Lonaprisan
Lonaprisan (INN, USAN) (developmental code names ZK-230211, BAY 86-5044, ZK-PRA) is a synthetic, steroidal antiprogestogen which was under development by Bayer HealthCare Pharmaceuticals for the treatment of endometriosis, dysmenorrhea, and breast cancer but was discontinued.[1][2][3] It is a potent and highly selective silent antagonist of the progesterone receptor (PR).[2][3][4] The drug reached phase II clinical trials prior to its discontinuation.[1]
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| Other names | ZK-230211; BAY 86-5044; ZK-PRA; 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)estra-4,9-dien-3-one |
| Routes of administration | Oral |
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| ECHA InfoCard | 100.190.674  |
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| Formula | C28H29F5O3 |
| Molar mass | 508.529 g·mol−1 |
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References
- "Lonaprisan - AdisInsight". adisinsight.springer.com.
- Whitaker LH, Williams AR, Critchley HO (2014). "Selective progesterone receptor modulators". Curr. Opin. Obstet. Gynecol. 26 (4): 237–42. doi:10.1097/GCO.0000000000000082. PMID 24950125. S2CID 37474964.
- Pluchino N, Freschi L, Wenger JM, Streuli I (2016). "Innovations in classical hormonal targets for endometriosis". Expert Rev Clin Pharmacol. 9 (2): 317–27. doi:10.1586/17512433.2016.1129895. PMID 26645363. S2CID 8624056.
- Busia L, Faus H, Hoffmann J, Haendler B (2011). "The antiprogestin Lonaprisan inhibits breast cancer cell proliferation by inducing p21 expression". Mol. Cell. Endocrinol. 333 (1): 37–46. doi:10.1016/j.mce.2010.11.034. PMID 21138753. S2CID 12818061.
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