ubrogepant
Brand: Ubrelvy
Prototype Drug
Drug Class: CGRP receptor antagonist (gepant)
Drug Family: antimigraine
Subclass: small-molecule CGRP receptor antagonist
Organ Systems: cns
Mechanism of Action
First FDA-approved small-molecule CGRP receptor antagonist for acute migraine; blocks CGRP-mediated trigeminal neuroinflammation and vasodilation without vasoconstriction. First gepant approved, establishing the class.
CGRP receptor
Indications
- acute treatment of migraine with or without aura (adults)
Contraindications
- concurrent strong CYP3A4 inhibitors
- concurrent strong CYP3A4 inducers
Adverse Effects
Common
- nausea
- somnolence
- dry mouth
Serious
- hypersensitivity reactions
- hepatotoxicity (rare)
Pharmacokinetics (ADME)
| Absorption | oral; bioavailability ~47%; food has minimal effect |
| Distribution | protein binding ~87% |
| Metabolism | primarily CYP3A4 |
| Excretion | fecal (~42%) and renal (~42%) |
| Half-life | 5-7 hours |
| Onset | 1-2 hours |
| Peak | 1.5 hours |
| Duration | 24 hours |
| Protein Binding | 87% |
| Vd | not well characterized |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 inhibitors | increase ubrogepant exposure; use 50 mg dose and no repeat dose within 24 hours | major |
| moderate CYP3A4 inhibitors | increase ubrogepant; use 50 mg dose | moderate |
| strong/moderate CYP3A4 inducers | decrease ubrogepant efficacy; avoid | major |
Nursing Considerations
- No cardiovascular contraindications; suitable alternative to triptans in patients with vascular disease.
- Can be taken with or without food; second dose may be taken 2 hours after first if migraine persists.
- Drug interaction with CYP3A4 inhibitors requires dose adjustment; verify all concurrent medications before prescribing.
- Distinguish from preventive CGRP therapies (erenumab, fremanezumab, galcanezumab); ubrogepant is for acute treatment only.
Clinical Pearls
- Ubrogepant established the gepant class as effective acute migraine therapy without cardiovascular concerns of triptans; its approval in 2019 represented the first CGRP pathway drug approved for acute treatment.
- Unlike erenumab and other anti-CGRP monoclonal antibodies (which block the ligand or receptor for prevention), gepants work acutely as small-molecule antagonists.
Safety Profile
Pregnancy avoid
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Guideline Update pending
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.