Drug intelligence / Profile preview

arterolane + piperaquine

Development stage
Unknown
Lead developer
Sun Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Synriam is a fixed-dose combination antimalarial medication composed of arterolane maleate (a synthetic trioxolane/ozonide) and piperaquine phosphate (a bisquinoline). Originally developed by Ranbaxy Laboratories (now Sun Pharmaceutical Industries) in collaboration with the Medicines for Malaria Venture (MMV), Synriam was approved in India in 2011 and subsequently in several African countries for the treatment of acute uncomplicated *Plasmodium falciparum* malaria. Arterolane acts rapidly to clear parasites by generating reactive free radicals upon activation by intraparasitic heme, which is believed to inhibit the sarcoplasmic/endoplasmic reticulum calcium ATPase (PfATP6). Piperaquine provides a longer-lasting schizontocidal effect by interfering with heme detoxification in the parasite's food vacuole, thereby preventing recrudescence. In addition to malaria, Synriam has been investigated for drug repurposing against schistosomiasis (caused by *Schistosoma mansoni* and *Schistosoma haematobium*), where it has been evaluated in Phase II clinical trials in Côte d'Ivoire.

Brand names
Synriam
Other names
arterolane maleate + piperaquine phosphatearterolane/piperaquinearterolane maleate/piperaquine phosphateOZ277 + piperaquine
02

Targets

Ferriprotoporphyrin IX/hemozoin formation pathway in Plasmodium food vacuolePfATP6 (Plasmodium falciparum ATP6)FPIX/HDP (Ferriprotoporphyrin IX/heme detoxification pathway in Plasmodium food vacuole)

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