Drug intelligence / Profile preview

GSK369796

Development stage
Phase 1
Lead developer
GSK
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral (preclinical/early Clinical Studies)
01

Overview

GSK369796 (N-tert-butyl isoquine) is a synthetic 4-aminoquinoline antimalarial drug candidate developed as part of a public-private partnership involving academic institutions and pharmaceutical companies. It was rationally designed to improve upon existing 4-aminoquinoline antimalarials such as chloroquine and amodiaquine. The compound demonstrates potent activity against Plasmodium falciparum in vitro and rodent malaria parasites in vivo. Mechanistically, it acts as an inhibitor of the hERG potassium ion channel with an IC50 of 7.5 μM and is considered both affordable and effective for potential use in malaria treatment[1][2][9]. Preclinical studies have established its pharmacokinetic, toxicity, and safety profiles[2].

Other names
N-tert-butyl isoquineGSK-369796GSK369796GSK 369796DE-0055DE0055DE 0055
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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