Acyline

Acyline (developmental code name MER-104) is a gonadotropin-releasing hormone analogue (GnRH analogue) and gonadotropin-releasing hormone antagonist (GnRH antagonist) which was never marketed.[1][2][3] It has been shown to suppress gonadotropin and testosterone levels in men.[1][2][3] Acyline is a peptide and under normal circumstances is not orally active.[3] For this reason, it has instead been administered by subcutaneous injection.[1][2]

Acyline
Clinical data
Other namesMER-104
Routes of
administration
Subcutaneous injection[1][2]
Drug classGnRH antagonist
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC80H102ClN15O14
Molar mass1533.24 g·mol−1
3D model (JSmol)

See also

References

  1. Herbst KL, Anawalt BD, Amory JK, Bremner WJ (July 2002). "Acyline: the first study in humans of a potent, new gonadotropin-releasing hormone antagonist". J. Clin. Endocrinol. Metab. 87 (7): 3215–20. doi:10.1210/jcem.87.7.8675. PMID 12107227.
  2. Herbst KL, Coviello AD, Page S, Amory JK, Anawalt BD, Bremner WJ (December 2004). "A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men". J. Clin. Endocrinol. Metab. 89 (12): 5959–65. doi:10.1210/jc.2003-032123. PMID 15579744.
  3. Amory JK, Leonard TW, Page ST, O'Toole E, McKenna MJ, Bremner WJ (August 2009). "Oral administration of the GnRH antagonist acyline, in a GIPET-enhanced tablet form, acutely suppresses serum testosterone in normal men: single-dose pharmacokinetics and pharmacodynamics". Cancer Chemother. Pharmacol. 64 (3): 641–5. doi:10.1007/s00280-009-1038-1. PMC 2721900. PMID 19479252.



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