Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H26F3N5O3.3H2O |
Molecular Weight | 603.5895 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.O.C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC5=NC=CC=C45)C(=O)N1CC(F)(F)F)C6=CC=CC=C6
InChI
InChIKey=ZFHQRKNHABBCOO-MONFIQOXSA-N
InChI=1S/C29H26F3N5O3.3H2O/c1-16-20(17-6-3-2-4-7-17)11-22(26(39)37(16)15-29(30,31)32)35-25(38)19-10-18-12-28(13-23(18)34-14-19)21-8-5-9-33-24(21)36-27(28)40;;;/h2-10,14,16,20,22H,11-13,15H2,1H3,(H,35,38)(H,33,36,40);3*1H2/t16-,20-,22+,28+;;;/m1.../s1
Ubrogepant, a small molecule drug, is being developed by Merck & Co for the treatment of migraine. The calcitonin gene-related peptide receptor (CGRP) antagonist is administered orally as a film coated tablet. Ubrogepant is a competitive antagonist with high affinity, potency, and selectivity for the human CGRP receptor. In the four clinical studies (ACHIEVE I, ACHIEVE II, UBR-MD-04 and 3110-105-002) ubrogepant demonstrated efficacy, safety and tolerability in the acute treatment of migraine among a broad patient population, including those who had an insufficient response to a triptan or those patients in whom triptans were contraindicated, as well as in patients who had moderate to severe CV risk profile.
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
281.97 nM |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: |
|
274.25 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1029.75 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1306.54 nM × h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: |
|
1249.39 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5127.06 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.54 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: |
|
4.41 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.06 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31628854/ |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
UBROGEPANT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
25 mg multiple, oral |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Other AEs: Upper respiratory tract infection, Nausea... Other AEs: Upper respiratory tract infection (1.3%) Sources: Nausea (2.9%) Nasopharyngitis (1%) Dizziness (2.3%) |
25 mg 1 times / day single, oral Dose: 25 mg, 1 times / day Route: oral Route: single Dose: 25 mg, 1 times / day Sources: |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Other AEs: Nausea, Dizziness... |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, 18-75 years n = 485 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 485 Sources: |
Disc. AE: Nausea... Other AEs: Nausea, Somnolence... AEs leading to discontinuation/dose reduction: Nausea Other AEs:Nausea (4%) Sources: Somnolence (3%) Dry mouth (2%) |
50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Other AEs: Upper respiratory tract infection, Nausea... Other AEs: Upper respiratory tract infection (2.7%) Sources: Nausea (2.5%) Nasopharyngitis (2.3%) Dizziness (2%) |
50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Other AEs: ALT increased, AST increased... Other AEs: ALT increased (0.4%) Sources: AST increased (0.2%) ALP increased (0.2%) |
50 mg multiple, oral Recommended Dose: 50 mg Route: oral Route: multiple Dose: 50 mg Sources: |
unhealthy, 18-75 years n = 954 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 954 Sources: |
Other AEs: Nausea, Somnolence... Other AEs: Nausea (2%) Sources: Somnolence (2%) Dry mouth (< 1%) |
50 mg 1 times / day single, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: single Dose: 50 mg, 1 times / day Sources: |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Other AEs: Nausea, Dizziness... |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Disc. AE: Abnormal ECG, Extrasystoles... Other AEs: Nasopharyngitis, Upper respiratory tract infection... AEs leading to discontinuation/dose reduction: Abnormal ECG (0.2%) Other AEs:Extrasystoles (0.2%) Nausea (0.2%) Palpitations (0.2%) Pruritus (0.2%) ALT increased (0.2%) AST increased (0.2%) Nasopharyngitis (grade 1-2, 11.5%) Sources: Upper respiratory tract infection (grade 1-2, 10.8%) Sinusitis (grade 1-2, 6.4%) Urinary tract infection (grade 1-2, 6.4%) Influenza (grade 1-2, 6.1%) Nausea (grade 1-2, 4.6%) Bronchitis (grade 1-2, 4.4%) Blood creatine phosphokinase increased (grade 1-2, 3.9%) ALT increased (grade 1-2, 3.7%) AST increased (grade 1-2, 3.4%) Back pain (grade 1-2, 3.4%) Nephrolithiasis (grade 1-2, 3.2%) Dizziness (grade 1-2, 2.9%) Anxiety (grade 1-2, 2.7%) Cough (grade 1-2, 2.7%) Diarrhea (grade 1-2, 2.7%) Arthralgia (grade 1-2, 2.4%) Gastroenteritis viral (grade 1-2, 2.4%) Muscle strain (grade 1-2, 2.4%) Depression (grade 1-2, 1.2%) Migraine (grade 1-2, 1%) Abdominal pain (grade 1-2, 0.5%) |
50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Disc. AE: Nausea, Thrombocytopenia... Other AEs: Nasopharyngitis, Upper respiratory tract infection... AEs leading to discontinuation/dose reduction: Nausea (0.2%) Other AEs:Thrombocytopenia (0.2%) Urticaria (0.2%) Vomiting (0.2%) Nasopharyngitis (grade 1-2, 8.2%) Sources: Upper respiratory tract infection (grade 1-2, 11.6%) Sinusitis (grade 1-2, 6.9%) Urinary tract infection (grade 1-2, 5.4%) Influenza (grade 1-2, 4.2%) Nausea (grade 1-2, 4.7%) Bronchitis (grade 1-2, 3.2%) Blood creatine phosphokinase increased (grade 1-2, 2.5%) ALT increased (grade 1-2, 2.2%) AST increased (grade 1-2, 1.7%) Back pain (grade 1-2, 3.5%) Nephrolithiasis (grade 1-2, 1%) Dizziness (grade 1-2, 1.2%) Anxiety (grade 1-2, 1.5%) Cough (grade 1-2, 2%) Diarrhea (grade 1-2, 2.5%) Arthralgia (grade 1-2, 2.7%) Gastroenteritis viral (grade 1-2, 1.7%) Muscle strain (grade 1-2, 0.5%) Depression (grade 1-2, 3.2%) Migraine (grade 1-2, 1.5%) Abdominal pain (grade 1-2, 1%) Epididymitis (grade 1-2, 3.2%) Testicular pain (grade 1-2, 3.2%) |
400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Other AEs: Nausea, Diarrhea... Other AEs: Nausea (1.3%) Sources: Diarrhea (2.6%) Abdominal pain (1.3%) Vomiting (1.3%) Medical device site reaction (1.3%) Vessel puncture site pain (2.6%) Electrocardiogram QT prolonged (1.3%) AST increased (1.3%) Headache (2.6%) Insomnia (1.3%) Cough (1.3%) Oropharyngeal pain (1.3%) |
400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Other AEs: Headache, Nausea... Other AEs: Headache (grade 1-2, 16.7%) Sources: Nausea (grade 1-2, 16.7%) Abdominal discomfort (grade 1-2, 16.7%) Abdominal pain upper (grade 1-2, 16.7%) Application site irritation (grade 1-2, 16.7%) Herpes simplex (grade 1-2, 16.7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Nasopharyngitis | 1% | 25 mg multiple, oral |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Upper respiratory tract infection | 1.3% | 25 mg multiple, oral |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Dizziness | 2.3% | 25 mg multiple, oral |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Nausea | 2.9% | 25 mg multiple, oral |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Dizziness | 2.1% | 25 mg 1 times / day single, oral Dose: 25 mg, 1 times / day Route: oral Route: single Dose: 25 mg, 1 times / day Sources: |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Nausea | 2.5% | 25 mg 1 times / day single, oral Dose: 25 mg, 1 times / day Route: oral Route: single Dose: 25 mg, 1 times / day Sources: |
unhealthy, 18-71 years n = 478 Health Status: unhealthy Condition: migraine Age Group: 18-71 years Sex: M+F Population Size: 478 Sources: |
Dry mouth | 2% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, 18-75 years n = 485 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 485 Sources: |
Somnolence | 3% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, 18-75 years n = 485 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 485 Sources: |
Nausea | 4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, 18-75 years n = 485 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 485 Sources: |
Nausea | Disc. AE | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, 18-75 years n = 485 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 485 Sources: |
Dizziness | 2% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Nasopharyngitis | 2.3% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Nausea | 2.5% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Upper respiratory tract infection | 2.7% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
ALP increased | 0.2% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
AST increased | 0.2% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
ALT increased | 0.4% | 50 mg multiple, oral Recommended |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Nausea | 2% | 50 mg multiple, oral Recommended Dose: 50 mg Route: oral Route: multiple Dose: 50 mg Sources: |
unhealthy, 18-75 years n = 954 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 954 Sources: |
Somnolence | 2% | 50 mg multiple, oral Recommended Dose: 50 mg Route: oral Route: multiple Dose: 50 mg Sources: |
unhealthy, 18-75 years n = 954 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 954 Sources: |
Dry mouth | < 1% | 50 mg multiple, oral Recommended Dose: 50 mg Route: oral Route: multiple Dose: 50 mg Sources: |
unhealthy, 18-75 years n = 954 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 954 Sources: |
Dizziness | 1.4% | 50 mg 1 times / day single, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: single Dose: 50 mg, 1 times / day Sources: |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
Nausea | 2% | 50 mg 1 times / day single, oral Recommended Dose: 50 mg, 1 times / day Route: oral Route: single Dose: 50 mg, 1 times / day Sources: |
unhealthy, 18-75 years n = 488 Health Status: unhealthy Condition: migraine Age Group: 18-75 years Sex: M+F Population Size: 488 Sources: |
ALT increased | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
AST increased | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Abnormal ECG | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Extrasystoles | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Nausea | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Palpitations | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Pruritus | 0.2% Disc. AE |
100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Abdominal pain | grade 1-2, 0.5% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Migraine | grade 1-2, 1% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Depression | grade 1-2, 1.2% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Upper respiratory tract infection | grade 1-2, 10.8% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Nasopharyngitis | grade 1-2, 11.5% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Arthralgia | grade 1-2, 2.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Gastroenteritis viral | grade 1-2, 2.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Muscle strain | grade 1-2, 2.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Anxiety | grade 1-2, 2.7% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Cough | grade 1-2, 2.7% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Diarrhea | grade 1-2, 2.7% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Dizziness | grade 1-2, 2.9% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Nephrolithiasis | grade 1-2, 3.2% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
AST increased | grade 1-2, 3.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Back pain | grade 1-2, 3.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
ALT increased | grade 1-2, 3.7% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Blood creatine phosphokinase increased | grade 1-2, 3.9% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Bronchitis | grade 1-2, 4.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Nausea | grade 1-2, 4.6% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Influenza | grade 1-2, 6.1% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Sinusitis | grade 1-2, 6.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Urinary tract infection | grade 1-2, 6.4% | 100 mg multiple, oral Recommended Dose: 100 mg Route: oral Route: multiple Dose: 100 mg Sources: |
unhealthy, average 42 years n = 409 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 409 Sources: |
Nausea | 0.2% Disc. AE |
50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Thrombocytopenia | 0.2% Disc. AE |
50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Urticaria | 0.2% Disc. AE |
50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Vomiting | 0.2% Disc. AE |
50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Muscle strain | grade 1-2, 0.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Abdominal pain | grade 1-2, 1% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Nephrolithiasis | grade 1-2, 1% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Dizziness | grade 1-2, 1.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Anxiety | grade 1-2, 1.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Migraine | grade 1-2, 1.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
AST increased | grade 1-2, 1.7% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Gastroenteritis viral | grade 1-2, 1.7% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Upper respiratory tract infection | grade 1-2, 11.6% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Cough | grade 1-2, 2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
ALT increased | grade 1-2, 2.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Blood creatine phosphokinase increased | grade 1-2, 2.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Diarrhea | grade 1-2, 2.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Arthralgia | grade 1-2, 2.7% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Bronchitis | grade 1-2, 3.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Depression | grade 1-2, 3.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Epididymitis | grade 1-2, 3.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Testicular pain | grade 1-2, 3.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Back pain | grade 1-2, 3.5% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Influenza | grade 1-2, 4.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Nausea | grade 1-2, 4.7% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Urinary tract infection | grade 1-2, 5.4% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Sinusitis | grade 1-2, 6.9% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
Nasopharyngitis | grade 1-2, 8.2% | 50 mg multiple, oral Recommended |
unhealthy, average 42 years n = 404 Health Status: unhealthy Condition: migraine Age Group: average 42 years Sex: M+F Population Size: 404 Sources: |
AST increased | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Abdominal pain | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Cough | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Electrocardiogram QT prolonged | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Insomnia | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Medical device site reaction | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Nausea | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Oropharyngeal pain | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Vomiting | 1.3% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Diarrhea | 2.6% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Headache | 2.6% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Vessel puncture site pain | 2.6% | 400 mg 1 times / day single, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 29.2 years n = 76 Health Status: healthy Age Group: mean age 29.2 years Sex: M+F Population Size: 76 Sources: |
Abdominal discomfort | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Abdominal pain upper | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Application site irritation | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Headache | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Herpes simplex | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Nausea | grade 1-2, 16.7% | 400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
healthy, range 21–51 years n = 6 Health Status: healthy Age Group: range 21–51 years Sex: M Population Size: 6 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | yes (co-administration study) Comment: Co-administration of ubrogepant with ketoconazole, a strong CYP3A4 inhibitor, resulted in a 9.7 fold increase in ubrogepant AUC0-inf and a 5.3-fold increase in ubrogepant Cmax Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=7 Page: 7.0 |
|||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
yes | |||
yes | likely (co-administration study) Comment: Drug interaction with verapamil (a combined P-gp inhibitor and moderate CYP3A4 inhibitor) resulted in a 3.5-fold increase in exposure. This increase in exposure can be due to the combined P-gp/CYP3A4 inhibition and the relative contribution of P-gp inhibition needs to be segregated to provide dose adjustment recommendation with P-gp only inhibitors Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000ClinPharmR.pdf#page=9 Page: 9.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000PharmR.pdf#page=18 Page: 18.0 |
PubMed
Title | Date | PubMed |
---|---|---|
A phase IIb randomized, double-blind, placebo-controlled trial of ubrogepant for the acute treatment of migraine. | 2016 Aug |
|
CGRP as the target of new migraine therapies - successful translation from bench to clinic. | 2018 Jun |
|
Therapeutic novelties in migraine: new drugs, new hope? | 2019 Apr 17 |
|
Advances in orally administered pharmacotherapy for the treatment of migraine. | 2019 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27269043
Migraine: ubrogepant 1 mg, 10 mg, 25 mg, 50 mg, 100 mg. Ubrogepant 100 mg was significantly superior to placebo for two-hour pain freedom but not for two-hour headache response.
Route of Administration:
Oral
The binding affinity for native (Ki=0.067 nM) and cloned human (Ki=0.070 nM) and rhesus (Ki=0.079 nM) receptors was similar for ubrogepant, with relatively lower affinities for CGRP receptors of other species (ranging from Ki=9.6 to 47 nM). Ubrogepant potently blocked human α-CGRP–stimulated cAMP response (IC50 of 0.08) and exhibited highly selective antagonist activity in relation to the CGRP receptor compared with other members of the human calcitonin receptor family.
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ACTIVE MOIETY
SUBSTANCE RECORD