A Single-Blind, Placebo-Controlled, Randomized First Time in Human Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Repeat Dose Escalation of GSK932121 in Healthy Adult Subjects

The purpose of this study is to determine if the study drug (antimalarial medication) is safe when given to healthy subjects as a single dose or as repeated doses, to understand the effect of food on single doses of study drug and to determine if the study drug has an effect on other approved medications such as rosiglitazone and rosuvastatin.

开始日期2008-12-11

申办/合作机构

GSK Plc

100 项与 GSK-932121 相关的临床结果

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100 项与 GSK-932121 相关的转化医学

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100 项与 GSK-932121 相关的专利（医药）

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项与 GSK-932121 相关的文献（医药）

2012-12-01·Future Medicinal Chemistry4区 · 医学

Exploration Of 4( 1H )-Pyridones As A Novel Family Of Potent Antimalarial Inhibitors Of The Plasmodial Cytochrome bc1

4区 · 医学

Review

作者: Fiandor, José M ; Ferrer, Santiago ; Derimanov, Geo ; Angulo-Barturen, Iñigo ; Herreros, Esperanza ; Bueno, José M ; Gamo, Francisco J ; Gargallo-Viola, Domingo

A novel family of antimalarials based on the 4(1H)-pyridone scaffold is described. The compounds display potent antimalarial activity against Plasmodium falciparum in vitro and in vivo. Like atovaquone, 4(1H)-pyridones exert their antimalarial action by inhibiting selectively the electron-transport chain in P. falciparum at the cytochrome bc1 level (complex III). However, despite the similar mechanism of action, no cross-resistance with atovaquone has been found, suggesting that the binding mode of 4(1H)-pyridones might be different from that of atovaquone. The medicinal chemistry program, focused on improving potency and physicochemical properties, ultimately led to the discovery of GSK932121, which was progressed efficiently into first time in human studies. However, progression of GSK932121 was terminated when new toxicology results were obtained in the rat with a soluble phosphate prodrug of the candidate, indicating a potentially narrow therapeutic index.

Chemical Communications2区 · 化学

Isoxazole mediated synthesis of 4-(1H)pyridones: improved preparation of antimalarial candidate GSK932121

2区 · 化学

Article

作者: Bueno, José M. ; Fernández, Jorge ; Lorenzo, Milagros ; Chicharro, Jesús

A new synthesis of the antimalarial clinical candidate GSK932121 is described.

100 项与 GSK-932121 相关的药物交易

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