Phase I Clinical Testing of Antimalarial Drugs

The Phase I clinical testing of antimalarial drugs in 1977 involved a 52-week safety and tolerance study of 500 mg mefloquine weekly, with 4 out of 5 groups (10 participants each) completing the drug administration. The only potential drug-related adverse reaction was telogen effluvium, observed in 2 subjects. Additional studies on oral mefloquine revealed gastrointestinal intolerance at higher doses, with transient nausea and diarrhea occurring at 1000 mg and 1500 mg doses. Pharmacokinetic studies of WR 184,806.H3PO4 were conducted with single oral doses of 250, 500, and 1000 mg. Initial clinical testing of a new agent, WR 180,409.H3PO4, was also performed using single rising dose levels.