Drug intelligence / Profile preview

artemisone + mefloquine

Development stage
Discontinued
Lead developer
University of Oxford
Modality
Small Molecules
Administration
Oral
01

Overview

**AmiM3** is an investigational oral co-administration regimen of the semisynthetic artemisinin derivative **artemisone** and the quinoline antimalarial **mefloquine** for uncomplicated *Plasmodium falciparum* malaria. In the University of Oxford-sponsored AMOS study, patients were assigned artemisone 4 mg/kg/day for 3 days plus mefloquine 15 mg/kg on day 3 and 10 mg/kg on day 4. Artemisone is a 10-amino-artemisinin derivative whose endoperoxide pharmacophore is activated in the parasite’s heme-rich environment, producing reactive intermediates that cause broad parasite macromolecular damage and disrupt redox homeostasis; mefloquine provides a mechanistically complementary blood-stage antimalarial effect associated with disruption of heme detoxification. The registered Western Cambodia study was withdrawn before approval was obtained. ([clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00936767))

Other names
AmiM3AmiM-3AmiM 3Artemisone/Mefloquine
02

Targets

KATP channel (ATP-sensitive potassium channel)ATP2A (Sarcoplasmic reticulum Ca2+-ATPase)

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