Deslorelin

Summary

Deslorelin is a potent synthetic GnRH superagonist used primarily in veterinary medicine for suppression of reproductive function. In humans, it has been investigated and used (under named-patient or compassionate-use programs in some countries) for precocious puberty, endometriosis, and as a component of gender-affirming hormone therapy in transgender youth. Approved veterinary products (Suprelorin) are available in several countries.

Mechanism of Action

Binds to pituitary GnRH receptors with high affinity; initial stimulation followed by receptor downregulation and desensitization leads to sustained suppression of LH and FSH secretion, resulting in decreased gonadal steroid production (testosterone in males, estradiol in females).

Routes of Administration

Goals & Uses

• Suppression of precocious pubertyEndocrinology / PediatricsModerate
• Gender-affirming puberty suppression (transgender youth)Endocrinology / Gender MedicineModerate
• Prostate cancer palliationOncologyLow
• Endometriosis treatmentGynecologyModerate
• Veterinary fertility control (male dogs)Veterinary MedicineHigh

Contraindications

• Undiagnosed vaginal bleedingGynecologicalModerate
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Hypersensitivity to GnRH or GnRH analogsAllergy / ImmunologyHigh
• Known or suspected hormone-sensitive malignancy (non-prostate, non-target)OncologyModerate

Adverse Effects

• Hot flashes / vasomotor symptomsAutonomic / ThermoregulatoryCommon
• Injection/implant site reactionsDermatological / LocalCommon
• AnaphylaxisImmunologicRareSevere life-threatening allergic reaction
• Decreased bone mineral densityMusculoskeletalCommon
• Mood changes / depressionPsychiatricUncommon
• Hormone flare (initial testosterone/estradiol surge)EndocrineCommon

Drug Interactions

• Androgen or estrogen supplementationModerate
• Antidiabetic agentsLow
• QT-prolonging agentsModerate

Population Constraints

• Osteoporosis or low bone densityMusculoskeletalRelative
• Pediatric patients (prepubertal)AgeRelative
• Patients with cardiovascular diseaseComorbidityRelative
• BreastfeedingReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Temporary suppression of fertility in male dogs (veterinary)Suprelorin implant approved by EMA for veterinary use. Human use is off-label or under named-patient programs in individual EU member states.
• United StatesUnapprovedNot FDA-approved for human use. Used in investigational or compassionate-use contexts. Ovuplant was previously used in equine medicine but not for humans.
• United KingdomApprovedApproved: Temporary suppression of fertility in male dogs (veterinary)Veterinary approval maintained post-Brexit. Human use in gender clinics (e.g., NHS) has occurred under specialist oversight.

Approved as a veterinary implant (Suprelorin) in the EU, Australia, and other jurisdictions for temporary suppression of fertility in male dogs. Not FDA-approved for human use in the US; used off-label or under compassionate use in some countries for precocious puberty and gender dysphoria.

Evidence & Sources

No sources recorded yet.