U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C27H27F2N5O3
Molecular Weight 507.5318
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of REMIBRUTINIB

SMILES

CN(CCOC1=C(N)N=CN=C1C2=CC(F)=CC(NC(=O)C3=CC=C(C=C3F)C4CC4)=C2C)C(=O)C=C

InChI

InChIKey=CUABMPOJOBCXJI-UHFFFAOYSA-N
InChI=1S/C27H27F2N5O3/c1-4-23(35)34(3)9-10-37-25-24(31-14-32-26(25)30)20-12-18(28)13-22(15(20)2)33-27(36)19-8-7-17(11-21(19)29)16-5-6-16/h4,7-8,11-14,16H,1,5-6,9-10H2,2-3H3,(H,33,36)(H2,30,31,32)

HIDE SMILES / InChI

Molecular Formula C27H27F2N5O3
Molecular Weight 507.5318
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
187 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
233 ng/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
518 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
551 ng/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
550 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
563 ng/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
180 ng/mL
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
REMIBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
306 ng/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
236 ng/mL
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
347 ng/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
315 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
485 ng × h/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
977 ng × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1280 ng × h/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1080 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1230 ng × h/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
337 ng × h/mL
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
REMIBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
496 ng × h/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
464 ng × h/mL
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
963 ng × h/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.41 h
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
8.51 h
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
8.29 h
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.84 h
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
12.4 h
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
REMIBRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Substance Class Chemical
Created
by admin
on Tue Apr 01 19:16:44 GMT 2025
Edited
by admin
on Tue Apr 01 19:16:44 GMT 2025
Record UNII
I7MVZ8HDNU
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LOU064-NXA
Preferred Name English
REMIBRUTINIB
INN   USAN  
Official Name English
remibrutinib [INN]
Common Name English
REMIBRUTINIB [USAN]
Common Name English
N-(3-(6-AMINO-5-(2-(N-METHYLACRYLAMIDO)ETHOXY)PYRIMIDIN-4-YL)-5-FLUORO-2-METHYLPHENYL)-4-CYCLOPROPYL-2-FLUOROBENZAMIDE
Systematic Name English
BENZAMIDE, N-(3-(6-AMINO-5-(2-(METHYL(1-OXO-2-PROPEN-1-YL)AMINO)ETHOXY)-4-PYRIMIDINYL)-5-FLUORO-2-METHYLPHENYL)-4-CYCLOPROPYL-2-FLUORO-
Systematic Name English
Remibrutinib [WHO-DD]
Common Name English
NVP-LOU064-NXA
Code English
Code System Code Type Description
USAN
JK-247
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
INN
11062
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
FDA UNII
I7MVZ8HDNU
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
NCI_THESAURUS
C175851
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
CAS
1787294-07-8
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
PUBCHEM
118107483
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
SMS_ID
300000010835
Created by admin on Tue Apr 01 19:16:44 GMT 2025 , Edited by admin on Tue Apr 01 19:16:44 GMT 2025
PRIMARY
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