U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ACHIRAL
Molecular Formula C21H23N5O3S
Molecular Weight 425.504
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FILGOTINIB

SMILES

O=C(NC1=NN2C(C=CC=C2C3=CC=C(CN4CCS(=O)(=O)CC4)C=C3)=N1)C5CC5

InChI

InChIKey=RIJLVEAXPNLDTC-UHFFFAOYSA-N
InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)

HIDE SMILES / InChI

Molecular Formula C21H23N5O3S
Molecular Weight 425.504
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including: http://adisinsight.springer.com/drugs/800032685 | http://www.glpg.com/docs/view/564327aec62e3-en | http://www.glpg.com/docs/view/5719315eea963-en

Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2580 ng/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1160 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
4.42 μg/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
565 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
556 ng/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10200 ng × h/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
4844 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
16.3 μg × h/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1743 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2380 ng × h/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.09 h
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
5.68 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
4.91 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.87 h
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FILGOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
42.5%
FILGOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
450 mg 1 times / day multiple, oral
Highest studied dose
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Sources:
Disc. AE: Skin rash...
AEs leading to
discontinuation/dose reduction:
Skin rash (grade 1, 2.1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Skin rash grade 1, 2.1%
Disc. AE
450 mg 1 times / day multiple, oral
Highest studied dose
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 110 uM]
no [IC50 140 uM]
no [IC50 151.6 uM]
no [IC50 158 uM]
no [IC50 168 uM]
no [IC50 188 uM]
no [IC50 90 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >105.8 uM]
no [IC50 >170 uM]
no [IC50 >200 uM]
no [IC50 >200 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >224 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >40 uM]
no [IC50 >50 uM]
no [IC50 >500 uM]
no [IC50 >60 uM]
no [IC50 >60 uM]
no [IC50 >60 uM]
no [IC50 >60 uM]
no [IC50 >60 uM]
no [IC50 >70.6 uM]
no [IC50 >70.6 uM]
no [IC50 >70.6 uM]
no [IC50 >70.6 uM]
no [IC50 >80 uM]
no [IC50 >80 uM]
no [IC50 >80 uM]
no [IC50 >80 uM]
no [IC50 >80 uM]
no
no
no
no
no
no
weak [IC50 >70.6 uM]
weak [IC50 >70.6 uM]
weak [IC50 >70.6 uM]
weak [IC50 >70.6 uM]
yes [IC50 10.9 uM]
yes [IC50 14.9 uM]
yes [IC50 5.21 uM]
yes [IC50 8.63 uM]
yes [IC50 8.7 uM]
Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

Daily dose range up to 200 mg
Route of Administration: Oral
Filgotinib inhibited IL-2– and IL-4–induced JAK1/JAK3/γc signaling and IFN-αB2–induced JAK1/TYK2 type II receptor signaling most potently. IC50 values ranged from 150 to 760 nM.
Substance Class Chemical
Created
by admin
on Mon Mar 31 21:24:27 GMT 2025
Edited
by admin
on Mon Mar 31 21:24:27 GMT 2025
Record UNII
3XVL385Q0M
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FILGOTINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
G-146034
Preferred Name English
GS-6034 FREE BASE
Code English
CYCLOPROPANECARBOXAMIDE, N-(5-(4-((1,1-DIOXIDO-4-THIOMORPHOLINYL)METHYL)PHENYL)(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)-
Systematic Name English
FILGOTINIB [USAN]
Common Name English
Filgotinib [WHO-DD]
Common Name English
filgotinib [INN]
Common Name English
G146034
Code English
N-(5-(4-((1,1-OXO-.LAMBDA.6-THIOMORPHOLIN-4-YL)METHYL)PHENYL((1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)CYCLOPROPANECARBOXAMIDE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
NCI_THESAURUS C1967
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C155799
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
ChEMBL
CHEMBL3301607
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
FDA UNII
3XVL385Q0M
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
EVMPD
SUB182273
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
EPA CompTox
DTXSID80152935
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
PUBCHEM
49831257
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
WIKIPEDIA
Filgotinib
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
USAN
BC-110
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
CAS
1206161-97-8
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
SMS_ID
100000168720
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
INN
9720
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
DRUG BANK
DB14845
Created by admin on Mon Mar 31 21:24:27 GMT 2025 , Edited by admin on Mon Mar 31 21:24:27 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
TARGETF->WEAK INHIBITOR
IC50
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGETF->WEAK INHIBITOR
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
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METABOLITE -> PARENT
FECAL
METABOLITE LESS ACTIVE -> PARENT
FECAL
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ACTIVE MOIETY