Section 02 · Monograph
Ubrogepant
Reviewed Nov 2026FDA label
UbrelvyGepant · oral
- Forms
- Tab: 50, 100mg
- Dose
- 50-100mg PRN (max 200mg/day)
- MOA
- CGRP receptor antagonist
Indications
- Acute treatment of migraine with or without aura in adultsFDA-labeled
- Not indicated for the preventive treatment of migraineFDA-labeled
Mechanism of Action
- Small-molecule calcitonin gene-related peptide (CGRP) receptor antagonist ("gepant")
- Blocks CGRP receptor activation, inhibiting CGRP-mediated neurogenic vasodilation and trigeminal nociceptive signaling implicated in migraine pathophysiology
- Does not cause vasoconstriction, distinguishing it mechanistically from triptans
Full Dosing
Adult / usual
- Initial dose: 50 mg or 100 mg orally, with or without food
- Repeat/second dose: an additional dose may be taken at least 2 hours after the initial dose if needed
- Maximum dose: 200 mg in a 24-hour period
- With moderate CYP3A4 inhibitors: limit to a single 50 mg dose in 24 hours
- With weak CYP3A4 inhibitors: 50 mg initial dose, second dose of 50 mg may be considered
- With strong or moderate CYP3A4 inducers: avoid concomitant use
Renal
- Renal impairment (severe, CLcr 15–29 mL/min): limit to 50 mg per dose
- Renal impairment (end-stage, CLcr <15 mL/min): avoid use
Hepatic
- Hepatic impairment (severe): initial dose 50 mg; if a second dose is needed, use 50 mg
Contraindications
- Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin)
- Known serious hypersensitivity to ubrogepant or any component of the formulation
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir): contraindicated — significantly increase ubrogepant exposure
- Moderate CYP3A4 inhibitors (e.g., verapamil, fluconazole): increase exposure — limit to single 50 mg dose per 24 hours
- Weak CYP3A4 inhibitors: modest increase in exposure — dose adjustment as above
- Strong or moderate CYP3A4 inducers (e.g., rifampin, carbamazepine): substantially decrease ubrogepant concentrations — avoid concomitant use
- BCRP and/or P-glycoprotein inhibitors (e.g., quinidine): may increase ubrogepant exposure — dose adjustment recommended
Adverse Effects
- Nausea (most common, ~2–4% depending on dose)
- Somnolence/fatigue
- Dry mouth
- Postmarketing reports: hypersensitivity reactions (including dyspnea, rash)
- Postmarketing reports: hypertension (new onset or worsening)
- Postmarketing reports: Raynaud's phenomenon
Monitoring Parameters
- Monitor for signs/symptoms of hypersensitivity reaction (can occur days after administration)
- Assess renal and hepatic function to guide dosing in impairment
- Screen concomitant medication list for CYP3A4 interacting drugs before and during therapy
- Monitor frequency of use to avoid medication-overuse headache with frequent dosing
Pregnancy & Lactation
- Pregnancy: Available human data are insufficient to establish drug-associated risk of major birth defects or miscarriage; animal studies showed embryofetal toxicity only at doses producing maternal toxicity
- Lactation: Ubrogepant is present in human breast milk in low amounts (relative infant dose approximately 0.15% of maternal weight-adjusted dose); no data on effects on milk production
- Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for ubrogepant and any potential adverse effects on the breastfed infant