Drug intelligence / Profile preview

amodiaquine

Development stage
Phase 4
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Amodiaquine is a 4-aminoquinoline antimalarial drug structurally related to chloroquine. It is primarily used for the treatment of uncomplicated malaria caused by *Plasmodium falciparum* and is often administered as part of artemisinin-based combination therapies (ACTs), such as with artesunate. Amodiaquine remains effective against some chloroquine-resistant strains of *P. falciparum*, though resistance to amodiaquine has also been reported and varies geographically[2][4][5]. The drug acts mainly by interfering with the detoxification process of heme in the parasite's food vacuole; it inhibits heme polymerase activity, leading to accumulation of toxic free heme that disrupts parasite membrane function and results in death[2][6]. After oral administration, amodiaquine is rapidly absorbed and extensively metabolized in the liver by CYP2C8 into its active metabolite N-desethylamodiaquine[5]. Both parent drug and metabolite possess antimalarial activity. Due to risks such as hepatotoxicity and agranulocytosis, its use for malaria prophylaxis has been discontinued in many regions but it remains important for therapy in endemic areas outside the United States[1][3]. Developed by Rhône-Poulenc, and now manufactured by Sanofi.

Brand names
CamoquinFlavoquineAmobinAmodiaquin
Other names
amodiaquine4-amino-2-[(diethylamino)methyl]phenol hydrochloride
02

Targets

Fe2+-heme in digestive vacuoleHNMT (Histamine N-methyltransferase)

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