Follitropin

Summary

Follitropin is a recombinant or urinary-derived follicle-stimulating hormone (FSH) used clinically to stimulate follicular development in women undergoing assisted reproduction and to treat infertility due to hypogonadotropic hypogonadism in both sexes. Several formulations exist including follitropin alfa (Gonal-F), follitropin beta (Follistim/Puregon), and follitropin delta (Rekovelle).

Mechanism of Action

Follitropin (FSH) binds to FSH receptors on granulosa cells (in females) and Sertoli cells (in males), stimulating follicular development and estrogen production in females, and supporting spermatogenesis in males via cAMP-mediated signaling pathways.

Routes of Administration

Goals & Uses

• Ovulation induction in anovulatory womenReproductive EndocrinologyHigh
• Treatment of male infertility due to hypogonadotropic hypogonadismMale Reproductive HealthHigh
• Controlled ovarian stimulation for ARTReproductive EndocrinologyHigh
• Stimulation of spermatogenesisMale Reproductive HealthModerate

Contraindications

• Hormone-sensitive tumors (ovarian, uterine, breast, pituitary)OncologyHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Primary ovarian failure / hypergonadotropic hypogonadismEndocrineHigh
• Uncontrolled thyroid or adrenal dysfunctionEndocrinologyHigh
• Ovarian cysts or enlargement of undetermined originGynecologicHigh
• Hypersensitivity to FSH or excipientsImmunologicHigh

Adverse Effects

• Injection site reactionsLocalCommon
• Multiple gestationReproductiveUncommon
• HeadacheNeurologicCommonPain in the head or upper neck
• Thromboembolic eventsCardiovascularRare
• Ovarian torsionReproductiveRare
• Ovarian hyperstimulation syndrome (OHSS)ReproductiveUncommon

Drug Interactions

• Human Chorionic Gonadotropin (hCG)Low
• GnRH antagonists (e.g., cetrorelix, ganirelix)Low
• Clomiphene citrateLow
• GnRH agonists (e.g., leuprolide)Low

Population Constraints

• Pediatric patientsAgeAbsolute
• Patients with thrombophiliaHematologicRelative
• Women of advanced reproductive age (>40 years)AgeRelative
• Patients with polycystic ovary syndrome (PCOS)EndocrineRelative
• Renal or hepatic impairmentOrgan DysfunctionRelative

Regulatory Status

• European UnionApprovedApproved: Controlled ovarian stimulation for ART, Anovulatory infertility including PCOS, Male hypogonadotropic hypogonadismGonal-F, Puregon, Rekovelle (follitropin delta), and biosimilars (Ovaleap, Bemfola) are EMA-approved.
• United StatesApprovedApproved: Controlled ovarian stimulation for ART, Induction of ovulation in anovulatory infertile women, Induction of spermatogenesis in hypogonadotropic hypogonadal menGonal-F (follitropin alfa) and Follistim AQ (follitropin beta) are FDA-approved. Biosimilar Bemfola approved in EU but not US.
• United KingdomApprovedApproved: Controlled ovarian stimulation for ART, Anovulatory infertility, Male infertility due to hypogonadotropic hypogonadismMHRA-approved products include Gonal-F, Puregon, and Rekovelle; biosimilars also available.

Multiple follitropin products are FDA-approved and EMA-approved for controlled ovarian stimulation and treatment of infertility. Biosimilar versions are also approved in some jurisdictions.

Evidence & Sources

No sources recorded yet.