ATOGEPANT

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 Search

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

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/215206Orig1s000lbl.pdf|https://pubmed.ncbi.nlm.nih.gov/34813050https://www.ncbi.nlm.nih.gov/pubmed/30403405 | https://www.ncbi.nlm.nih.gov/pubmed/30484333

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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 2 Target ID: CHEMBL2107838 Sources: https://pubmed.ncbi.nlm.nih.gov/32058712\|https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/215206Orig1s000lbl.pdf\|https://patents.google.com/patent/US20120122911	Antagonist 2849		0.015 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine 107 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/215206Orig1s000lbl.pdf	Preventive		Approved 8583	QULIPTA Approved Use QULIPTA is indicated for the preventive treatment of episodic migraine in adults. Launch Date 2021

C_max

Value	Dose	Analyte	Population
538.55 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=163	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=163	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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	Analyte	Population
2633.43 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=31	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=163	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=163	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=189	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

T_1/2

Value	Dose	Analyte	Population
9.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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 OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=172	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

F_unbound

Value	Dose	Analyte	Population
5% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=158		ATOGEPANT plasma	Homo sapiens
1.79% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=164 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf#page=218	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf

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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 substrate 1946 inducer 1087	inhibitor 2438	substrate 1388 inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 926 CYP2C8 1057 OCT1 620 UGT1A1 246 CYP2C19 2057 OATP1B1 1079 MRP3 246 MATE2-K 77 P-gp 1741 MAO-A 2 BCRP 910 CYP1A2 2153 MATE1 415 OATP1B3 961 OAT1 725 NTCP 39 OCT2 779 MRP4 290 OAT3 747 BSEP 550	BCRP 697 OATP1B1 503 OATP1B3 435 OAT1 395 OAT3 391 P-gp 2052 MATE1 182 OCT2 434	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no [IC50 1.23 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33.0	no [IC50 16 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no [IC50 2.24 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no [IC50 3.3 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 34 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33.0	no [IC50 41 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no [IC50 8.4 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 83 uM]
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 83 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no [IC50 >10 uM]
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no [IC50 >10 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 >100 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 >100 uM]
MAO-A 2	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no [IC50 >122 uM]
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no [IC50 >15 uM]
MRP3 326	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 161.0	no [IC50 >15 uM]
NTCP 40	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no [IC50 >20 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 159.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 159	no
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no
MRP4 345	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 161	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 33 \| 160	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 159.0	weak [IC50 59 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 112 \| 159 \| 166
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 159.0	minor
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 160.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 159.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 160.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 160	yes
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 113 \| 159
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 113 \| 160 \| 167
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 113 \| 160 \| 167
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 113 \| 159	yes	yes (co-administration study) Comment: Quinidine increased AUCinf and Cmax by 1.3-fold and 1.04-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215206Orig1s000IntegratedR.pdf Page: 32 \| 33 \| 113 \| 159

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

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

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