Ubrelvy (Ubrogepant)
Indications
| Indication | Approved Population | Therapy Type | Status |
|---|---|---|---|
| Acute treatment of migraine, with or without aura | Adults (≥18 years) | Monotherapy (acute, as-needed) | FDA Approved |
Ubrogepant is approved by the U.S. FDA only; it does not currently hold marketing authorisation in the European Union. The indication is narrow: acute, abortive treatment of an active migraine attack in adults. The label explicitly states that ubrogepant is not indicated for migraine prevention, and that the safety of treating more than 8 migraines in a 30-day period has not been established.
The principal clinical role is as an oral, non-vasoconstrictive option for adults requiring acute migraine therapy. It is particularly useful when triptans are ineffective, poorly tolerated, or contraindicated — most notably in patients with established or high-risk cardiovascular disease. The 2021 American Headache Society consensus statement positions gepants as appropriate acute therapy for patients with cardiovascular contraindications to triptans, and as a reasonable choice when triptans fail or are not tolerated.
Treatment during the migraine prodrome: The phase 3 PRODROME trial (Dodick et al., Lancet 2023) showed that ubrogepant 100 mg taken during prodromal symptoms (1–6 hours before headache) reduced the development of moderate-to-severe headache compared with placebo. While the FDA-approved indication remains acute treatment of an established migraine, prodromal dosing is supported by RCT-level evidence — quality moderate.
Use in patients on CGRP-targeted monoclonal antibody preventives: No clinically significant pharmacokinetic interaction was demonstrated between ubrogepant and erenumab or galcanezumab in dedicated DDI studies; combination is increasingly used in clinical practice for breakthrough attacks — quality moderate.
Dosing
Ubrogepant is taken at the onset of a migraine attack and may be repeated once after at least 2 hours if the headache persists or recurs. The maximum dose in any 24-hour period is 200 mg in healthy adults. Both available strengths (50 mg and 100 mg) are clinically active; the higher strength offers a modest numeric advantage in pivotal trials.
| Clinical Scenario | Starting Dose | Repeat Dose (≥2 h) | Maximum / 24 h | Notes |
|---|---|---|---|---|
| Acute migraine — otherwise healthy adult, no dose-modifying conditions | 50 mg or 100 mg PO | 50 mg or 100 mg PO | 200 mg | Take at onset of attack; with or without food Safety not established for >8 migraines/30 days |
| Migraine with prior triptan failure or cardiovascular contraindication to triptans | 50 mg or 100 mg PO | 50 mg or 100 mg PO | 200 mg | Preferred over triptans in coronary artery disease, prior MI, prior stroke No vasoconstrictive activity |
| Co-administration with moderate CYP3A4 inhibitor (e.g. verapamil, diltiazem, fluconazole, ciprofloxacin, fluvoxamine, cyclosporine, grapefruit juice) | 50 mg PO | Avoid within 24 h | 50 mg | Verapamil increases AUC ~3.5-fold Single 50 mg dose only in 24 h |
| Co-administration with weak CYP3A4 inhibitor | 50 mg PO | 50 mg PO | 100 mg | Predicted ≤2-fold rise in exposure |
| Co-administration with strong CYP3A4 inhibitor (e.g. ketoconazole, itraconazole, clarithromycin, ritonavir, cobicistat) | Contraindicated | Ketoconazole increases AUC ~9.7-fold Use alternative acute migraine therapy | ||
| Co-administration with weak or moderate CYP3A4 inducer (e.g. modafinil, efavirenz, etravirine) | 100 mg PO | 100 mg PO | 200 mg | Use higher strength to offset induction No dedicated DDI study; based on conservative prediction of ~50% reduction |
| Co-administration with strong CYP3A4 inducer (e.g. rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s wort) | Avoid | Rifampin reduced AUC by 80% Loss of efficacy expected | ||
| Co-administration with BCRP and/or P-gp only inhibitor (e.g. quinidine, carvedilol, eltrombopag, curcumin) | 50 mg PO | 50 mg PO | 100 mg | Predicted ≤2-fold rise in exposure |
Dose Adjustment for Renal Impairment
| Renal Function | Starting Dose | Repeat Dose | Maximum / 24 h | Notes |
|---|---|---|---|---|
| Mild–moderate (CrCl 30–89 mL/min) | 50 or 100 mg | 50 or 100 mg | 200 mg | No adjustment |
| Severe (CrCl 15–29 mL/min) | 50 mg | 50 mg | 100 mg | Use 50 mg strength only |
| End-stage renal disease (CrCl <15 mL/min) | Avoid | Pharmacokinetics not characterised | ||
Dose Adjustment for Hepatic Impairment
| Hepatic Function | Starting Dose | Repeat Dose | Maximum / 24 h | Notes |
|---|---|---|---|---|
| Mild (Child-Pugh A) | 50 or 100 mg | 50 or 100 mg | 200 mg | AUC increased by ~7%; no adjustment |
| Moderate (Child-Pugh B) | 50 or 100 mg | 50 or 100 mg | 200 mg | AUC increased by ~50%; no formal adjustment |
| Severe (Child-Pugh C) | 50 mg | 50 mg | 100 mg | AUC increased by ~115%; use 50 mg strength only |
Special Populations
- Pediatric (<18 years): Safety and effectiveness have not been established. Not recommended.
- Geriatric (≥65 years): No clinically significant pharmacokinetic differences observed. Trial data in this age group are limited; cautious dose selection (start at 50 mg) is reasonable.
- Pregnancy: No adequate human data. Animal studies showed embryofetal mortality (rabbits) and decreased offspring body weight (rats) at doses associated with maternal toxicity. AbbVie maintains a pregnancy exposure registry: 1-833-277-0206.
- Lactation: A study in 12 healthy adult lactating females found ubrogepant excreted in low amounts in breast milk (estimated relative infant dose ~0.15%; milk-to-plasma ratio 0.23). Effects on the breastfed infant are not characterised — weigh maternal need against potential exposure.
Patients should be coached to take ubrogepant at the earliest sign of a definite migraine attack — not at every minor head sensation. If headache persists or returns after 2 hours, a single repeat dose is allowed within the same 24-hour window (subject to interaction caps). The 24-hour ceiling is 200 mg in healthy adults. The label explicitly states that the safety of treating more than 8 migraines in a 30-day period has not been established — patients exceeding this threshold should be evaluated for preventive therapy.
Although gepants do not appear to drive medication-overuse headache (MOH) to the degree seen with triptans or combination analgesics, the FDA labelling cap of 8 treatment days per month is a practical guide for ubrogepant. Patients exceeding this threshold — or using ≥10–15 days/month across all acute agents combined — should be considered for a preventive strategy.
Pharmacology
Mechanism of Action
Calcitonin gene-related peptide (CGRP) is a vasodilatory neuropeptide released from trigeminal sensory neurons during a migraine attack and a key mediator of migraine pain through pro-nociceptive transmission within the trigeminovascular system. Ubrogepant is a small-molecule, orally bioavailable, competitive antagonist at the human CGRP receptor (a heterodimer of the calcitonin receptor-like receptor and RAMP1). Preclinical characterisation by Moore and colleagues demonstrated high binding affinity for the human CGRP receptor (Ki ~0.07 nM) and high functional potency (IC50 ~0.08 nM in CGRP-stimulated cAMP assays), with selective antagonism over related calcitonin family receptors. By blocking endogenous CGRP from binding its receptor, ubrogepant interrupts trigeminovascular pain signalling without producing arterial vasoconstriction — the mechanistic feature that supports its use in patients with cardiovascular disease.
At doses up to twice the maximum recommended daily dose, ubrogepant does not prolong the QT interval to a clinically relevant extent.
ADME Profile
| Parameter | Value | Clinical Implication |
|---|---|---|
| Absorption | Tmax ~1.5 h; high-fat meal delays Tmax by 2 h and reduces Cmax 22% with no change in AUC; dose-proportional within recommended range | Rapid onset; food does not require dose timing changes — patients can take with or without food |
| Distribution | Apparent V/F ~350 L; plasma protein binding 87% in vitro | Wide tissue distribution; protein-binding interactions are not clinically significant |
| Metabolism | Primarily hepatic via CYP3A4; two glucuronide conjugate metabolites are major circulating species but ~6000× less potent at the CGRP receptor; substrate of P-gp and BCRP | CYP3A4 inhibitors and inducers dominate the interaction profile; transporter inhibitors add a secondary layer requiring dose adjustment |
| Elimination | t½ ~5–7 h; mean apparent oral clearance ~87 L/h; primarily biliary/fecal — 42% of dose recovered in feces and 6% in urine as unchanged drug | Renal route is minor — no dose adjustment for mild–moderate renal impairment; ESRD avoided due to absent data |
Drug interaction conclusions from clinical PK studies: No clinically significant pharmacokinetic interactions were observed when ubrogepant was co-administered with sumatriptan, oral contraceptives (norgestimate/ethinyl estradiol), acetaminophen, naproxen, esomeprazole, or the CGRP-targeted monoclonal antibodies erenumab and galcanezumab, or with atogepant.
Side Effects
Ubrogepant has a notably mild adverse-effect profile in the pivotal acute treatment trials (Studies 1 and 2; ACHIEVE I and ACHIEVE II), with most events being low-grade and transient. The most common adverse reactions occurring at ≥2% and at a frequency greater than placebo were nausea and somnolence. Compared with triptans, the absence of chest tightness, paraesthesia, and vasoconstrictive symptoms is notable.
| Adverse Effect | Incidence | Clinical Note |
|---|---|---|
| No adverse effect occurred at ≥10% incidence in placebo-controlled trials. Ubrogepant has a uniformly low-frequency tolerability profile. | ||
| Adverse Effect | 50 mg | 100 mg | Placebo | Clinical Note |
|---|---|---|---|---|
| Nausea | 2% | 4% | 2% | Usually mild; can be migraine-related rather than drug-related |
| Somnolence (incl. sedation, fatigue) | 2% | 3% | 1% | Counsel against driving until individual response is known after the first dose |
| Dry mouth | <1% | 2% | 1% | Symptomatic and self-limited |
| Adverse Effect | Estimated Frequency | Typical Onset | Required Action |
|---|---|---|---|
| Hypersensitivity reactions (anaphylaxis, dyspnoea, facial or throat oedema, rash, urticaria, pruritus) | Rare post-marketing | Minutes, hours, or days after administration | Discontinue permanently; emergency care if airway, dyspnoea, or anaphylaxis; do not re-challenge |
| Hypertension (new-onset or worsening of pre-existing) | Frequency not established labelled warning 5.2 | Variable; can be acute or insidious with repeated use | Monitor BP; consider discontinuation if alternative aetiology excluded or BP inadequately controlled |
| Raynaud’s phenomenon (new-onset or worsening of pre-existing) | Rare post-marketing; class effect of CGRP antagonists, labelled warning 5.3 | Median ~1.5 days after dosing in reported cases | Discontinue ubrogepant; evaluate if symptoms do not resolve; some reported cases included hospitalisation or disability |
| Reason for Discontinuation | Frequency | Context |
|---|---|---|
| Adverse event — any (1-year safety study) | 2.5% | Pooled 50 mg and 100 mg long-term safety population |
| Nausea | Most common | Leading cause of discontinuation in long-term use |
| Hypersensitivity reaction | Rare | Mandatory permanent discontinuation if confirmed |
| Raynaud’s phenomenon | Rare | Per labelled warning, discontinue if signs/symptoms develop |
Nausea and somnolence are also core migraine-associated symptoms — clinical attribution between drug and disease is often difficult. If a patient reports new nausea after dosing, assess whether it preceded or followed the headache, whether it improves alongside headache resolution, and whether prior attacks (untreated) were similarly nauseating. Genuine drug-induced nausea is mild, low-frequency (4% on 100 mg vs 2% on placebo), and rarely treatment-limiting.
Drug Interactions
Ubrogepant’s interaction profile is dominated by CYP3A4. The drug is also a substrate of P-glycoprotein (P-gp) and BCRP. Strong CYP3A4 inhibition is contraindicated; moderate inhibition mandates a 50 mg cap with no repeat within 24 h. Strong CYP3A4 induction is to be avoided as efficacy is markedly reduced; weak/moderate inducers permit use with a switch to the 100 mg strength. Patients should also be advised that grapefruit juice is a relevant moderate CYP3A4 inhibitor.
Before any new ubrogepant prescription, screen explicitly for: (1) “Are you taking any antifungal pills?” — captures azoles; (2) “Any HIV or hepatitis C medicines?” — captures protease inhibitors and cobicistat; (3) “Any antiseizure medicines?” — captures carbamazepine, phenytoin, phenobarbital; (4) “Any herbal supplements, especially St. John’s wort?”; (5) “Do you drink grapefruit juice?” — easily missed but a labelled moderate CYP3A4 inhibitor.
Monitoring
Ubrogepant requires minimal laboratory monitoring. The most important post-marketing additions to the label — hypertension and Raynaud’s phenomenon (both class-effect warnings) — make blood pressure surveillance and digital symptom screening clinically relevant additions to routine follow-up.
-
Blood pressure
Baseline, then 2–4 weeks after initiation; then periodically
Routine Monitor for new-onset or worsening hypertension. Consider discontinuation if BP is inadequately controlled and an alternative aetiology is excluded. -
Digital / extremity symptoms (Raynaud’s)
Every visit and on patient report
Trigger-based Ask about colour change, numbness, coolness, or pain in fingers/toes. Onset has been reported a median of ~1.5 days after dosing in post-marketing cases. Discontinue if symptoms develop. -
Migraine days / month
Every visit (e.g. 3-monthly)
Routine Track via headache diary or app. Rising frequency is the cue to consider preventive therapy rather than escalating acute use. -
Acute treatment days / month
Every visit
Routine Sum across all acute agents. Per FDA labelling, safety of treating >8 migraines/30 days has not been established — use this as an explicit threshold. -
Treatment response (2-h pain freedom, MBS freedom)
After 2–3 attacks treated
Routine Reasonable trial period before declaring failure. If 2/3 or 3/3 attacks fail, step from 50 to 100 mg or switch to another class. -
Renal function (CrCl)
Recheck if status changes
Trigger-based No routine monitoring in stable normal renal function. Reassess if CrCl drops below 30 mL/min — switch to 50 mg cap; avoid use if CrCl <15 mL/min. -
Hepatic function (LFTs)
On symptoms; consider baseline in known liver disease
Trigger-based Routine LFT monitoring is not required at acute treatment doses; published healthy-volunteer data have not shown clinically meaningful ALT elevation. -
Concomitant medication review
Every visit and at each new prescription
Routine Specifically screen for new strong/moderate CYP3A4 inhibitors and inducers, P-gp/BCRP inhibitors, and grapefruit juice intake.
The single most useful “monitoring” metric for ubrogepant is treatment days per month. The FDA-labelled threshold is >8 migraines treated in 30 days; beyond this, safety has not been established. A patient repeatedly hitting that ceiling — across any combination of acute agents — should be assessed for migraine prevention rather than offered more acute therapy. Combine BP monitoring at the 2–4-week post-initiation visit with the medication-days conversation: it captures both the new labelled hypertension warning and the medication-overuse risk in one visit.
Contraindications & Cautions
Absolute Contraindications
- Concomitant use of a strong CYP3A4 inhibitor — including ketoconazole, itraconazole, voriconazole, posaconazole, clarithromycin, ritonavir-boosted regimens, and cobicistat. Ketoconazole co-administration produces a ~9.7-fold increase in AUC.
- History of serious hypersensitivity to ubrogepant or any component of Ubrelvy — including prior anaphylaxis, dyspnoea, facial or throat oedema, severe cutaneous reaction, or angioedema temporally linked to a prior dose.
Relative Contraindications (Specialist Input Recommended)
- End-stage renal disease (CrCl <15 mL/min) or dialysis dependence — the FDA label advises avoiding use; no pharmacokinetic data are available in this population.
- Severe hepatic impairment (Child-Pugh C) — ubrogepant exposure is approximately 115% higher than in normal hepatic function; use only at the 50 mg dose with no second dose >50 mg in 24 h.
- Pregnancy — no adequate human data; animal studies showed embryofetal mortality (rabbits) and decreased offspring body weight (rats) at maternally-toxic exposures. Use only if alternatives are unsuitable; encourage enrolment in the AbbVie pregnancy registry (1-833-277-0206).
- Concurrent strong CYP3A4 inducer — efficacy is markedly reduced (rifampin reduces AUC by 80%); avoid use and select an alternative acute therapy.
- History of Raynaud’s phenomenon with ischaemic complications (e.g. prior digital ulcers, tissue loss) — case reports of debilitating Raynaud’s with CGRP antagonists indicate caution; specialist input is appropriate.
- Suspected medication-overuse headache — co-manage with a headache specialist; adding more acute therapy will not resolve the underlying pattern.
Use with Caution
- Severe renal impairment (CrCl 15–29 mL/min) — cap at 50 mg starting dose, 50 mg repeat, and 100 mg/24 h.
- Concomitant moderate CYP3A4 inhibitor — cap at 50 mg single dose; no repeat dose within 24 h. Includes verapamil, diltiazem, fluconazole, fluvoxamine, ciprofloxacin, cyclosporine, and grapefruit juice.
- Concomitant P-gp / BCRP only inhibitor (e.g. quinidine, carvedilol, eltrombopag, curcumin) — cap at 50 mg starting dose and 50 mg repeat dose.
- Pre-existing hypertension — monitor blood pressure at baseline and at the 2–4-week follow-up; adjust antihypertensive therapy or discontinue ubrogepant if blood pressure becomes uncontrolled.
- Pre-existing Raynaud’s phenomenon (uncomplicated) — counsel on symptom recognition; discontinue at first signs of worsening.
- Older adults (≥65 years) — limited trial data; cautious dose selection (start at 50 mg) is reasonable.
- Lactation — low transfer demonstrated (RID ~0.15%, milk-to-plasma ratio 0.23); risk-benefit decision; effects on the breastfed infant are uncharacterised.
- Operators of heavy machinery / professional drivers — confirm absence of somnolence after the first treated attack before unsupervised use during work.
Hypersensitivity (5.1): Reactions including anaphylaxis, dyspnoea, facial or throat oedema, rash, urticaria, and pruritus have been reported. Reactions can occur minutes, hours, or days after administration. Discontinue Ubrelvy permanently and institute appropriate therapy if a serious or severe reaction occurs.
Hypertension (5.2): New-onset hypertension or worsening of pre-existing hypertension may occur with Ubrelvy. Monitor blood pressure during therapy. If hypertension develops, evaluate for alternative aetiologies; consider discontinuation if blood pressure is inadequately controlled.
Raynaud’s phenomenon (5.3): Development or worsening of Raynaud’s phenomenon has been reported in the post-marketing setting with CGRP antagonists, including Ubrelvy. In reported cases with small-molecule CGRP antagonists, symptom onset occurred a median of 1.5 days following dosing; many cases involved serious outcomes including hospitalisation and disability. Discontinue Ubrelvy if signs or symptoms of Raynaud’s phenomenon develop, and arrange specialist evaluation if symptoms do not resolve.
There is no FDA boxed warning for ubrogepant. The above are class-wide labelled Warnings and Precautions that all prescribers must address with patients before initiation.
Patient Counselling
Purpose of Therapy
Ubrogepant is taken at the start of a migraine attack to stop it — it is not a daily preventive medicine. It works by blocking a chemical messenger called CGRP that is released during migraine and is responsible for much of the pain. It is a useful alternative for people who cannot take triptans (for example, because of heart or circulation problems), or for whom triptans have not worked or have been poorly tolerated. The medicine has no narrowing effect on blood vessels, which is why it is considered safer in cardiovascular disease.
How to Take
Swallow one tablet whole at the first definite sign of a migraine — not at every minor headache. The dose can be taken with or without food. If the headache is still present or has come back after at least 2 hours, a second tablet may be taken (subject to any cap your prescriber has set). Do not exceed 200 mg in any 24-hour period. The label states that the safety of treating more than 8 migraines in any 30-day period has not been established — keep a simple diary of how many days each month any acute migraine medicine is used and share this at every follow-up visit.
Sources
- U.S. Food and Drug Administration. UBRELVY (ubrogepant) tablets — full Prescribing Information. AbbVie. Most recent revision available at: accessdata.fda.gov Primary regulatory document — source of dosing, contraindications, drug interactions, adverse reaction incidence, and the Hypertension and Raynaud’s phenomenon warnings (sections 5.2 and 5.3).
- U.S. Food and Drug Administration. NDA 211765 Approval Letter — UBRELVY (ubrogepant). 23 December 2019. accessdata.fda.gov Documents the original FDA approval pathway and labelled indication for acute migraine in adults; confirms US-only approval status.
- DailyMed. UBRELVY (ubrogepant) tablet — current label. National Library of Medicine. dailymed.nlm.nih.gov Public-facing repository of the most current FDA-approved label, including the post-marketing class-wide additions for hypertension and Raynaud’s phenomenon.
- Dodick DW, Lipton RB, Ailani J, et al. Ubrogepant for the Treatment of Migraine. N Engl J Med. 2019;381(23):2230–2241. doi: 10.1056/NEJMoa1813049 Pivotal phase 3 ACHIEVE I trial establishing efficacy of 50 mg and 100 mg doses on 2-hour pain freedom and most bothersome symptom freedom.
- Lipton RB, Dodick DW, Ailani J, et al. Effect of Ubrogepant vs Placebo on Pain and the Most Bothersome Associated Symptom in the Acute Treatment of Migraine: The ACHIEVE II Randomized Clinical Trial. JAMA. 2019;322(19):1887–1898. doi: 10.1001/jama.2019.16711 Confirmatory phase 3 trial supporting efficacy of 50 mg ubrogepant; informs the lower-strength dosing strategy used in many patients.
- Ailani J, Lipton RB, Hutchinson S, et al. Long-Term Safety Evaluation of Ubrogepant for the Acute Treatment of Migraine: Phase 3, Randomized, 52-Week Extension Trial. Headache. 2020;60(1):141–152. doi: 10.1111/head.13682 52-week open-label extension informing the 2.5% discontinuation rate and long-term tolerability profile referenced in this monograph.
- Dodick DW, Goadsby PJ, Schwedt TJ, et al. Ubrogepant for the treatment of migraine attacks during the prodrome: a phase 3, multicentre, randomised, double-blind, placebo-controlled, crossover trial in the USA. Lancet. 2023;402(10419):2307–2316. doi: 10.1016/S0140-6736(23)01683-5 PRODROME trial demonstrating efficacy of 100 mg ubrogepant taken during prodromal symptoms in preventing development of moderate-to-severe headache; underpins the off-label prodromal-dosing discussion.
- Ailani J, Burch RC, Robbins MS; Board of Directors of the American Headache Society. The American Headache Society Consensus Statement: Update on integrating new migraine treatments into clinical practice. Headache. 2021;61(7):1021–1039. doi: 10.1111/head.14153 AHS consensus statement positioning gepants (including ubrogepant) for acute migraine treatment, including in patients with cardiovascular contraindications to triptans.
- Charles AC, Digre KB, Goadsby PJ, Robbins MS, Hershey A; American Headache Society. Calcitonin gene-related peptide-targeting therapies are a first-line option for the prevention of migraine: An American Headache Society position statement update. Headache. 2024;64(4):333–341. doi: 10.1111/head.14692 2024 AHS position update on CGRP-targeting therapies as first-line prevention; relevant for combined preventive-plus-acute strategies in patients on anti-CGRP mAbs who use ubrogepant for breakthrough attacks.
- National Institute for Health and Care Excellence (NICE). Headaches in over 12s: diagnosis and management. Clinical Guideline CG150. nice.org.uk/guidance/cg150 UK reference for stepwise migraine management against which gepant positioning is benchmarked, with the caveat that ubrogepant is not currently EMA-approved.
- Edvinsson L, Haanes KA, Warfvinge K, Krause DN. CGRP as the target of new migraine therapies — successful translation from bench to clinic. Nat Rev Neurol. 2018;14(6):338–350. doi: 10.1038/s41582-018-0003-1 Authoritative review of CGRP biology in migraine; provides the mechanistic framework for gepants and anti-CGRP monoclonal antibodies.
- Moore E, Fraley ME, Bell IM, et al. Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene-Related Peptide Receptor. J Pharmacol Exp Ther. 2020;373(1):160–166. doi: 10.1124/jpet.119.261065 Preclinical characterisation of ubrogepant binding affinity (Ki ~0.07 nM) and selectivity at the human CGRP receptor; basis for the mechanism statements in this monograph.
- Jakate A, Boinpally R, Butler M, Ankrom W, Dockendorf MF, Periclou A. Effects of CYP3A4 and P-glycoprotein inhibition or induction on the pharmacokinetics of ubrogepant in healthy adults: Two phase 1, open-label, fixed-sequence, single-center, crossover trials. Cephalalgia Reports. 2021;4. doi: 10.1177/25158163211037344 DDI study quantifying ubrogepant exposure changes with ketoconazole (~9.7-fold AUC), verapamil (~3.5-fold AUC), and rifampin (80% reduction); supports contraindication and dose-adjustment rules.
- Jakate A, Boinpally R, Butler M, et al. Pharmacokinetics and safety of ubrogepant when coadministered with calcitonin gene-related peptide-targeted monoclonal antibody migraine preventives in participants with migraine: A randomized phase 1b drug-drug interaction study. Headache. 2021;61(4):642–652. doi: 10.1111/head.14095 Phase 1b DDI study showing no clinically significant pharmacokinetic interaction between ubrogepant and erenumab or galcanezumab; supports combined acute + preventive strategy.
- Ankrom W, Bondiskey P, Li CC, et al. Ubrogepant Is Not Associated With Clinically Meaningful Elevations of Alanine Aminotransferase in Healthy Adult Males. Clin Transl Sci. 2020;13(3):462–472. doi: 10.1111/cts.12728 Healthy-volunteer hepatic safety study supporting the absence of routine LFT monitoring at therapeutic doses.
- Scott LJ. Ubrogepant: First Approval. Drugs. 2020;80(3):323–328. doi: 10.1007/s40265-020-01264-5 Concise overview of ubrogepant’s development, mechanism, pharmacokinetics, and the December 2019 FDA approval as the first oral gepant for acute migraine.