Ganaplacide
Ganaplacide is a drug in development by Novartis for the purpose of treating malaria. It is a imidazolopiperazine derivative. It has shown activity against the Plasmodium falciparum and Plasmodium vivax forms of the malaria parasite.
Clinical development
The antimalarial activity of the imidazolopiperazine compound class was initially discovered through a series of sensitive phenotypic antimalarial screens that were developed and run in 2007 and 2008 by a group of biologists working at the Genomics Institute of the Novartis Research Foundation and the Scripps Research Institute. The lead product was published in 2012 as a leader of the imidazolopiperazine class. This was followed by studies in animal models published in 2014. Preclinical studies found no significant in vitro safety liabilities. A Phase 1 study found some gastrointestinal and neurological effects but these were self-limited in 70 healthy males and established dosing for a future Phase 2 Trial.The just completed Phase 2 Trial was completed with 4 study locations in Thailand and one study location in Vietnam. This study looked at the effect of 400 mg given daily for 3 days as well as a single 800 mg dose. In the 21 Patients who received a single 800 mg dose 67% of patients cleared the infection which is comparable to other antimalarial medications. More than half of the patients had some reported adverse event and the rate was higher in patients who received a single 800 mg dose over patients who received 3 400 mg doses. The most common effect was asymptomatic bradycardia where patients heart rates fell below 60 Beats Per Minute. Other reported events include hypokalemia, elevated liver enzymes as well as anemia.