arterolane maleate + piperaquine phosphate

The drug arterolane maleate + piperaquine phosphate is a fixed-dose combination antimalarial medication that combines a synthetic trioxolane (arterolane maleate) with a long-acting antimalarial (piperaquine phosphate). This combination was developed as an alternative to artemisinin-based combination therapies for treating malaria. ## Composition and Formulation The medication is available as a fixed-dose combination containing 150 mg of arterolane maleate and 750 mg of piperaquine phosphate for adults[1][3]. A pediatric formulation is also available as dispersible tablets containing 37.5 mg of arterolane maleate and 187.5 mg of piperaquine phosphate[3][5]. ## Mechanism of Action Arterolane maleate is a synthetic trioxolane that acts as an adenosine triphosphatase inhibitor[4][5]. It works by increasing the levels of heme in the blood, which is toxic to the malarial parasite[6]. This mechanism is similar to artemisinin but with a different chemical structure. Piperaquine phosphate is a bisquinoline compound with a long half-life (approximately 15 days)[7]. It provides extended protection against recrudescence of the parasite. Its activity against chloroquine-resistant strains may be attributed to its bulky bisquinoline structure, which possibly inhibits chloroquine efflux transporters from the parasite food vacuole[7]. ## Clinical Efficacy Clinical trials have demonstrated that the combination effectively treats uncomplicated Plasmodium falciparum malaria with a cure rate of over 95%[5]. The median parasite clearance time and fever clearance time are comparable to other artemisinin-based combinations (approximately 30 hours and 24 hours, respectively)[1]. ## Dosing and Administration The medication is administered as a once-daily dose for three consecutive days[1][3]. This simplified dosing regimen may improve patient compliance compared to other antimalarial treatments that require multiple daily doses[7]. ## Development and Approval The drug was originally developed through a collaboration between Ranbaxy Laboratories (now acquired by Sun Pharmaceutical Industries) and the Medicines for Malaria Venture (MMV)[4][5]. It received approval in India in 2012 under the brand name Synriam, making it India's first new drug for treating Plasmodium falciparum malaria in adults[5]. It has since been approved in several African countries including Nigeria, Uganda, Senegal, Cameroon, Guinea, Kenya, and Ivory Coast[5]. ## Advantages The combination offers several advantages: - Once-daily dosing for three days (compared to twice-daily dosing with other antimalarials) - No dietary restrictions for fatty foods or milk - Rapid relief from malaria-related symptoms - High cure rate (>95%) - Alternative to artemisinin-based therapies, potentially addressing artemisinin resistance concerns[5][7] This fixed-dose combination represents an important addition to the antimalarial armamentarium, particularly in regions where resistance to existing therapies is a growing concern.

Brand names

Synriam

Other names

Arterolane maleate/piperaquine phosphate