Drug intelligence / Profile preview

[14C]artefenomel

Development stage
Unknown
Lead developer
Medicines for Malaria Venture
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

Artefenomel (OZ439) is an investigational synthetic trioxolane (ozonide) antimalarial compound developed by Medicines for Malaria Venture (MMV). It features a peroxide pharmacophore similar to artemisinin derivatives but is designed with improved pharmacokinetic properties, including high oral bioavailability and a long elimination half-life of 46-62 hours, making it a candidate for single-dose combination therapy. The drug acts as a fast-acting inhibitor of all asexual erythrocytic stages of *Plasmodium falciparum* and *Plasmodium vivax*. The [14C]-OZ439 variant is a carbon-14 radiolabeled version of the compound used specifically in Phase 1 clinical trials to determine absolute bioavailability and metabolic pathways through simultaneous intravenous microdosing and oral administration.

Other names
[14C]-artefenomelcarbon-14 labeled OZ439carbon14 labeled OZ439carbon 14 labeled OZ439
02

Targets

PfATP6 (Plasmodium falciparum ATP6)Heme

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