Histrelin

Definition

Like goserelin, triptorelin, buserelin and leuprorelin (Raja 2022), histrelin is a gonadotropin-releasing hormone agonist (GnRH) (Herold 2022).

Histrelin has been on the market since 2007 (Raja 2022). In the same year, it was approved for use in children with pubertas praecox (Olson- Kennedy 2021).

Pharmacodynamics

Histrelin inhibits the release of LH and FSH, which in turn reduces the testosterone concentration and thus inhibits hormone-dependent tumor growth. The bioavailability is 92 % and the plasma half-life is up to 4 h (Nabieva 2024).

When used s. c. as a 50 mg implant in pubertas praecox, there is a strong suppression of the hypothalamic-pituitary-gonadal axis (HPG) after approx. one month (Eugster 2016).

Indication

- Advanced prostate carcinoma as part of palliative therapy with chemical castration (Nabieva 2024 / Freissmuth 2012)

- Central pubertas praecox (Eugster 2015)

- On the suppression of puberty in transgender people (Olson- Kennedy 2021)

- Endometriosis

- Certain forms of breast carcinoma

- Uterus myomatosus

- Myomas (Freissmuth 2012)

Dosage and type of application

Histrelin is used as an implant (Nabieva 2024). It is effective for 12 months (Raja 2022).

Undesirable effects

- Hot flushes

- Headaches, joint and bone pain

- depression

- insomnia

- hematuria

- Respiratory diseases

- Liver diseases

- Local reactions at the site of application

- Gynecomastia

- Neuropathies

- dizziness

- dyspnea

- Nausea

- Constipation (Nabieva 2024)

- Removal of the implant in pubertas praecox has an approx. 25 % rupture rate (Eugster 2015)

Contraindication

Hypersensitivity to GnRH analogs (Nabieva 2024)

Preparations

Vantas®

1. Eugster E A (2016) Experience with the Histrelin Implant in Pediatric Patients. Endocr Dev. (30) 54 - 59 doi: 10.1159/000439330
2. Freissmuth M, Böhm S, Offermann S (2012) Pharmacology and Toxicology: From Molecular Basis to Pharmacotherapy. Springer Medizin Verlag Heidelberg 528
3. Herold G et al. (2022) Internal medicine. Herold Publishing House 118
4. Kasper D L et al (2015) Harrison's Principles of Internal Medicine. Mc Graw Hill Education
5. Olson- Kennedy J, Streeter L H, Garofalo R, Chan Y M, Rosenthal S M (2021) Histrelin Implants for Suppression of Puberty in Youth with Gender Dysphoria: A Comparison of 50 mcg/Day (Vantas) and 65 mcg/Day (SupprelinLA). Transgender Health 6 (1) 36 - 42
6. Nabieva N (2024) Histrelin. DocCheck Flexicon. DOI: https://flexikon.doccheck.com/en/Histrelin
7. Raja T, Sud R, Addla S, Sarkar K, Kalyan K, Sridhar P S, Talreja V, Jain M, Patil K (2022) Gonadotropin-releasing hormone agonists in prostate cancer: A comparative review of efficacy and safety. Indian Journal of Cancer 59 (1) 142 - 159