Valette (drug)
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| Clinical data | |
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| Trade names | Visanne; With EV: Natazia, Qlaira; With EE: Valette |
| AHFS/Drugs.com | International Drug Names |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 90% |
| Protein binding |
Albumin (90%); Free (10%) |
| Metabolism | Hepatic (CYP3A4) |
| Metabolites | Inactive |
| Biological half-life | 10 hours |
| Excretion | Renal |
| Identifiers | |
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| Synonyms | M-18575, MJR-35, SH-660, STS-557, ZK-37659; 17α-Cyanomethyl-17β-hydroxy-estra-4,9(10)-dien-3-one; 17-Hydroxy-3-oxo-19-nor-17α-pregna-4,9-diene-21-nitrile |
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| ChEMBL | |
| ECHA InfoCard | 100.167.087 |
| Chemical and physical data | |
| Formula | C20H25NO2 |
| Molar mass | 311.42 g/mol |
| Density | 1.2 g/cm3 |
| Boiling point | 549 °C (1,020 °F) |
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Dienogest is a progestin, or a synthetic progestogen, of the 19-nortestosterone group. It is available in combination with estradiol valerate (as Natazia, Qlaira) or ethinylestradiol (as Valette) for use as an oral contraceptive, and by itself (as Visanne, Dinagest) for the treatment of endometriosis in Europe, Australia, and Japan. Although available in combination with estrogen as a contraceptive in the United States, dienogest is not available in this country by itself. In addition to its progestogenic effects, dienogest has antiandrogenic activity, and as a result can improve androgenic symptoms such as acne. It is a non-ethynylated progestin which is structurally related to testosterone.
Dienogest is used primarily as a contraceptive in combination with ethinylestradiol. It is given as a tablet containing 2 mg of dienogest and 30 μg of ethinylestradiol. Dienogest is also available in a quadriphasic oral contraceptive pill combined with estradiol valerate, marketed as Natazia in the United States and Qlaira in some European countries and Russia. This formulation is also approved for the treatment of heavy menstrual bleeding.
Dienogest is also approved in Europe, Australia, Malaysia, Singapore and Japan for the treatment of endometriosis. It has been shown to be equally effective as leuprorelin, which is a second line medication against endometriosis.
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