Ubrogepant
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From MedlinePlus, U.S. National Library of Medicine
Calcitonin Gene-related Peptide Receptor Antagonist
Dosing in kidney impairment
Renal Impairment The renal route of elimination plays a minor role in the clearance of ubrogepant [see Clinical Pharmacology] . 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) [see Dosage and Administration and Clinical Pharmacology] .
Avoid use of UBRELVY in patients with end-stage renal disease (ESRD) (CLcr <15 mL/min).
| Dosage Modifications | Initial Dose | Second Dosea (if needed) |
| Concomitant Drug [see Drug Interactions (7)] | ||
| Moderate CYP3A4 Inhibitors (7.1) | 50 mg | Avoid within 24 hours |
| Weak CYP3A4 Inhibitors (7.1) | 50 mg | 50 mg |
| Strong CYP3A4 Inducers (7.2) | Avoid concomitant use | |
| Weak & Moderate CYP3A4 Inducers (7.2) | 100 mg | 100 mg |
| BCRP and/or P-gp only Inhibitors (7.3) | 50 mg | 50 mg |
| Specific Populations [see Use in Specific Populations (8)] | ||
| Severe Hepatic Impairment (Child-Pugh Class C) (8.6) | 50 mg | 50 mg |
| Severe Renal Impairment (CLcr 15-29 mL/min) (8.7) | 50 mg | 50 mg |
| End-Stage Renal Disease (CLcr <15 mL/min) (8.7) | Avoid use | |
| a Second dose may be taken at least 2 hours after the initial dose | ||
Dosing in liver impairment
Dosage Modification s Dosing modifications for concomitant use of specific drugs and for patients with hepatic or renal impairment are provided in Table 1. [See table below.]
| Dosage Modifications | Initial Dose | Second Dosea (if needed) |
| Concomitant Drug [see Drug Interactions (7)] | ||
| Moderate CYP3A4 Inhibitors (7.1) | 50 mg | Avoid within 24 hours |
| Weak CYP3A4 Inhibitors (7.1) | 50 mg | 50 mg |
| Strong CYP3A4 Inducers (7.2) | Avoid concomitant use | |
| Weak & Moderate CYP3A4 Inducers (7.2) | 100 mg | 100 mg |
| BCRP and/or P-gp only Inhibitors (7.3) | 50 mg | 50 mg |
| Specific Populations [see Use in Specific Populations (8)] | ||
| Severe Hepatic Impairment (Child-Pugh Class C) (8.6) | 50 mg | 50 mg |
| Severe Renal Impairment (CLcr 15-29 mL/min) (8.7) | 50 mg | 50 mg |
| End-Stage Renal Disease (CLcr <15 mL/min) (8.7) | Avoid use | |
| a Second dose may be taken at least 2 hours after the initial dose | ||
Drug interactions
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- Ubrogepant
Label text (5 paragraphs)
Strong CYP3A4 Inducers: Should be avoided as concomitant use will result in reduction of ubrogepant exposure. ( 2.2 , 7.2 ) For additional dose modifications for moderate or weak CYP3A4 inhibitors and inducers or BCRP and/or P-gp only inhibitors, refer to section 2.2 . ( 7.1 , 7.2 , 7.3 )
7.1 CYP3A4 I nhibitors Co-administration of UBRELVY with ketoconazole, a strong CYP3A4 inhibitor, resulted in a significant increase in exposure of ubrogepant [see Clinical Pharmacology ( 12.3 ) ] . UBRELVY should not be used with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) [see Contraindication s ( 4 )] . Co-administration of UBRELVY with verapamil, a moderate CYP3A4 inhibitor, resulted in an increase in ubrogepant exposure [see Clinical Pharmacology ( 12.3 ) ] .
Dose adjustment is recommended with concomitant use of UBRELVY and moderate CYP3A4 inhibitors (e.g., cyclosporine, ciprofloxacin, fluconazole, fluvoxamine, grapefruit juice) [see Dosage and Administration ( 2.2 )] . No dedicated drug interaction study was conducted with ubrogepant and weak CYP3A4 inhibitors. Dose adjustment is recommended with concomitant use of UBRELVY with weak CYP3A4 inhibitors [see Dosage and Administration ( 2.2 )] .
7.2 CYP3A4 I nducers Co-administration of UBRELVY with rifampin, a strong CYP3A4 inducer, resulted in a significant reduction in ubrogepant exposure [ s ee Clinical Pharmacology ( 12.3 ) ] . In patients taking strong CYP3A4 inducers (e.g., phenytoin, barbiturates, rifampin, St. John’s Wort), loss of ubrogepant efficacy is expected, and concomitant use should be avoided. Co-administration of UBRELVY with moderate or weak CYP3A4 inducers was not evaluated in a clinical study. Dose adjustment is recommended with concomitant use of UBRELVY and moderate or weak CYP3A4 inducers [see Dosage and Administration ( 2.2 )] .
7 .3 BCRP and / or P-gp Only Inhibitors Ubrogepant is a substrate of BCRP and P-gp efflux transporters. Use of BCRP and/or P-gp only inhibitors (e.g., quinidine, carvedilol, eltrombopag, curcumin) may increase the exposure of ubrogepant [ s ee Clinical Pharmacology ( 12.3 ) ] . Clinical drug interaction studies with inhibitors of these transporters were not conducted. Dose adjustment is recommended with BCRP and/or P-gp only inhibitors [see Dosage and Administration ( 2.2 ) ] .
Contraindications
4 CONTRAINDICATIONS UBRELVY is contraindicated: With concomitant use of strong CYP3A4 inhibitors [see Drug Interactions ( 7.1 )] In patients with a history of serious hypersensitivity to ubrogepant or any component of UBRELVY. Reactions have included anaphylaxis, dyspnea, and facial or throat edema [see Warnings and Precautions ( 5.1 )] Concomitant use with strong CYP3A4 inhibitors. ( 4 ) History of serious hypersensitivity to ubrogepant or any component of UBRELVY. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
ELikelihood score E: Unlikely cause of clinically apparent acute liver injury.
Ubrogepant is an orally available, small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Ubrogepant is approved for treatment of acute migraine attacks. In clinical trials, urbrogepant was generally well tolerated with only rare instances of transient serum aminotransferase elevations during therapy and with no reported instances of clinically apparent liver injury.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors outcomes in women who become pregnant while taking UBRELVY. Patients should be encouraged to enroll by calling 1-833-277-0206 or visiting http://empresspregnancyregistry.com . Risk Summary There are no adequate data on the developmental risk associated with the use of UBRELVY 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 ( see Data ) . 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. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Published data have suggested that women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy. Data 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. 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. 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,…
Breastfeeding (LactMed)
No information is available on the clinical use of ubrogepant during breastfeeding. However, amounts in breastmilk are low and virtually absent from milk 16 hours after a dose. Ubrogepant is not expected to cause any adverse effects in breastfed infants. If ubrogepant is required by the mother of an older infant, it is not a reason to discontinue breastfeeding, but until more data become available, an alternate drug may be preferred while nursing a newborn or preterm infant. Some experts recommend withholding breastfeeding for 8 to 12 hours after a dose.
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Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
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