Experiences with gossypol as a male pill

In 1981 to 1983 we performed a clinical study with gossypol involving 152 participants, and in 1983 to 1985 we conducted another study of 120 participants. The first study was aimed at confirming gossypol's antifertility efficacy and determining the existence of side effects. The objective of the latter study was to find out whether the addition of a potassium salt supplement or a potassium-sparing agent could alleviate the side effect of hypokalemia. In both studies, the participants took a gossypol pill, 20 mg/day for 60 to 75 days for loading, and 50 mg/wk for maintenance. All participants were followed up for a year. The antifertility efficacy was found to be more than 90%, and the chief side effect was lowered serum potassium. In our 1983 to 1985 study, we concluded that since neither potassium supplementation nor triamterene solved the problem, it is very likely that gossypol is a nephrotoxic agent. With 1 year of gossypol treatment, serum testosterone and serum luteinizing hormone showed no change, whereas serum follicle-stimulating hormone showed some elevation after 6 months. The Shanghai researchers found that in their gossypol users, plasma and urinary beta 2-microglobulin levels were elevated to a certain extent. However, 25 subjects in our 1983 to 1985 study showed no appreciable change. Our volunteers had stopped taking gossypol for more than 1 year. In 1986 we started a third study, which was aimed at finding the lowest antifertility dose to minimize possible renal toxicity.