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
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
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.
CNS Activity
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
Disc. AE: Fatifue, Nausea... AEs leading to discontinuation/dose reduction: Fatifue (3.3%) Sources: Nausea (1.1%) Constipation (1.1%) Dizziness (2.2%) Decreased appetite (1.1%) Insomnia (1.1%) |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
Disc. AE: Constipation, Nausea... AEs leading to discontinuation/dose reduction: Constipation (2 patients) Sources: Nausea (1 patient) Fatigue (1 patient) ALT increased (1 patient) Decreased appetite (1 patient) Insomnia (1 patient) Rash (2 patients) Migraine (1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
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 Health Status: unhealthy Age Group: ADULT Sex: M F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 33 | 161 |
no [IC50 1.23 uM] | |||
Page: 33.0 |
no [IC50 16 uM] | |||
Page: 33 | 161 |
no [IC50 2.24 uM] | |||
Page: 33 | 160 |
no [IC50 3.3 uM] | |||
Page: 33 | 159 |
no [IC50 34 uM] | |||
Page: 33.0 |
no [IC50 41 uM] | |||
Page: 33 | 160 |
no [IC50 8.4 uM] | |||
Page: 33 | 159 |
no [IC50 83 uM] | |||
Page: 33 | 159 |
no [IC50 83 uM] | |||
Page: 33 | 160 |
no [IC50 >10 uM] | |||
Page: 33 | 160 |
no [IC50 >10 uM] | |||
Page: 33 | 159 |
no [IC50 >100 uM] | |||
Page: 33 | 159 |
no [IC50 >100 uM] | |||
Page: 33 | 159 |
no [IC50 >122 uM] | |||
Page: 33 | 161 |
no [IC50 >15 uM] | |||
Page: 161.0 |
no [IC50 >15 uM] | |||
Page: 33 | 161 |
no [IC50 >20 uM] | |||
Page: 33 | 159 |
no | |||
Page: 159.0 |
no | |||
Page: 33 | 159 |
no | |||
Page: 33 | 161 |
no | |||
Page: 33 | 161 |
no | |||
Page: 33 | 160 |
no | |||
Page: 33 | 160 |
no | |||
Page: 33 | 160 |
no | |||
Page: 159.0 |
weak [IC50 59 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 32 | 33 | 112 | 159 | 166 |
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 |
||
Page: 159.0 |
minor | |||
Page: 160.0 |
no | |||
Page: 159.0 |
no | |||
Page: 160.0 |
no | |||
Page: 32 | 33 | 160 |
yes | |||
Page: 32 | 33 | 113 | 159 |
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 |
||
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 |
||
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 |
||
Page: 32 | 33 | 113 | 159 |
yes | yes (co-administration study) Comment: Quinidine increased AUCinf and Cmax by 1.3-fold and 1.04-fold Page: 32 | 33 | 113 | 159 |
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
Substance Class |
Chemical
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
BINDS TO RECEPTOR AND BLOCKS BINDING
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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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
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