Drug intelligence / Profile preview

lumefantrine + artemether + rifampicin

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy involving the antimalarial fixed-dose combination of artemether and lumefantrine (commonly known as Coartem) administered together with rifampicin, an antibiotic primarily used to treat tuberculosis. Artemether and lumefantrine are both antimalarial agents; artemether acts rapidly against Plasmodium falciparum by generating cytotoxic radicals through interaction with heme in the parasite's food vacuole, while lumefantrine has a longer half-life and clears residual parasites. Rifampicin is a potent inducer of cytochrome P450 3A4 (CYP3A4), which significantly reduces plasma concentrations of both artemether and lumefantrine when co-administered. This drug-drug interaction leads to markedly lower exposure to both antimalarials, resulting in reduced efficacy for malaria treatment and increased risk of treatment failure or recrudescence. Therefore, this combination is not recommended due to significant pharmacokinetic interactions that compromise malaria therapy effectiveness[1][2][3].

Brand names
CoartemRifadin
Other names
lumefantrine-artemether + rifampicinartemether-lumefantrine + rifampicin
02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)CYP2B6 (Cytochrome P450 2B6)rpoB (DNA-directed RNA polymerase subunit beta)HemeCYP2C19 (Cytochrome P450 2C19)

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