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Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
108 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
5270 pg/mL
100 μg single, intravenous
dose: 100 μg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
336 ng × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1830 pg × h/mL
100 μg single, intravenous
dose: 100 μg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.2 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.78 h
100 μg single, intravenous
dose: 100 μg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RILZABRUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Substance Class Mixture
Created
by admin
on Mon Mar 31 22:17:23 GMT 2025
Edited
by admin
on Mon Mar 31 22:17:23 GMT 2025
Record UNII
NWN58M4F5T
Record Status FAILED
Record Version
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Name Type Language
(3R)-3-[4-Amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-?-[2-methyl-2-[4-(3-oxetanyl)-1-piperazinyl]propylidene]-?-oxo-1-piperidinepropanenitrile
Preferred Name English
Rilzabrutinib
USAN   INN  
Official Name English
Rilzabrutinib [WHO-DD]
Common Name English
PRN-1008
Code English
1-Piperidinepropanenitrile, 3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-?-[2-methyl-2-[4-(3-oxetanyl)-1-piperazinyl]propylidene]-?-oxo-, (3R)-
Systematic Name English
PRN1008
Code English
rilzabrutinib [INN]
Common Name English
RILZABRUTINIB [USAN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 582517
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
FDA ORPHAN DRUG 605717
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
Code System Code Type Description
SMS_ID
100000177401
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
INN
10966
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
CAS
1575591-66-0
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
USAN
HI-144
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
NCI_THESAURUS
C174769
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
FDA UNII
NWN58M4F5T
Created by admin on Mon Mar 31 22:17:23 GMT 2025 , Edited by admin on Mon Mar 31 22:17:23 GMT 2025
PRIMARY
All of the following components must be present:
Related Record Type Details
TARGET -> INHIBITOR
PRN-1008 is a covalent, but reversible BTK inhibitor
BINDING
IC50
Related Record Type Details
ACTIVE MOIETY
Definition References