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| Routes of administration | Oral |
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| Formula | C20H23ClO2 |
| Molar mass | 330.85 g·mol−1 |
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Ethynerone (INN,USAN), also known as17α-(2-chloroethynyl)estra-4,9-dien-17β-ol-3-one, is asteroidalprogestin of the19-nortestosterone group that was first reported in 1961 but was never marketed.[1] Under the developmental code nameMK-665, it was studied incombination withmestranol as anoral contraceptive.[2] Development of the drug was discontinued due to concerns surrounding toxicity findings in dogs.[2] It is achloroethynylated derivative ofnorethisterone.[3]
In 1966, during itsclinical development, ethynerone was found to producemammary glandtumors in dogs treated with it at very high doses for prolonged periods of time.[4][5][6] Subsequent investigation found that17α-hydroxyprogesterone derivatives includedanagestone acetate,chlormadinone acetate,medroxyprogesterone acetate, andmegestrol acetate produced similar mammary gland tumors, and that their ability to do so correlated directly with their progestogenic actions.[6][7] In contrast, the non-halogenated19-nortestosterone derivativesnorgestrel,norethisterone,noretynodrel, andetynodiol diacetate, which are much less potent as progestogens, did not produce such effects at the dosages tested.[6] Clinical development of ethynerone was discontinued, and many of the 17α-hydroxyprogesterone derivatives were withdrawn for the indication ofhormonal contraception.[6][7] Research later on revealed species differences between dogs and humans and established that there is no similar risk in humans.[2]
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