Histrelin acetate
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Histrelin acetate

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An acetate salt obtained by combining histrelin with acetic acid. The amount of acetic acid present can vary and a variable amount of water may be present. Histrelin acetate is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.

Peptide Inhibitors
Catalog number
CAS number
Molecular Formula
Molecular Weight
1323.50 (free base)
Histrelin acetate
acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-(1-benzylimidazol-4-yl)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
1-9-Luteinizing hormone-releasing factor (swine), 6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-, acetate (1:x); 1-9-Luteinizing hormone-releasing factor (swine), 6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-, acetate (salt); Supprelin; H-Pyr-His-Trp-Ser-Tyr-D-His(1-Bn)-Leu-Arg-Pro-NHEt.xCH3CO2H; L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-L-arginyl-L-proline ethylamide acetic acid
Related CAS
76712-82-8 (free base) 2743427-40-7 (diacetate salt) 1233495-06-1 (monoacetate salt) 2240176-37-6 (TFA salt) 785814-23-5 (citrate salt)
XHWSYXLRP-NHEt.xCH3CO2H (Modifications: X-1 = Pyr, X-6 = D-His{1-Bn})
Store at -20°C
Soluble in DMSO
InChI Key
Canonical SMILES
1.Histrelin: in advanced prostate cancer.
Deeks ED1. Drugs. 2010 Mar 26;70(5):623-30. doi: 10.2165/11204800-000000000-00000.
Histrelin is a gonadotropin-releasing hormone agonist available in a diffusion-controlled reservoir drug delivery system for subcutaneous implantation. The subcutaneous histrelin implant provided sustained suppression of serum testosterone, luteinizing hormone (LH) and prostate-specific antigen levels for up to 1 year in patients with advanced prostate cancer in two phase II or III trials. In the noncomparative, multicentre, phase III study, serum testosterone was suppressed to castrate levels (i.e. < or =50 ng/dL) within 4 weeks in all patients who received a histrelin acetate 50 mg implant, with 99-100% of histrelin implant recipients maintaining castrate levels for the remainder of the 1-year treatment period. Such efficacy was provided irrespective of patient age or stage of disease. Although a transient surge in serum testosterone levels occurred after placement of the initial histrelin implant, no acute elevations in testosterone or LH levels were observed in patients whose implant was replaced after 1 year of therapy and suppression of these hormones continued to be maintained.
2.Efficacy and safety of histrelin subdermal implant in patients with advanced prostate cancer.
Schlegel PN1; Histrelin Study Group. J Urol. 2006 Apr;175(4):1353-8.
PURPOSE: This open label, multicenter study was done to evaluate the efficacy and safety of the gonadotropin hormone-releasing hormone agonist histrelin acetate administered as a 50 mg subdermal implant in men with advanced prostatic cancer.
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