Gossypol

Scientific Name(s): Gossypium spp.
Common Name(s): ApoG2, AT-101, Gossypol

Medically reviewed by Drugs.com. Last updated on Jan 24, 2022.

Clinical Overview

Use

According to Chinese studies, gossypol is effective as a nonhormonal male contraceptive; however, it has been documented to have irreversible effects on male fertility and is not recommended for this use. Gossypol is being studied for clinical applications in cancer therapy with equivocal results.

Dosing

Antifertility: There are no dosing recommendations for gossypol due to its potential irreversible effects on male fertility. Cancer: Maximum tolerated dosage appears to be 40 mg/day of gossypol (as AT-101).

Contraindications

None well documented.

Pregnancy/Lactation

Avoid use. Documented abortifacient effects.

Interactions

None well documented.

Adverse Reactions

Nausea, emesis, anorexia, diarrhea, altered taste sensation, small intestine obstruction, and fatigue have been reported in clinical trials. The irreversible effects of gossypol on male fertility have been well documented, as has the incidence of hypokalemia. Dose-limiting elevations in liver enzymes have been noted at total doses of 60 mg/day for AT-101, and an increased incidence of hematological toxicities has been observed when AT-101 is combined with cancer chemotherapy, depending on the regimen.

Toxicology

No data.

Scientific Family

• Malvaceae (mallow)

Botany

Gossypol is derived from members of the family Malvaceae. The stem, seed, and root of the cotton plant Gossypium hirsutum represent the most common sources of gossypol. Gossypium species are shrubs that grow to a height of 3 m, have broad lobed leaves, and contain seeds in a capsule or "boll" of fibers. These fibers are harvested and woven in the textile industry. The seeds of Gossypium species vary widely in gossypol content, with levels ranging from 0.13% to 6.6%.USDA 2010, Wang 2009

History

Gossypol was first identified as an antifertility agent as a result of epidemiologic studies conducted in China during the 1950s. Investigators had noted extremely low birth rates in a particular geographic region and found the men in the region had very low sperm counts and many women had amenorrhea. Eventually the phenomenon was attributed to the use of crude cottonseed oil for cooking and the consumption of cotton cake left over after extraction of the oil and fiber from the cotton plant. Further investigation revealed that the antifertility component was gossypol; crystalline extracts were then supplied to Chinese doctors for widespread use in the 1970s as the principle contraceptive method in China. However, irreversible effects on fertility and cases of hypokalemia led to a reduced scientific interest in gossypol.Coutinho 2002

Chemistry

Gossypol is a polyphenolic compound that can be made synthetically or produced inexpensively on a very large scale by the extraction of cottonseed. Different versions of the compound have been developed to improve efficacy and reduce toxicity of the original chemical. Apogossypolone (ApoG2) and R-(-)-gossypol (AT-101) have been used in clinical trials.Azmi 2009, Cheson 2009, Wang 2009, Zhan 2009

Uses and Pharmacology

Antifertility/Contraceptive

Gossypol is a nonsteroidal compound that inhibits sperm production and motility in a variety of male animals and in humans, but it does not affect sex hormone levels or libido. Gossypol exerts its contraceptiv...