Osaterone acetate

Osaterone acetate
Clinical data
Trade names Ypozane
Routes of
By mouth (tablets)
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

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


  1. 1 2 3 4 Georg F. Weber (22 July 2015). Molecular Therapies of Cancer. Springer. pp. 316–. ISBN 978-3-319-13278-5.
  2. 1 2 Marthina L. Greer (18 December 2014). Canine Reproduction and Neonatology. Teton NewMedia. pp. 296–. ISBN 978-1-4987-2850-8.
  3. 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.
  4. Etienne Cote (9 December 2014). Clinical Veterinary Advisor: Dogs and Cats. Elsevier Health Sciences. pp. 848–. ISBN 978-0-323-24074-1.
  5. Stephen J. Ettinger; Edward C. Feldman (24 December 2009). Textbook of Veterinary Internal Medicine. Elsevier Health Sciences. pp. 2055–. ISBN 1-4377-0282-1.
  6. 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.
  7. Jill E. Maddison; Stephen W. Page; David Church (BVSc.) (2008). Small Animal Clinical Pharmacology. Elsevier Health Sciences. pp. 536–. ISBN 0-7020-2858-4.

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