Andarine Article

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Andarine
Andarine.svg
Clinical data
SynonymsAcetamidoxolutamide; Androxolutamide; GTx-007; S-4
ATC code
  • None
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
ChEMBL
ECHA InfoCard 100.230.653 Edit this at Wikidata
Chemical and physical data
FormulaC19H18F3N3O6
Molar mass441.357 g/mol
3D model ( JSmol)
  ‹See TfM›☒N☑Y  (what is this?)   (verify)

Andarine (developmental code names 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 nonsteroidal antiandrogen bicalutamide as a lead compound. [2]

Andarine is an orally active partial agonist of the androgen receptor (AR). 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 antiandrogenic 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 actions at the AR prevent the side effects associated with the antiandrogens traditionally used for treatment of BPH. [4]

See also

References

  1. ^ Hott JL, Borkman RF (November 1989). "The non-fluorescence of 4-fluorotryptophan". The Biochemical Journal. 264 (1): 297–9. doi: 10.1124/jpet.102.040840. PMC  1133577. PMID  2604714.
  2. ^ Chen J, Kim J, Dalton JT (June 2005). "Discovery and therapeutic promise of selective androgen receptor modulators". Molecular Interventions. 5 (3): 173–88. doi: 10.1124/mi.5.3.7. PMC  2072877. PMID  15994457.
  3. ^ GGao W, Kearbey JD, Nair VA, Chung K, Parlow AF, Miller DD, Dalton JT (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. 145 (12): 5420–8. doi: 10.1210/en.2004-0627. PMC  2098692. PMID  15308613.
  4. ^ Gao W, Kim J, Dalton JT (August 2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research. 23 (8): 1641–58. doi: 10.1007/s11095-006-9024-3. PMC  2072875. PMID  16841196.