Drug intelligence / Profile preview

MMV390048

Development stage
Phase 2
Lead developer
Medicines for Malaria Venture
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

MMV390048 is a novel, orally administered small-molecule antimalarial compound from the aminopyridine class. It acts as a selective inhibitor of Plasmodium phosphatidylinositol 4‑kinase (PI4K), binding to the ATP-binding site of the enzyme and showing minimal off-target activity against other kinases, including human kinases except for PIP4K2C[1][5]. Preclinical studies demonstrated that it is highly potent against blood-stage malaria and can cure animal models with a single dose[2]. It also shows activity against other stages of the parasite lifecycle and all known resistant strains, suggesting potential for malaria control, transmission blocking, and eradication[2]. Clinical trials have shown that single oral doses are well tolerated in healthy volunteers and patients with malaria, with rapid absorption and long elimination half-life supporting its use as part of a single-dose cure regimen[4][7].

Other names
MMV390048MMV-390048MMV 390048MMV 048MMV048MMV-048
02

Targets

KCNE1 (Misshapen-like kinase 1)PfPI4KIIIβ (Plasmodium falciparum phosphatidylinositol 4-kinase type III beta)PI4KB (Phosphatidylinositol 4-kinase beta)PIP4K2C (Phosphatidylinositol-5-phosphate 4-kinase type-2 gamma)PI4KA (PI4Kα)MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4)

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