Tanaproget (INN; developmental code names NSP-989, WAY-166989) is an investigational nonsteroidal progestin.[1] It is a high affinity, high efficacy, and very selective agonist of the progesterone receptor (PR).[1] Due to its much more selective binding profile relative to most conventional, steroidal progestins, tanaproget may prove to produce fewer side effects in comparison.[1] As of December 2010,[2] it is in phase II clinical trials in the process of being developed for clinical use as a contraceptive by Ligand Pharmaceuticals.[3][4]

An analog of tanaproget, 4-fluoropropyltanaproget (18F), has been developed as a radiotracer for imaging of the PR in positron emission tomography.[5]

See also

References

  1. ^ a b c Zhang Z, Olland AM, Zhu Y, et al. (August 2005). "Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget". J. Biol. Chem. 280 (31): 28468–75. doi:10.1074/jbc.M504144200. PMID 15937332.
  2. ^ Tanaproget
  3. ^ Bapst JL, Ermer JC, Ferron GM, Foss D, Orczyk GP (November 2006). "Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women". Contraception. 74 (5): 414–8. doi:10.1016/j.contraception.2006.06.004. PMID 17046384.
  4. ^ Bayés M, Rabasseda X, Prous JR (September 2005). "Gateways to clinical trials". Methods Find Exp Clin Pharmacol. 27 (7): 505–22. PMID 16258596.
  5. ^ Lee JH, Zhou HB, Dence CS, Carlson KE, Welch MJ, Katzenellenbogen JA (June 2010). "Development of [F-18]fluorine-substituted Tanaproget as a progesterone receptor imaging agent for positron emission tomography". Bioconjug. Chem. 21 (6): 1096–104. doi:10.1021/bc1001054. PMID 20496889.


Allikas: https://en.wikipedia.org/wiki/Tanaproget
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