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Details

Stereochemistry ABSOLUTE
Molecular Formula C29H23F6N5O3
Molecular Weight 603.515
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ATOGEPANT

SMILES

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=C(F)C(F)=CC=C6F

InChI

InChIKey=QIVUCLWGARAQIO-OLIXTKCUSA-N
InChI=1S/C29H23F6N5O3/c1-13-16(22-18(30)4-5-19(31)23(22)32)8-20(26(42)40(13)12-29(33,34)35)38-25(41)15-7-14-9-28(10-21(14)37-11-15)17-3-2-6-36-24(17)39-27(28)43/h2-7,11,13,16,20H,8-10,12H2,1H3,(H,38,41)(H,36,39,43)/t13-,16-,20+,28+/m1/s1

HIDE SMILES / InChI

Molecular Formula C29H23F6N5O3
Molecular Weight 603.515
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

MK-8031 (also known as Atogepant) is piperidinonylcarboxamideazaindane derivative patented by Merck Sharp & Dohme Corp as CGRP receptor antagonist useful for prevention and treatment of Migraine. A press release in June 2018 announced positive results for MK-8031, in a Phase 2 trial of daily use for episodic migraine prevention. MK-8031appeared to show good efficacy in migraine prevention and no significant liver toxicity signal at any dose despite daily dosing for 3 months. Phase III clinical trial was initiated in 2019 and currently in progress.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventive
QULIPTA

Approved Use

QULIPTA is indicated for the preventive treatment of episodic migraine in adults.

Launch Date

2021
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
538.55 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
586.89 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
474.85 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
515.45 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
81.7 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
271 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
561 ng/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
527.4 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: HIGH-FAT
677.01 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
57.2 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
191.5 ng/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
396.5 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
55.3 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
183.1 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
381.8 ng/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
651 ng/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
576 ng/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1013 ng/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
989 ng/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2021 ng/mL
170 mg 1 times / day multiple, oral
dose: 170 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1706 ng/mL
170 mg 1 times / day multiple, oral
dose: 170 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
392 ng/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
444 ng/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
521 ng/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
695 ng/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2633.43 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
3273.58 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
3028.57 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
3633.22 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
525 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1830 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3740 ng × h/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2606.55 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: HIGH-FAT
3158.38 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
345.7 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1253 ng × h/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2671.4 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
319.8 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1147.6 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2424.2 ng × h/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2474 ng × h/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2275 ng × h/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3729 ng × h/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3965 ng × h/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10863 ng × h/mL
170 mg 1 times / day multiple, oral
dose: 170 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
9475 ng × h/mL
170 mg 1 times / day multiple, oral
dose: 170 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1376 ng × h/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1442 ng × h/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2518 ng × h/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3757 ng × h/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
9.4 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
8.7 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
11.9 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
7.54 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
8.6 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8.5 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8.5 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.3 h
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.2 h
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.2 h
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
ATOGEPANT plasma
Homo sapiens
1.79%
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
2.64%
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
2.95%
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
4.66%
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATOGEPANT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Disc. AE: Fatifue, Nausea...
AEs leading to
discontinuation/dose reduction:
Fatifue (3.3%)
Nausea (1.1%)
Constipation (1.1%)
Dizziness (2.2%)
Decreased appetite (1.1%)
Insomnia (1.1%)
Sources:
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Disc. AE: Constipation, Nausea...
AEs leading to
discontinuation/dose reduction:
Constipation (2 patients)
Nausea (1 patient)
Fatigue (1 patient)
ALT increased (1 patient)
Decreased appetite (1 patient)
Insomnia (1 patient)
Rash (2 patients)
Migraine (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Constipation 1.1%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Decreased appetite 1.1%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Insomnia 1.1%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Nausea 1.1%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Dizziness 2.2%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
Fatifue 3.3%
Disc. AE
60 mg 2 times / day steady, oral
Highest studied dose
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, ADULT
ALT increased 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Decreased appetite 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Fatigue 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Insomnia 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Migraine 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Nausea 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Constipation 2 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
Rash 2 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, ADULT
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 1.23 uM]
no [IC50 16 uM]
no [IC50 2.24 uM]
no [IC50 3.3 uM]
no [IC50 34 uM]
no [IC50 41 uM]
no [IC50 8.4 uM]
no [IC50 83 uM]
no [IC50 83 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >122 uM]
no [IC50 >15 uM]
no [IC50 >15 uM]
no [IC50 >20 uM]
no
no
no
no
no
no
no
no
weak [IC50 59 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Itraconazole increased AUCinf and Cmax by 5.5-fold and 2.2-fold
Page: 32 | 33 | 112 | 159 | 166
minor
no
no
no
yes
yes
yes (co-administration study)
Comment: BCRP inhibitor increased AUCinf and Cmax by 1.2-fold and 1.3-fold
Page: 32 | 33 | 113 | 159
yes
yes (co-administration study)
Comment: Rifampicin increased AUCinf and Cmax by 2.9-fold and 2.2-fold
Page: 32 | 33 | 113 | 160 | 167
yes
yes (co-administration study)
Comment: Rifampicin increased AUCinf and Cmax by 2.9-fold and 2.2-fold
Page: 32 | 33 | 113 | 160 | 167
yes
yes (co-administration study)
Comment: Quinidine increased AUCinf and Cmax by 1.3-fold and 1.04-fold
Page: 32 | 33 | 113 | 159
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

The recommended dosage of QULIPTA is 10 mg, 30 mg, or 60 mg taken orally once daily with or without food.
Route of Administration: Oral
The inhibition of vasodilatory responses to CGRP resulted in significant blockade with atogepant 10 nM (P = 0.003), 100 nM (P = 0.001) and 1 uM (P < 0.01) in distal HCA.
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:17:05 GMT 2025
Edited
by admin
on Mon Mar 31 22:17:05 GMT 2025
Record UNII
7CRV8RR151
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
atogepant [INN]
Preferred Name English
ATOGEPANT
INN  
USAN   INN  
Official Name English
ATOGEPANT [ORANGE BOOK]
Common Name English
ATOGEPANT [USAN]
Common Name English
QULIPTA
Brand Name English
SPIRO(6H-CYCLOPENTA(B)PYRIDINE-6,3'-(3H)PYRROLO(2,3-B)PYRIDINE)-3-CARBOXAMIDE, 1',2',5,7-TETRAHYDRO-N-((3S,5S,6R)-6-METHYL-2-OXO-1-(2,2,2-TRIFLUOROETHYL)-5-(2,3,6-TRIFLUOROPHENYL)-3-PIPERIDINYL)-2'-OXO-, (3'S)-
Systematic Name English
Atogepant [WHO-DD]
Common Name English
(3'S)-1',2',5,7-TETRAHYDRO-N-((3S,5S,6R)-6-METHYL-2-OXO-1-(2,2,2-TRIFLUOROETHYL)-5-(2,3,6-TRIFLUOROPHENYL)-3-PIPERIDINYL)-2'-OXOSPIRO(6H-CYCLOPENTA(B)PYRIDINE-6,3'-(3H)PYRROLO(2,3-B)PYRIDINE)-3-CARBOXAMIDE
Systematic Name English
AGN-241689
Code English
MK-8031
Code English
Code System Code Type Description
CAS
1374248-81-3
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
PUBCHEM
72163100
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
SMS_ID
300000011223
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
FDA UNII
7CRV8RR151
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
INN
10510
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
DAILYMED
7CRV8RR151
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
USAN
EF-106
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
WIKIPEDIA
Atogepant
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
EPA CompTox
DTXSID901337079
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
NCI_THESAURUS
C167018
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
RXCUI
2571813
Created by admin on Mon Mar 31 22:17:05 GMT 2025 , Edited by admin on Mon Mar 31 22:17:05 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
BINDS TO RECEPTOR AND BLOCKS BINDING
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Originator: Merck & Co; Class: Piperidine, Small molecule, Spiro compound; Mechanism of Action: Calcitonin gene-related peptide receptor antagonists; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: Preclinical for Migraine; Most Recent Events: 09 Jul 2015 Merck enters into an agreement with Allergan for the divestiture of MK 8031, 07 Jul 2015 Merck plans a phase II study for Migraine, 07 Jul 2015 Preclinical development is underway in USA