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
Legal status
Legal status
  • Investigational new drug
Identifiers
CAS Number 401900-40-1 N
ATC code none
PubChem CID 9824562
IUPHAR/BPS 7849
DrugBank DB07423 YesY
ChemSpider 8000309 YesY
ChEMBL CHEMBL125236 YesY
Synonyms Acetamidoxolutamide, androxolutamide
Chemical data
Formula C19H18F3N3O6
Molar mass 441.357 g/mol
 NYesY (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]

See also[edit]

References[edit]

  1. ^ Hott, J. L.; Borkman, R. F. (1989). "The non-fluorescence of 4-fluorotryptophan". The Biochemical journal. 264 (1): 297–9. doi:10.1124/jpet.102.040840. PMC 1133577free to read. PMID 2604714. 
  2. ^ Chen, J; Kim, J; Dalton, J. T. (2005). "Discovery and therapeutic promise of selective androgen receptor modulators". Molecular interventions. 5 (3): 173–88. doi:10.1124/mi.5.3.7. PMC 2072877free to read. PMID 15994457. 
  3. ^ GGao, W; Kearbey, J. D.; Nair, V. A.; Chung, K; Parlow, A. F.; Miller, D. D.; Dalton, J. T. (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. 145 (12): 5420–8. doi:10.1210/en.2004-0627. PMC 2098692free to read. PMID 15308613. 
  4. ^ Gao, W; Kim, J; Dalton, J. T. (2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research. 23 (8): 1641–58. doi:10.1007/s11095-006-9024-3. PMC 2072875free to read. PMID 16841196.