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.

Start Date11 Dec 2008

Sponsor / Collaborator

GSK Plc

100 Clinical Results associated with GSK-932121

100 Translational Medicine associated with GSK-932121

100 Patents (Medical) associated with GSK-932121

Literatures (Medical) associated with GSK-932121

01 Dec 2012·Future Medicinal ChemistryQ4 · MEDICINE

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

Q4 · MEDICINE

Review

Author: 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 CommunicationsQ2 · CHEMISTRY

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

Q2 · CHEMISTRY

Article

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

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

100 Deals associated with GSK-932121

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Indication	Highest Phase	Country/Location	Organization	Date
Malaria	Phase 2	-	MMV Medicines for Malaria Venture	-
Malaria	Phase 2	-	MMV Medicines for Malaria Venture	-

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