TFM-4AS-1 explained

TFM-4AS-1 is a dual selective androgen receptor modulator (SARM) and 5α-reductase inhibitor.[1] [2] It is a potent and selective partial agonist (Emax = 55%) of the androgen receptor (IC50 = 30nM) and inhibitor of 5α-reductase types I and II (IC50 = 2 and 3 nM, respectively). TFM-4AS-1 shows tissue-selective androgenic effects; it promotes the accumulation of bone and muscle mass and has reduced effects in reproductive tissues and sebaceous glands. In an animal study, TFM-4AS-1 stimulated sebaceous gland formation only 31% as much as dihydrotestosterone (DHT) at doses that were as anabolic or more so than DHT.[3] In addition, TFM-4AS-1 only weakly promoted growth of the prostate gland and it partially antagonized the actions of DHT in the seminal vesicles and endogenous androgens in the prostate gland. Structurally, TFM-4AS-1 is a 4-azasteroid. A structurally related and more advanced version of TFM-4AS-1, MK-0773, was developed and pursued for potential pharmaceutical use.

See also

Notes and References

  1. Tolman RL, Sahoo SP, Bakshi RK, Gratale D, Patel G, Patel S, Toney J, Chang B, Harris GS . 4-Methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-N-aryl-carboxamides: an approach to combined androgen blockade [5alpha-reductase inhibition with androgen receptor binding in vitro] . J. Steroid Biochem. Mol. Biol. . 60 . 5–6 . 303–9 . 1997 . 9219921 . 10.1016/s0960-0760(96)00199-9. 54405031 .
  2. Schmidt A, Harada S, Kimmel DB, Bai C, Chen F, Rutledge SJ, Vogel RL, Scafonas A, Gentile MA, Nantermet PV, McElwee-Witmer S, Pennypacker B, Masarachia P, Sahoo SP, Kim Y, Meissner RS, Hartman GD, Duggan ME, Rodan GA, Towler DA, Ray WJ . Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands . J. Biol. Chem. . 284 . 52 . 36367–76 . 2009 . 19846549 . 2794752 . 10.1074/jbc.M109.049734 . free .
  3. Zhang X, Sui Z . Deciphering the selective androgen receptor modulators paradigm . Expert Opin Drug Discov . 8 . 2 . 191–218 . February 2013 . 23231475 . 10.1517/17460441.2013.741582 . 2584722 .

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