Metapristone Explained

Metapristone (developmental code name RU-42633; also known as desmethylmifepristone) is the major metabolite of mifepristone (RU-486, RU-38486) and a selective progesterone receptor modulator (SPRM) which itself was never marketed.[1] [2] [3] [4] It is formed from mifepristone in the liver by the enzyme CYP3A4 via monodemethylation, and circulates at concentrations higher than those of mifepristone.[5] The metabolite retains partial but considerable affinity for the progesterone receptor (PR) and the glucocorticoid receptor (GR) (= 21% and 61% of that of mifepristone for the human forms of these receptors, respectively).[6] On the basis of actions that are apparently independent of its hormonal activity, metapristone is being researched as a potential cancer metastatic chemopreventive agent.

Notes and References

  1. Heikinheimo O . Clinical pharmacokinetics of mifepristone . Clin Pharmacokinet . 33 . 1 . 7–17 . July 1997 . 9250420 . 10.2165/00003088-199733010-00002 . 25101911 .
  2. Wang J, Chen J, Wan L, Shao J, Lu Y, Zhu Y, Ou M, Yu S, Chen H, Jia L . Synthesis, spectral characterization, and in vitro cellular activities of metapristone, a potential cancer metastatic chemopreventive agent derived from mifepristone (RU486) . AAPS J . 16 . 2 . 289–98 . March 2014 . 24442753 . 3933578 . 10.1208/s12248-013-9559-2 .
  3. Wang J, Chen J, Zhu Y, Zheng N, Liu J, Xiao Y, Lu Y, Dong H, Xie J, Yu S, Shao J, Jia L . In vitro and in vivo efficacy and safety evaluation of metapristone and mifepristone as cancer metastatic chemopreventive agents . Biomed. Pharmacother. . 78 . 291–300 . March 2016 . 26898454 . 10.1016/j.biopha.2016.01.017 .
  4. Chen W, Xiao Y, Chen J, Liu J, Shao J, Li T, Zhu Y, Ma J, Gao Y, Wang J, Xu J, Lu Y, Jia L . Sex-related pharmacokinetic differences and mechanisms of metapristone (RU486 metabolite) . Sci Rep . 7 . 1 . 17190 . December 2017 . 29215040 . 5719405 . 10.1038/s41598-017-17225-0 . 2017NatSR...717190C .
  5. Book: United States Pharmacopeial Convention. USP DI: United States Pharmacopeia Dispensing Information. 2006. United States Pharmacopeial Convention. 978-1-56363-574-8. 1992.
  6. Heikinheimo O, Kekkonen R, Lähteenmäki P . The pharmacokinetics of mifepristone in humans reveal insights into differential mechanisms of antiprogestin action . Contraception . 68 . 6 . 421–6 . December 2003 . 14698071 . 10.1016/S0010-7824(03)00077-5 .

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