Andarine

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Andarine
Andarine.svg
Systematic (IUPAC) name
(2S)-3-(4-acetamido-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide
Clinical data
Legal status
  • Investigational new drug
Identifiers
CAS number 401900-40-1 N
ATC code None
PubChem CID 9824562
DrugBank DB07423
ChemSpider 8000309 YesY
ChEMBL CHEMBL125236 YesY
Chemical data
Formula C19H18F3N3O6 
Mol. mass 441.357 g/mol
 N (what is this?)  (verify)

Andarine (GTx-007, S-4) is an investigational selective androgen receptor modulator (SARM) developed by GTX, Inc for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy,[1] using the non-steroidal androgen antagonist bicalutamide as a lead compound.[2]

Andarine is an orally active partial agonist for androgen receptors. It is less potent in both anabolic and androgenic effects than other SARMs. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.[3] This suggests that it is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist effects at androgen receptors prevent the side effects associated with the anti-androgenic drugs traditionally used for treatment of BPH.[4]

References[edit]

  1. ^ Yin D, Gao W, Kearbey JD, Xu H, Chung K, He Y, Marhefka CA, Veverka KA, Miller DD, Dalton JT. Pharmacodynamics of selective androgen receptor modulators. Journal of Pharmacology and Experimental Therapeutics. 2003 Mar;304(3):1334-40. doi:10.1124/jpet.102.040840 PMID 12604714
  2. ^ Chen J, Kim J, Dalton JT. Discovery and therapeutic promise of selective androgen receptor modulators. Molecular Interventions. 2005 Jun;5(3):173-88. doi:10.1124/mi.5.3.7 PMID 15994457
  3. ^ Gao W, Kearbey JD, Nair VA, Chung K, Parlow AF, Miller DD, Dalton JT. 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. 2004 Dec;145(12):5420-8. PMID 15308613
  4. ^ Gao W, Kim J, Dalton JT. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands. Pharmaceutical Research. 2006 Aug;23(8):1641-58. PMID 16841196