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| Clinical data | |
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| Trade names | Arterolo, Atheran, Colesterel, Iposclerone, Liprotene, Persclerol |
| Other names | SC-8246; 16α-Chloroestrone 3-methyl ether; 16α-Chloro-3-methoxyestra-1,3,5(10)-trien-17-one |
| Routes of administration | By mouth |
| Drug class | Estrogen;Estrogen ether |
| Identifiers | |
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| CAS Number | |
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| ChemSpider | |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.021.669 |
| Chemical and physical data | |
| Formula | C19H23ClO2 |
| Molar mass | 318.84 g·mol−1 |
| 3D model (JSmol) | |
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Clomestrone (brand namesArterolo,Atheran,Colesterel,Iposclerone,Liprotene,Persclerol, others; former developmental code nameSC-8246), also known as16α-chloroestrone 3-methyl ether, is asynthetic,steroidal, weakestrogen derived fromestrone and used as ananticholesterolemic agent in the treatment ofatherosclerosis.[1][2]
It is said to have beneficial effects onserumlipid profiles while producing minimalfeminization, though some estrogenicside effects, includingbreast tenderness, loss oflibido, andfatigue oravolition, were observed in most patients in clinical studies.[3][4] The drug is a closeanalogue ofmytatrienediol, and the two estrogens have similar drug profiles.[5] Clomestrone was described in the literature in 1958 and introduced for medical use shortly thereafter.[1]
SC-8246 (16-alpha chlorestrone 3-methyl ether) was administered for periods of six to twelve months to 20 male survivors of acute myocardial infarction ranging in age from 30 to 63 years. A significant decrease in serum cholesterol concentration occurred in only 6 of 13 patients with an initial cholesterol level above 250 mg. per 100 ml., and there was no change in the other 7. Of 7 initial cholesterol levels below 250 mg. per 100 ml., no level decreased, 3 increased, and 4 were unchanged. In 9 of 11 patients with an initial alpha:beta lipoprotein ratio of less than 20 per cent, a significant increase occurred, but no change in the other 2. Among 9 subjects with a ratio initially above 20 per cent, a further increase occurred in 8 while taking the drug. This estrogen appeared to have an advantage in terms of lessening side-effects. Mild breast tenderness or gynecomastia occurred in 15 of the 17 patients with a "favorable" lipoprotein change. When the dosage was reduced to 5 mg. daily or every other day, the lipoprotein effect in 8 of them could be sustained while the breast changes disappeared. Libido disappeared from 2 patients and was diminished in 1 other. Other side-effects were nausea in 1 patient, loss of ambition in 5, and itching or dryness of the skin in 4.
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