Osaterone acetate
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| Clinical data | |
|---|---|
| Trade names | Ypozane |
| Routes of administration | By mouth (tablets) |
| Identifiers | |
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| Synonyms | TZP-4238; 2-Oxachloromadinone acetate; 17α-Acetoxy-6-chloro-2-oxa-6-dehydroprogesterone; 17α-Acetoxy-6-chloro-2-oxapregna-4,6-diene-3,20-dione |
| CAS Number | 105149-00-6 |
| PubChem (CID) | 114992 |
| ChemSpider | 102924 |
| Chemical and physical data | |
| Formula | C22H27ClO5 |
| Molar mass | 406.89978 g/mol |
| 3D model (Jmol) | Interactive image |
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Osaterone acetate (brand name Ypozane; former developmental code name TZP-4238), also known as 17α-acetoxy-6-chloro-2-oxa-6-dehydroprogesterone, as well as 2-oxachloromadinone acetate, is a steroidal antiandrogen and progestogen used in veterinary medicine in Europe in the treatment of benign prostatic hyperplasia (BPH) in dogs.[1][2] It was also investigated in Japan in the treatment of prostate cancer and BPH in humans but was never marketed for these indications.[1][3] Osaterone acetate produces remission of clinical symptoms of BPH in ~83% of dogs for six months after a single one-week course of treatment,[4] and can be used long-term.[2] It is a 17α-hydroxyprogesterone derivative and a derivative of the less potent chlormadinone acetate.[1] The drug is the C17α acetate ester of osaterone.
Osaterone acetate has virtually no estrogenic or androgenic activity.[1] However, it can decrease cortisol levels, interfere with adrenocorticotropic hormone response, induce or exacerbate adrenal insufficiency, and exacerbate diabetes mellitus, side effects indicative that it possesses clinically relevant glucocorticoid properties.[5][6] Other side effects of osaterone acetate include diminished sperm quality (for up to 6 weeks post-treatment), transient elevation of liver enzymes (caution should be observed with known liver disease), vomiting, diarrhea, polyuria/polydipsia, lethargy, and hyperplasia of the mammary glands.[6] The drug has a long half-life of 197 ± 109 hours in dogs.[7]
See also
References
- 1 2 3 4 Georg F. Weber (22 July 2015). Molecular Therapies of Cancer. Springer. pp. 316–. ISBN 978-3-319-13278-5.
- 1 2 Marthina L. Greer (18 December 2014). Canine Reproduction and Neonatology. Teton NewMedia. pp. 296–. ISBN 978-1-4987-2850-8.
- ↑ JORDAN V. CRAIG; B.J.A. Furr (5 February 2010). Hormone Therapy in Breast and Prostate Cancer. Springer Science & Business Media. pp. 328–. ISBN 978-1-59259-152-7.
- ↑ Etienne Cote (9 December 2014). Clinical Veterinary Advisor: Dogs and Cats. Elsevier Health Sciences. pp. 848–. ISBN 978-0-323-24074-1.
- ↑ Stephen J. Ettinger; Edward C. Feldman (24 December 2009). Textbook of Veterinary Internal Medicine. Elsevier Health Sciences. pp. 2055–. ISBN 1-4377-0282-1.
- 1 2 Catherine Lamm; Chelsea Makloski (28 May 2012). Theriogenology, An Issue of Veterinary Clinics: Small Animal Practice. Elsevier Health Sciences. pp. 112–. ISBN 1-4557-4447-6.
- ↑ Jill E. Maddison; Stephen W. Page; David Church (BVSc.) (2008). Small Animal Clinical Pharmacology. Elsevier Health Sciences. pp. 536–. ISBN 0-7020-2858-4.