Drug intelligence / Profile preview

Arterolane

Development stage
Phase 3
Lead developer
Sun Pharma
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Arterolane (RBx11160, OZ277) is a fully synthetic peroxidic antimalarial drug developed for the treatment of malaria. It features an ozonide (trioxolane) group and an adamantane substituent in its structure. The drug was discovered through a collaboration coordinated by the Medicines for Malaria Venture (MMV), with development led by Ranbaxy Laboratories. Arterolane acts as a prodrug that is activated by heme released from hemoglobin digestion within the malarial parasite; this activation generates free radicals that alkylate heme and parasite proteins, disrupting critical biological processes necessary for parasite survival[1][7][8]. Its mechanism of action shares similarities with artemisinin derivatives but also exhibits distinct properties—arterolane inhibits the *Plasmodium falciparum* sarco/endoplasmic reticulum calcium ATPase (PfATP6), though less potently than artemisinin[3][5][6]. Arterolane has been approved in India since 2012 and subsequently received marketing authorization in several African countries as part of a fixed-dose combination with piperaquine under the brand name Synriam[1][7].

Brand names
Synriam
Other names
arterolaneRBx11160RBx-11160RBx 11160OZ277OZ-277OZ 277
02

Targets

PfHRP2 (Plasmodium falciparum histidine-rich protein II)

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