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Histrelin Acetate

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CAT#
10-101-21
Synonyms/Alias
(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH
CAS No.
76712-82-8 (net)
Sequence
Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt acetate salt
M.W/Mr.
1323.5
Molecular Formula
C66H86N18O12
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children.
Description
Histrelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Areas of Interest
Hormonal therapy
  • Background
  • Related Products
  • References

Histrelin Acetate is the acetate salt form of histrelin, a long-acting, synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with potential anti-tumor activity. Upon administration, histrelin binds to and activates GnRH receptors; prolonged administration results in pituitary GnRH receptor desensitization and inhibition of follicle stimulating hormone (FSH) and luteinizing hormone (LH) secretion, leading to a significant decline in testosterone production in males and may inhibit androgen receptor-positive tumor progression; in females, prolonged administration results in decreased estradiol production.

CAS: 63968-82-1
Sequence: Asp-Val-Pro-Lys-Ser-Asp-Gln-Phe-Val-Gly-Leu-Met-NH2
M.W: 1334.54
Molecular Formula: C59H95N15O18S
CAS: 74381-53-6
Sequence: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
M.W: 1269.46
Molecular Formula: C59H84N16O12.C2H4O2
CAS: 50-57-7
Sequence: c[Cys-Tyr-Phe-Gln-Asn-Cys]-Pro-Lys-Gly-NH2
M.W: 1056.2
Molecular Formula: C46H65N13O12S2
CAS: 62305-91-3
Sequence: 6-Me-5-oxothiomorpholinyl-3-carbonyl-His-Pro-NH2
M.W: 408.48
Molecular Formula: C17H24N6O4S
CAS: 76932-56-4 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-D-2-Nal-Leu-Arg-Pro-Gly-NH2 acetate salt
M.W: 1322.5
Molecular Formula: C10H18N2O7

The once-yearly histrelin implant maintained testosterone suppression for repeated treatment cycles and was generally well tolerated. The histrelin implant provides a clinically attractive option for long-term androgen deprivation therapy in patients with advanced prostate cancer seeking fewer office visits and repeated injections.

Shore, N., Cookson, M. S., & Gittelman, M. C. (2012). Long‐term efficacy and tolerability of once‐yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU international, 109(2), 226-232.

The LHRH agonist histrelin acetate is the only available sustained-release hydrogel implant for once-yearly administration. The once-yearly implant allows patients to receive fewer cycles of implanting and replanting to maintain continuous ADT therapy. The histrelin acetate implant is 3.5 cm long, is 3 mm in diameter, and is administered subcutaneously into the inner aspect of the upper arm or abdomen. The inner aspect of the upper arm can clinically be difficult for the surgeon as it is a mobile insertion site and difficult for elderly patients limited by strength/arthritis to maintain the necessary abducted and extended arm position. Thus, the arm compared to the abdomen site is more difficult for surgeon and is less tolerated by patients.

Woolen, S., Holzmeyer, C., Nesbitt, E., & Siami, P. F. (2014). Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancer. Prostate cancer, 2014.

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