Benorterone

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Benorterone (INN, USAN) (developmental code names SKF-7690, FC-612), also known as 17α-methyl-β-nortestosterone, is a steroidal, pure antiandrogen that was never marketed.[1] Unlike other steroidal antiandrogens such as cyproterone acetate (CPA), it is not also a progestogen, instead acting as a selective androgen receptor antagonist similarly to non-steroidal antiandrogens such as bicalutamide.[2][3] However, although it is described as not being a progestogen, benorterone was found to produce "a highly variable decrease in plasma testosterone levels"; the reasons for this are unclear, as other pure antiandrogens such as cyproterone (not CPA) and bicalutamide do not do this and instead produce consistent increases in testosterone levels).[3]

Developed in the late 1950s and trialed in the 1960s,[1] benorterone was the first antiandrogen to be studied in humans.[4] The drug was found to be effective in the treatment of acne, seborrhea, and hirsutism in women,[3][5][6] and unlike progestogenic antiandrogens such as CPA, seldom produced side effects in women, nor affected menstruation.[3] However, in men, the drug produced gynecomastia, and upon the observance of this side effect, was soon withdrawn from clinical trials.[4][3] Subsequently, CPA, which has a much reduced risk of gynecomastia by virtue of its antigonadotropic actions, was developed and introduced in 1973 instead.[7]

See also

References

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