Deslorelin

Hormonal / Reproductive

Also known as: Suprelorin, Ovuplant, Deslorelin Acetate

GnRH AgonistsResearch phase: Approved (veterinary)Regulatory: Veterinary-approved (Suprelorin) in EU, Australia, and other markets. Not FDA-approved for human use. Some off-label human use for precocious puberty in certain countries.

Mechanism

Deslorelin is a synthetic GnRH agonist primarily used in veterinary medicine. Like leuprolide and goserelin in humans, it initially stimulates and then suppresses reproductive hormones through continuous GnRH receptor activation. It is used as a subcutaneous implant (Suprelorin) for chemical castration in dogs and for inducing ovulation in mares.

Technical detail

Deslorelin is a synthetic GnRH agonist nonapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt) with D-Trp6 substitution and C-terminal ethylamide modification conferring enhanced GnRHR binding affinity and resistance to enzymatic degradation. Chronic administration causes GnRHR downregulation on pituitary gonadotrophs, suppressing LH/FSH secretion and downstream gonadal steroidogenesis. Approximately 10-fold more potent than native GnRH. Available as a slow-release subcutaneous implant (4.7mg or 9.4mg) providing 6-12 months of suppression.

Evidence

Treatment of Endometriosis with the GnRHa Deslorelin and Add-Back Estradiol and Supplementary Testosterone.
Agarwal SK, Daniels A, Drosman SR, Udoff L, Foster WG, Pike MC (2015) — BioMed research international — PMID: 26881208
Randomized multicenter pilot trial reported substantial reduction in endometriosis symptom and sign scores over 3 to 6 months with daily intranasal deslorelin plus low-dose add-back hormones, with minimal BMD loss, hot flashes, or endometrial hyperplasia.
moderate
Reduced mammographic density with use of a gonadotropin-releasing hormone agonist-based chemoprevention regimen in BRCA1 carriers.
Weitzel JN, Buys SS, Sherman WH, Daniels A, Ursin G, Daniels JR (2007) — Clinical cancer research : an official journal of the American Association for Cancer Research — PMID: 17255289
Small open-label BRCA1-carrier study found a 29.2% median reduction in mammographic percent density over 12 months with intranasal deslorelin plus steroid add-back, while bone density and endometrial safety remained acceptable.
emerging

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