Mechanism of Action
- Initial agonist activity: single dose causes GnRHR activation, LH/FSH surge, and transient testosterone/estradiol rise
- Continuous release from implant causes complete GnRHR desensitization and down-regulation within 2-4 weeks; castrate-level sex steroids maintained
- Suprelorin 4.7 mg (6-month) and 9.4 mg (12-month) implants used in dogs; equivalent testosterone suppression to surgical castration
- Ovuplant (2.1 mg deslorelin): single-use implant placed under clitoral fossa or vulva in mares to reliably induce ovulation within 36-42 hours
- Human off-label use: implant or compounded SC injection for testosterone suppression in gender-affirming care or fertility preservation
Research Findings
- Veterinary (Suprelorin): >95% of treated male dogs achieved testosterone suppression to castrate levels within 6 weeks; behavior modifications comparable to surgical castration
- Equine (Ovuplant): 90%+ of mares ovulated within 36-42 hours of deslorelin implant placement; reliable protocol for timed breeding
- Human research: small series of deslorelin implants in transgender adolescents showed complete GnRH axis suppression comparable to leuprolide or histrelin
- Fertility suppression in ferrets: Suprelorin effectively prevents adrenal disease (a common complication of surgical castration in ferrets) vs surgical approach
- Recovery after implant removal: GnRH axis recovery in 2-6 months in humans; testosterone returns to baseline in most cases
Research Protocols
- Canine (Suprelorin): single 4.7 mg SC implant for 6-month suppression or 9.4 mg for 12 months; implant between shoulder blades with trocar
- Equine (Ovuplant): single 2.1 mg implant under clitoral fossa when dominant follicle >35 mm; ovulation expected at 36-42 hours
- Human off-label puberty blockade: 3 mg SC injection monthly or 3.75 mg implant; monitor LH, FSH, estradiol/testosterone
- Ferret adrenal disease prevention: 4.7 mg implant SC every 12-18 months; monitor urinary cortisol and adrenal size by ultrasound
Interactions
- Anti-androgens (in veterinary or human use): short-term co-administration during first 2 weeks prevents testosterone flare after first implant
- Progesterone (equine use): sometimes combined to synchronize estrus before deslorelin-induced ovulation
- GnRH antagonists: would block deslorelin receptor binding; contraindicated for concurrent use
Safety Profile
Veterinary approval (Suprelorin, Ovuplant); not FDA-approved for humans. In veterinary use: well-tolerated with expected side effects of chemical castration (weight gain, coat changes, behavior changes). Human off-label use: similar safety to other GnRH agonists. Local implant reactions possible.
Legal & Regulatory
Veterinary approved (Suprelorin EU/AU; Ovuplant USA for mares); not FDA-approved for human use; used off-label in human medicine