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GENITO URINARY SYSTEM AND SEX HORMONES › OTHER GYNECOLOGICALS › OTHER GYNECOLOGICALS › Other gynecologicals
fezolinetant
G02CX06
Adult Dosing
- Moderate to severe vasomotor symptoms associated with menopause: 45 mg orally once daily with or without food
- Swallow whole; do not crush, cut, or chew
Pediatric Dosing
- Not indicated for pediatric use
Indications
- Treatment of moderate to severe vasomotor symptoms due to menopause
Mechanism of Action
- Selective neurokinin 3 (NK3) receptor antagonist
- Blocks neurokinin B binding on KNDy neurons in the hypothalamus to modulate neuronal activity and restore body temperature control
Contraindications
- Known cirrhosis or severe hepatic impairment
- Severe renal impairment or end-stage renal disease (eGFR < 30 mL/min/1.73 m²)
- Concomitant use with strong CYP1A2 inhibitors (e.g., fluvoxamine)
- Known hypersensitivity to fezolinetant or any excipients
Adverse Reactions
- Abdominal pain
- Diarrhea
- Insomnia
- Back pain
- Elevated transaminases (ALT/AST)
Drug Interactions
- Strong CYP1A2 inhibitors: Contraindicated due to significantly increased fezolinetant exposure
- Moderate CYP1A2 inhibitors: May increase fezolinetant exposure; monitor for adverse reactions
- CYP1A2 inducers: May decrease fezolinetant efficacy
Curated Content: Needs Vetting Before Put to Clinical Use