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Andarine

Chemical compound

Summary

Chemical compound

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Andarine (developmental code names GTx-007, S-4) is a selective androgen receptor modulator (SARM) which was developed by GTX, Inc for the treatment of conditions such as muscle wasting, osteoporosis, and benign prostatic hyperplasia (BPH), using the nonsteroidal antiandrogen bicalutamide as a lead compound. Development of andarine for all indications has been discontinued, in favor of the structurally related and improved compound enobosarm (ostarine; GTx-024; S-22).

Andarine is an orally active partial agonist of the androgen receptor (AR). In intact male rats, 0.5 mg andarine daily was shown to reduce prostate weight to 79.4%, and non-significantly increased levator ani muscle weight. In castrated male rats, this dose restored only 32.5% prostate weight, but 101% levator ani muscle weight This suggests that andarine is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist actions at the androgen receptor prevent the side effects associated with the antiandrogens traditionally used for treatment of BPH.

Andarine was first described in the literature by 2002. It completed phase 1 clinical trials for cachexia in 2003. Three phase 1 trials (1a, 1b, 1c) were completed with the drug involving 86 healthy male and female volunteers. Phase 2 trials were planned for 2004. However, development of andarine was discontinued, reportedly due to findings of visual disturbances in clinical studies. Andarine is thought to have been the first SARM to enter human clinical trials.

References

References

  1. (March 2003). "Pharmacodynamics of selective androgen receptor modulators". American Society for Pharmacology & Experimental Therapeutics (ASPET).
  2. (June 2005). "Discovery and therapeutic promise of selective androgen receptor modulators". Molecular Interventions.
  3. "Andarine". Springer Nature Switzerland AG.
  4. (December 2004). "Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia". Endocrinology.
  5. (August 2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research.
  6. (August 2002). "Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor". European Journal of Medicinal Chemistry.
  7. (March 2003). "Pharmacodynamics of selective androgen receptor modulators". The Journal of Pharmacology and Experimental Therapeutics.
  8. (2003). "The pharmacology, pharmacokinetics and metabolism of a novel nonsteroidal selective androgen receptor modulator".
  9. (June 2009). "Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit". Journal of Medicinal Chemistry.
  10. (22 December 2003). "Form S-1: GTx, Inc.". U.S. Securities and Exchange Commission.
  11. (May 2013). "Detection of the selective androgen receptor modulator S-4 (Andarine) in a doping control sample". Drug Testing and Analysis.
  12. (3 March 2004). "Form 8-K". U.S. Securities and Exchange Commission.
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1-nitro-2-(trifluoromethyl)benzene-derivatives 4-aminophenyl-compounds abandoned-drugs acetamides anilides phenol-ethers selective-androgen-receptor-modulators tertiary-alcohols
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