Histrelin

Products

Histrelin is commercially available as an implant (Vantas). It was approved in many countries in 2010.

Structure and properties

Histrelin is present in drugs as histrelin acetate. The nonapeptide is a synthetic analog of the natural gonadotropin-releasing hormone GnRH.

  • Histrelin: 5-oxo-Pro-His-Trp-Ser-Tyr-Ntbenzyl-D-His-Leu-Arg-N-ethyl-L-prolinamide.
  • GnRH: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly

Effects

Histrelin (ATC H01CA03) blocks the release of LH and FSH when used over the long term. This reduces testosterone concentrations, which inhibits hormone-dependent tumor growth.

Indications

For palliative treatment of advanced prostate cancer.

Dosage

According to the SmPC. The implant remains under the skin on the inner side of the upper arm (subcutaneous) for 12 months.

Contraindications

Histrelin is contraindicated in hypersensitivity and in women. For complete precautions, see the drug label.

Interactions

There are no known interactions with other drugs.

Adverse effects

The most common possible adverse effects include hot flashes, decreased libido, urinary dysfunction, and erectile dysfunction.