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Ubrogepant

Class: Calcitonin Gene-related Peptide (CGRP) Antagonists
Chemical Name: (3S)-N-[(3S,5S,6R)-6-methyl-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)piperidin-3-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6'-5,7-dihydrocyclopenta[b]pyridine]-3'-carboxamide
Molecular Formula: C29H26F3N5O3
CAS Number: 1374248-77-7
Brands: Ubrelvy

Medically reviewed by Drugs.com. Last updated on Jan 13, 2020.

Introduction

Ubrogepant is a calcitonin gene-related peptide (CGRP) antagonist.

Uses for Ubrogepant

Ubrogepant has the following uses:

Ubrogepant is a calcitonin gene-related peptide receptor antagonist indicated for the acute treatment of migraine with or without aura in adults.1

Ubrogepant has the following limitations of use:

Ubrogepant is not indicated for the preventive treatment of migraine.1

Ubrogepant Dosage and Administration

General

Ubrogepant is available in the following dosage form(s) and strength(s):

Tablets: 50 mg and 100 mg.1

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Adults

Dosage and Administration
  • The recommended dose is 50 mg or 100 mg taken orally, as needed.1

  • If needed, a second dose may be administered at least 2 hours after the initial dose.1

  • The maximum dose in a 24-hour period is 200 mg.1

  • The safety of treating more than 8 migraines in a 30-day period has not been established.1

  • Severe Hepatic or Severe Renal Impairment: Recommended dose is 50 mg; if needed, a second 50 mg dose may be taken at least 2 hours after the initial dose.1

Cautions for Ubrogepant

Contraindications

• Concomitant use with strong CYP3A4 inhibitors.1

Warnings/Precautions

Specific Populations

Pregnancy

Risk Summary: There are no adequate data on the developmental risk associated with the use of ubrogepant in pregnant women. In animal studies, adverse effects on embryofetal development were observed following administration of ubrogepant during pregnancy (increased embryofetal mortality in rabbits) or during pregnancy and lactation (decreased body weight in offspring in rats) at doses greater than those used clinically and which were associated with maternal toxicity.1

In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2–4% and 15–20%, respectively. The estimated rate of major birth defects (2.2–2.9%) and miscarriage (17%) among deliveries to women with migraine are similar to rates reported in women without migraine.1

Clinical Considerations: Published data have suggested that women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy.1

Animal Data: Oral administration of ubrogepant (0, 1.5, 5, 25, 125 mg/kg/day) to pregnant rats during the period of organogenesis resulted in no adverse effects on embryofetal development. Plasma exposure (AUC) at the highest dose tested is approximately 45 times that in humans at the maximum recommended human dose (MRHD) of 200 mg/day.1

In pregnant rabbits, ubrogepant (0, 15, 45, 75, or 250 mg/kg/day) was administered orally throughout organogenesis in two separate studies. In both studies, the highest dose tested (250 mg/kg/day) was associated with maternal toxicity. In the first study, ubrogepant produced abortion and increased embryofetal mortality in surviving litters at the high dose (250 mg/kg/day). In the second study, excessive maternal toxicity at the high dose (250 mg/kg/day) resulted in early termination and lack of fetal data for that dose group. Plasma exposure (AUC) at the highest no-effect dose (75 mg/kg/day) for adverse effects on embryofetal development in rabbit is approximately 8 times that in humans at the MRHD.1

Oral administration of ubrogepant (0, 25, 60, or 160 mg/kg/day) to rats throughout gestation and lactation resulted in decreased body weight in offspring at birth and during the lactation period at the mid and high doses, which were associated with maternal toxicity. Plasma exposure (AUC) at the no-effect dose for adverse effects on pre- and postnatal development in rats (25 mg/kg/day) is approximately 15 times that in humans at the MRHD.1

Lactation

There are no data on the presence of ubrogepant in human milk, the effects of ubrogepant on the breastfed infant, or the effects of ubrogepant on milk production. In lactating rats, oral dosing with ubrogepant resulted in levels of ubrogepant in milk comparable to peak plasma concentrations. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for ubrogepant and any potential adverse effects on the breastfed infant from ubrogepant or from the underlying maternal condition.1

Pediatric Use

Safety and effectiveness in pediatric patients have not been established. 1

Geriatric Use

In pharmacokinetic studies, no clinically significant pharmacokinetic differences were observed between elderly and younger subjects. Clinical studies of ubrogepant did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently from younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range.1

Hepatic Impairment

In patients with pre-existing mild (Child-Pugh Class A), moderate (Child-Pugh Class B), or severe hepatic impairment (Child-Pugh Class C), ubrogepant exposure was increased by 7%, 50%, and 115%, respectively. No dose adjustment is recommended for patients with mild or moderate hepatic impairment. Dose adjustment for ubrogepant is recommended for patients with severe hepatic impairment.1

Renal Impairment

The renal route of elimination plays a minor role in the clearance of ubrogepant. No dose adjustment is recommended for patients with mild or moderate renal impairment. Dose adjustment is recommended for patients with severe renal impairment (Clcr 15-29 mL/min) . Avoid use of ubrogepant in patients with end-stage renal disease (ESRD) (Clcr <15 mL/min). 1

Common Adverse Effects

The most common adverse reactions (at least 2% and greater than placebo) were nausea and somnolence.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

  • Strong CYP3A4 inducers: Should be avoided as concomitant use will result in reduction of ubrogepant exposure.1

  • Moderate or weak CYP3A4 inhibitors and inducers: Consult manufacturer's labeling for dosage recommendations.1

  • BCRP and/or P-gp only inhibitors: Consult manufacturer's labeling for dosage recommendations.1

Actions

Mechanism Of Action

Ubrogepant is a calcitonin gene-related peptide receptor antagonist.1

Advice to Patients

Advise the patient to read the FDA-approved patient labeling.1

Drug Interactions

Inform patients that ubrogepant may interact with certain other drugs; therefore, advise patients to report to their healthcare provider the use of any other prescription medications, over-the-counter medications, or herbal products. Advise patients to inform their healthcare provider of grapefruit juice intake because a dosage modification is recommended with co-administration. 1

Pregnancy

Advise patients to notify their healthcare provider if they become pregnant during treatment or plan to become pregnant. 1

Lactation

Inform patients to notify their healthcare provider if they are breastfeeding or plan to breastfeed.1

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Ubrogepant

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablet

50 mg

Ubrelvy

Allergan

100 mg

Ubrelvy

Allergan

AHFS Drug Information. © Copyright 2021, Selected Revisions January 13, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Allergan, Inc.. UBRELVY (ubrogepant) ORAL prescribing information. 2020 Jan. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fd9f9458-fd96-4688-be3f-f77b3d1af6ab

Frequently asked questions