

Cuine, J., Charman, W.N., Pouton, C.W., Edwards, G.A., Porter, C.J., 2007, Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs, Pharmaceutical Research, vol 24, issue 4, Springer Science & Business Media, New York, pp. 748-757.

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.

Porter, C.J., Trevaskis, N., Charman, W.N., 2007, Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs, Nature Reviews - Drug Discovery, vol 6, issue 14, Nature Publishing Group, UK, pp. 231-248.

Kossena, G.A., Charman, W.N., Wilson, C., O'Mahony, B., Lindsay, B., Hempenstall, J., Davidson, C., Crowley, P., Porter, C.J., 2007, Low dose lipid formulations: effects on gastric emptying and biliary secretion, Pharmaceutical Research, vol 24, issue 11, Springer New York LLC, US, pp. 2084-2096.

Horne, H.J., d'Auvergne, E.J., Coles, M., Velkov, T., Chin, Y., Charman, W.N., Prankerd, R.J., Gooley, P., Scanlon, M., 2007, Probing the Flexibility of the DsbA Oxidoreductase from Vibrio cholerae-a 15N - 1H Heteronuclear NMR Relaxation Analysis of Oxidized and Reduced Forms of DsbA, Journal of Molecular Biology, vol 371, issue 3, Academic Press, England, pp. 703-716.

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.

Trevaskis, N.L., Lo, C., Ma, L., Tso, P., Irving, H.R., Porter, C.J.H., Charman, W.N., 2006, An acute and coincident increase in FABP expression and lymphatic lipid and drug transport occurs during intestinal infusion of lipid-based drug formulations to rats, Pharmaceutical Research, vol 23, issue 8, Springer New York LLC, USA, pp. 1786-1796.

Trevaskis, N., Porter, C.J.H., Charman, W.N., 2006, An examination of the interplay between enterocyte-based metabolism and lymphatic drug transport in the rat, Drug Metabolism and Disposition, vol 34, issue 5, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 729-733.

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., Christopher Snyder, 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.

Sek, L., Boyd, B.J., Charman, W.N., Porter, C.J.H., 2006, Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone, Journal of Pharmacy and Pharmacology, vol 58, issue 6, Pharmaceutical Press, UK, pp. 809-820.

Holm, R., Porsgaard, T., Porter, C.J.H., Hoy, C., Edwards, G.A., Mullertz, A., Kristensen, H.G., Charman, W.N., 2006, Lymphatic fatty acids in canines dosed with pharmaceutical formulations containing structured triacylglycerols, European Journal of Lipid Science and Technology, vol 108, issue 9, Wiley - V C H Verlag GmbH & Co. KGaA, Germany, pp. 714-722.

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.

Leveque, N.L., Charman, W.N., Chiu, F.C.K., 2006, Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography-mass spectrometry, Journal of Chromatography B, vol 830, issue 2, Elsevier, The Netherlands, pp. 314-321.

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.

Trevaskis, N., Porter, C.J.H., Charman, W.N., 2006, The lymph lipid precursor pool is a key determinant of intestinal lymphatic drug transport, The Journal of Pharmacology and Experimental Therapeutics, vol 316, issue 2, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 881-891.

Trevaskis, N.L., Tso, P., Rider, T., Charman, W.N., Porter, C.J.H., Jandacek, R., 2006, Tissue uptake of DDT is independent of chylomicron metabolism, Archives of Toxicology, vol 80, issue 4, Springer, Germany, pp. 196-200.

Trevaskis, N., Porter, C.J.H., Charman, W.N., 2005, Bile increases intestinal lymphatic drug transport in the fasted rat, Pharmaceutical Research, vol 22, issue 11, Springer, USA, pp. 1863-1870.

Kossena, G.A., Charman, W.N., Boyd, B.J., Porter, C.J.H., 2005, Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water-soluble drug, Journal of Pharmaceutical Sciences, vol 94, issue 3, John Wiley & Sons, Inc., USA, pp. 481-492.

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.

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.

Velkov, T., Chuang, S., Wielens, J., Sakellaris, H.H., Charman, W.N., Porter, C.J., Scanlon, M., 2005, The interaction of lipophilic drugs with intestinal fatty acid-binding protein, The Journal of Biological Chemistry, vol 280, issue 18, The American Society for Biochemistry and Molecular Biology, Inc., USA, pp. 17769-17776.

Kossena, G.A., Charman, W.N., Boyd, B.J., Porter, C.J.H., 2004, A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs, Journal of Controlled Release, vol 99, issue 2, Elsevier, The Netherlands, pp. 217-229.

Campbell, M., Prankerd, R.J., Davie, A.S., Charman, W.N., 2004, Degradation of berenil (diminazene aceturate) in acidic aqueous solution, Journal of Pharmacy and Pharmacology, vol 56, issue 10, Pharmaceutical Press, London UK, pp. 1327-1332.

Kaukonen, A., Boyd, B.J., Porter, C.J.H., Charman, W.N., 2004, Drug solubilization behavior during in vitro digestion of simple triglyceride lipid solution formulations, Pharmaceutical Research, vol 21, issue 2, Kluwer Academic/Plenum Publishers, Dordrecht The Netherlands, pp. 245-253.

Kaukonen, A., Boyd, B.J., Charman, W.N., Porter, C.J.H., 2004, Drug solubilization behaviour during in vitro digestion of suspension formulations of poorly water-soluble drugs in triglyceride lipids, Pharmaceutical Research, vol 21, issue 2, Kluwer Academic/Plenum Publishers, Dordrecht The Netherlands, pp. 254-260.

McIntosh, M.P., Batey, A.J., Coker, S.J., Porter, C.J.H., Charman, W.N., 2004, Evaluation of the impact of altered lipoprotein binding conditions on halofantrine induced QTc interval prolongation in an anaesthetised rabbit model, Journal of Pharmacy and Pharmacology, vol 56, issue 11, Pharmaceutical Press, Wallingford UK, pp. 69-77.

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.

McIntosh, M.P., Charman, W.N., Campbell, M., Porter, C.J.H., 2004, Influence of physicochemical properties on the patterns of association of a series of aliphatic esters of halofantrine with plasma lipoproteins, Journal of Controlled Release, vol 95, issue 2, Elsevier, The Netherlands, pp. 275-289.

Yousaf, M., Hammond, N.L., Peng, J., Wahyuono, S., McIntosh, K.A., Charman, W.N., Mayer, A.M.S., Hamann, M.T., 2004, New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases, Journal of Medicinal Chemistry, vol 47, issue 14, American Chemical Society, Washington USA, pp. 3512-3517.

Grellepois, F., Chorki, F., Ourevitch, M., Charneau, S., Grellier, P., McIntosh, K.A., Charman, W.N., Pradines, B., Crousse, B., Bonnet-Delpon, D., Begue, J., 2004, Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin, Journal of Medicinal Chemistry, vol 47, issue 6, American Chemical Society, Washington USA, pp. 1423-1433.

Kossena, G.A., Charman, W.N., Boyd, B.J., Dunstan, D.E., Porter, C.J.H., 2004, Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach, Journal of Pharmaceutical Sciences, vol 93, issue 2, Wiley-Liss, Inc., Hoboken USA, pp. 332-348.

Porter, C.J.H., Kaukonen, A., Boyd, B.J., Edwards, G.A., Charman, W.N., 2004, Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation, Pharmaceutical Research, vol 21, issue 8, Kluwer Academic/Plenum Publishers, Dordrecht The Netherlands, pp. 1405-1412.

Porter, C.J.H., Kaukonen, A., Taillardat-Bertschinger, A., Boyd, B.J., O'Connor, J.M., Edwards, G.A., Charman, W.N., 2004, Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine, Journal of Pharmaceutical Sciences, vol 93, issue 5, John-Liss, Inc., Hoboken USA, pp. 1110-1121.

Johnson, B.M., Chen, W., Borchardt, R.T., Charman, W.N., Porter, C.J.H., 2003, A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum, The Journal of Pharmacology and Experimental Therapeutics, vol 305, issue 1, American Society for Pharmacology and Experimental Therapeutics (ASPET), USA, pp. 151-158.

Johnson, B.M., Charman, W.N., Porter, C.J.H., 2003, Application of compartmental modeling to an examination of in vitro intestinal permeability data: assessing the impact of tissue uptake, P-glycoprotein, and CYP3A, Drug metabolism and Disposition, vol 31, issue 9, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 1151-1160.

Shackleford, D.M., Faassen, W.A.(., Houwing, N., Lass, H., Edwards, G.A., Porter, C.J.H., Charman, W.N., 2003, Contribution of lymphatically transported testosterone undecanoate to the systemic exposure of testosterone after oral administration of two andriol formulations in conscious lymph duct-cannulated dogs, The Journal of Pharmacolgy and Experimental Therapeutics, vol 306, issue 3, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 925-933.

McIntosh, M.P., Batey, A.J., Porter, C.J.H., Charman, W.N., Coker, S.J., 2003, Desbutylhalofantrine: evaluation of QT prolongation and other cardiovascular effects after intravenous administration in vivo, Journal of Cardiovascular Pharmacology, vol 41, issue 3, Lippincott Williams & Wilkins, USA, pp. 406-413.

Shackleford, D.M., Porter, C.J.H., Charman, W.N., 2003, Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine in vivo?, Biopharmaceutics & Drug Disposition, vol 24, issue 4, John Wiley & Sons Ltd., UK, pp. 153-157.

Holm, R., Porter, C.J.H., Edwards, G.A., Mullertz, A., Kristensen, H.G., Charman, W.N., 2003, Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides, European Journal of Pharmaceutical Sciences, vol 20, issue 1, Elsevier, The Netherlands, pp. 91-97.

Khoo, S., Shackleford, D.M., Porter, C.J.H., Edwards, G.A., Charman, W.N., 2003, Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs, Pharmaceutical Research, vol 20, issue 9, Kluwer Academic/Plenum Publishers, USA, pp. 1460-1465.

Taillardat-Bertschinger, A., Perry, C.S., Galland, A., Prankerd, R.J., Charman, W.N., 2003, Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil: effects on its apparent ionization constant, Journal of Pharmaceutical Sciences, vol 92, issue 11, John Wiley & Sons, Inc., USA, pp. 2217-2228.

Shackleford, D.M., Prankerd, R.J., Scanlon, M.J., Charman, W.N., 2003, Self-micellization of gemfibrozil 1-0- acyl glucuronide in aqueous solution, Pharmaceutical Research, vol 20, issue 3, Kluwer Academic/Plenum Publishers, USA, pp. 465-470.

Kossena, G.A., Boyd, B.J., Porter, C.J.H., Charman, W.N., 2003, Separation and characterization of the colloidal phases produced on digestion of common formulation lipids and assessment of their impact on the apparent solubility of selected poorly water-soluble drugs, Journal of Pharmaceutical Sciences, vol 92, issue 3, John Wiley & Sons, Inc., USA, pp. 634-648.

Boyd, B.J., Porter, C.J.H., Charman, W.N., 2003, Using the polymer partitioning method to probe the thermodynamic activity of poorly water-soluble drugs solubilized in model lipid digestion products, Journal of Pharmaceutical Sciences, vol 92, issue 6, John Wiley & Sons, Inc., USA, pp. 1262-1271.

Khoo, S.M., Prankerd, R.J., Edwards, G.A., Porter, C., Charman, W.N., 2002, A physicochemical basis for the extensive intestinal lymphatic transport of a poorly lipid soluble antimalarial, halofantrine hydrochloride, after postprandial administration to dogs, Journal of Pharmaceutical Sciences, vol 91, issue 3, John Wiley and Sons Inc., USA, pp. 647-659.

Johnson, B.M., Charman, W.N., Porter, C., 2002, An in vitro examination of the impact of polyethylene glycol 400, pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised Rat intestine, American Association of Pharmaceutical Scientists Pharmacy Science, vol 4, issue 4, American Association of Pharmaceutical Scientists, USA, pp. 1-13.

Sek, L., Porter, C., Kaukonen, A., Charman, W.N., 2002, Evaluation of the in-vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products, Journal of Pharmacy and Pharmacology, vol 54, issue 1, Pharmaceutical Press, UK, pp. 29-41.

Avery, M.A., Alvim-Gaston, M., Vroman, J.A., Wu, B., Ager, A., Peters, W., Robinson, B.L., Charman, W.N., 2002, Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates, Journal of Medicinal Chemistry, vol 45, issue 19, American Chemical Society, USA, pp. 4321-4335.

Holm, R., Porter, C., Mullertz, A., Kristensen, H.G., Charman, W.N., 2002, Structured triglyceride vehicles for oral delivery of halofantrine: examination of intestinal lymphatic transport and bioavailability in conscious rats, Pharmaceutical Research, vol 19, issue 9, Kluwer Academic/Plenum Publishers, USA, pp. 1354-1361.

Khoo, S., Edwards, G.A., Porter, C.J.H., Charman, W.N., 2001, A conscious dog model for assessing the absorption, enterocyte-based metabolism, and intestinal lymphatic transport of halofantrine, Journal of Pharmaceutical Sciences, vol 90, issue 10, John Wiley & Sons, Inc., USA, pp. 1599-1607.

Edwards, G.A., Porter, C.J.H., Caliph, S.M., Khoo, S., Charman, W.N., 2001, Animal models for the study of intestinal lymphatic drug transport, Advanced Drug Delivery Reviews, vol 50, Elsevier Science BV, The Netherlands, pp. 45-60.

Sek, L., Porter, C.J.H., Charman, W.N., 2001, Characterisation and quantification of medium chain and long chain triglycerides and their In vitro digestion products, by HPTLC coupled with In situ densitometric analysis, Journal of Pharmaceutical and Biomedical Analysis, vol 25, Elsevier Science BV, The Netherlands, pp. 651-661.

Porter, C.J.H., Charman, W.N., 2001, In vitro assessment of oral lipid based formulations, Advanced Drug Delivery Reviews, vol 50, Elsevier Science BV, The Netherlands, pp. 127-147.

Porter, C.J.H., Charman, W.N., 2001, Intestinal lymphatic drug transport: an update, Advanced Drug Delivery Reviews, vol 50, Elsevier Science BV, Netherlands, pp. 61-80.

Porter, C.J.H., Charman, W.N., 2001, Lipid-based formulations for oral administration: opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs, Journal of Receptor and Signal Transduction Research, vol 21, issue 2&3, Marcel Dekker Inc., USA, pp. 215-257.

Johnson, B.M., Charman, W.N., Porter, C.J.H., 2001, The impact of P-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil, Journal of Pharmacy and Pharmacology, vol 53, issue 12, Pharmaceutical Press, UK, pp. 1611-1619.

Caliph, S.M., Charman, W.N., Porter, C.J.H., 2000, Effect of short-, medium-, and long-chain fatty acid based vehicles on the absolute oral bioavailability and intestinal lymphatic transport of halofantrine and assessment of mass balance in lymph-cannulated and non-cannulated rats, Journal of Pharmaceutical Sciences, vol 89 issue 8, John Wiley & Sons Inc., New York NY USA, pp. 1073-1084.

Lyons, K.C., Charman, W.N., Miller, R., Porter, C.J.H., 2000, Factors limiting the oral bioavailability of N- acetylglucosaminyl-N-acetylmuramyl dipeptide (GMDP) and enhancement of absorption in rats by delivery in a water-in-oil microemulsion, International Journal of Pharmaceutics, vol 199 issue 1, Elsevier Science B.V., Amsterdam Netherlands, pp. 17-28.

Charman, W.N., 2000, Lipids, lipophilic drugs,and oral drug delivery-Some emerging concepts, Journal of Pharmaceutical Sciences, vol 89 issue 8, John Wiley & Sons Inc., New York NY USA, pp. 967-978.

Khoo, S., Porter, C.J.H., Charman, W.N., 2000, The formulation of halofantrine as either non-solubilising PEG 6000 or solubilising lipid based solid dispersions: Physical stability and absolute bioavailability assessment, International Journal of Pharmaceutics, vol 205 issues 1-2, Elsevier Science B.V., Netherlands, pp. 65-78.

Other

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

Grants

Title:

A Proof of Concept Pilot Study Aimed at Developing a Kinome-wide Screening Programme for Plasmodium falciparum.

Investigators:

Charman, W, Charman, S, Wilks, A

Funding:

(2009 - 2013). Medicines for Malaria Venture (MMV). $528,738.71

(2011 - 2015). Medicines for Malaria Venture (MMV). $248,036.89

Title:

An Australian Centre of Pharmaceutical Innovation to design and develop next generation formulation platforms and products.

Investigators:

Morton, D, Charman, W, Orlando, L

Funding:

(2009 - 2013). Victorian Department of Innovation, Industry & Regional Development (DIIRD). $1,500,000.00

(2010 - 2015). GlaxoSmithKline, Australia. $1,059,000.00

Title:

Assessment of the ADME and pharmacokinetic properties of P218 as a preclinical candidate in the field of Malaria (part of MMV Dihydrofolate Reductase (DHFR) project).

Investigators:

Charman, S, Charman, W

Funding:

(2003 - 2008). Medicines for Malaria Venture (MMV). $635,914.10

(2007 - 2011). Medicines for Malaria Venture (MMV). $777,060.00

Title:

Drug Absorption Research Facility.

Investigators:

Charman, W, Charman, S, Porter, C

Funding:

(1999 - 2017). Monash University. $240,000.00

Title:

DsbA: A target for the design of drug candidates as selective inhibitors of oxidative protein folding in Gram-negative bacteria.

Investigators:

Scanlon, M, Charman, W, Sakellaris, H, Farrell, L

Funding:

(2004 - 2008). Australian Research Council (ARC). $104,450.00

(2004 - 2008). GBS Ventures. $90,000.00

Title:

GSK Analytical-Prof B Charman.

Investigators:

Charman, W

Funding:

(2002 - ). GlaxoSmithKline Biologicals, Belgium. $0.00

Title:

Integrating drug delivery principles into drug design to transform the treatment of immune disease.

Investigators:

Porter, C, Charman, W, Alderuccio, F, Trevaskis, N

Funding:

(2011 - 2015). National Health & Medical Research Council (NHMRC). $533,390.00

(2011 - 2016). National Health & Medical Research Council (NHMRC). $0.00

Title:

Low cost, needle-free and non-refrigerated treatment for post-partum haemorrhage.

Investigators:

McIntosh, M, Prankerd, R, Morton, D, Charman, W, Bischof, R, Meeusen, E, Parkington, H

Funding:

(2011 - 2015). U.S. Agency for International Development (USAID, USA). $249,622.00

Title:

Lymphotropic Prodrugs: A Novel Mechanism for Targeted Drug Delivery.

Investigators:

Porter, C, Charman, W, Stella, V

Funding:

(2011 - 2015). Australian Research Council (ARC). $13,000.00

(2011 - 2015). Australian Research Council (ARC). $450,000.00

(2011 - 2015). Monash University. $8,000.00

Title:

Optimizing Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Malaria.

Investigators:

Charman, S, Charman, W

Funding:

(2007 - 2011). Medicines for Malaria Venture (MMV). $1,575,135.21

Title:

Recognition of macromolecular complexes by cell surface receptors: A novel mechanism of lipid and drug absorption.

Investigators:

Porter, C, Charman, W, Tso, P

Funding:

(2008 - 2011). National Health & Medical Research Council (NHMRC). $377,125.00

(2010 - 2014). National Health & Medical Research Council (NHMRC). $0.00

Title:

Structure-based design of inhibitors of oxidative protein folding in enterobacteriaceae.

Investigators:

Scanlon, M, Charman, W, Simpson, J, Heras, B

Funding:

(2011 - 2015). National Health & Medical Research Council (NHMRC). $505,470.00

Title:

Targeting virulence of Pseudomonas aeruginosa by inhibiting oxidative protein folding.

Investigators:

Scanlon, M, Martin, J, Charman, W, Simpson, J, Nation, R, Morton, C

Funding:

(2009 - 2013). Australian Research Council (ARC). $600,000.00

(2009 - 2013). Biota Holdings Ltd. $180,000.00

Title:

Translational Medicinal Chemistry Facility - Equipment.

Investigators:

Charman, W

Funding:

(2010 - 2014). Victorian Department of Innovation, Industry & Regional Development (DIIRD). $700,000.00

Title:

DsbA inhibitors as potential antimicrobials - shared grant administered by UQ.

Investigators:

Martin, J, Scanlon, M, Charman, W, Heras, B, Reid, R

Funding:

(2007 - 2011). National Health & Medical Research Council (NHMRC). $254,250.00