FILGOTINIB

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 Search

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
Sources: http://www.glpg.com/filgotinib
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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Tyrosine-protein kinase JAK1 36 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460\|https://www.ncbi.nlm.nih.gov/pubmed/24417533\|https://www.ncbi.nlm.nih.gov/pubmed/25369270	Inhibitor 8146	10.0 nM [IC50]
Tyrosine-protein kinase JAK1 36 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8146	10.0 nM [IC50]
Tyrosine-protein kinase JAK2 53 Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8146	28.0 nM [IC50]
Tyrosine-protein kinase JAK3 26 Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8146	810.0 nM [IC50]
Tyrosine-protein kinase TYK2 16 Target ID: CHEMBL3553 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8146	116.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Crohn's disease 37 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 651	Unknown Approved Use Unknown
Ulcerative colitis 122 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 651	Unknown Approved Use Unknown
Rheumatoid arthritis 310 Sources: http://adisinsight.springer.com/drugs/800032685 https://www.ncbi.nlm.nih.gov/pubmed/25681059 http://www.glpg.com/filgotinib	Primary	Phase III 651	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
2580 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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
4.42 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31797578	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
1160 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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

AUC

Value	Dose	Analyte	Population
10200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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
16.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31797578	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
4844 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.09 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	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

Doses

Dose	Population	Adverse 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: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	Disc. AE: Skin rash... AEs leading to discontinuation/dose reduction: Skin rash (grade 1, 2.1%) Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6

AEs

AE	Significance	Dose	Population
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: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 753	inhibitor 1695	inhibitor 1789	inhibitor 1570

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 670 UGT1A1 200 UGT1A4 76 UGT1A6 107 CYP1A2 1463 CYP2B6 770 CYP2E1 846 UGT1A9 115 CYP3A4/5 261 CYP2C8 869 CYP2C19 1410 UGT2B7 145 P-gp 1401 OCT2 630 OCT1 498 OAT3 625 OAT1 584 OATP1B3 691 OCT3 143 BSEP 392 OATP1B1 770 BCRP 678 MATE1 302 OAT2 144 MATE2-K 9	CES1b 4 CES1c 4 CES2 24 P-gp 1491 BCRP 545 OATP1B1 389 OATP1B3 333	CYP1A2 671 CYP2B6 521

Drug as perpetrator

Target	Modality	Activity	Metabolite
OATP1B1 785	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 110 uM]
OCT1 513	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 140 uM]	GS-829845 4
OCT1 513	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 151.6 uM]
OATP1B3 700	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 158 uM]	GS-829845 4
OATP1B3 700	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 168 uM]
OCT3 143	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 188 uM]
OATP1B1 785	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 90 uM]	GS-829845 4
OAT1 588	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
OAT3 627	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
CYP2A6 702	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >105.8 uM]
BSEP 393	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >170 uM]
BCRP 751	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
P-gp 1588	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
CYP1A2 1620	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2A6 702	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2B6 946	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C19 1484	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C8 923	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C9 1747	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2D6 1826	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2E1 929	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP3A4/5 314	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
MATE1 304	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT1 588	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT2 146	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]
OAT2 146	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT3 627	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OCT3 143	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
P-gp 1588	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >40 uM]	GS-829845 4
BCRP 751	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >50 uM]	GS-829845 4
BSEP 393	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >500 uM]	GS-829845 4
UGT1A1 249	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A4 79	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A6 139	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A9 120	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT2B7 156	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
CYP2C19 1484	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2C8 923	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2C9 1747	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2E1 929	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
UGT1A1 249	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A4 79	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A6 139	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A9 120	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT2B7 156	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
CYP1A2 1620	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP1A2 1620	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP2B6 946	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP2B6 946	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP3A4 1857	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP3A4 1857	inducer 1515 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP1A2 1620	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP2B6 946	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP2D6 1826	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP3A4/5 314	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
MATE2-K 9	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 10.9 uM]	GS-829845 4
OCT2 631	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 14.9 uM]	GGS-829845 4
MATE2-K 9	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 5.21 uM]
MATE1 304	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 8.63 uM]
OCT2 631	inhibitor 3185 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 8.7 uM]

Drug as victim

Target	Modality	Activity
CES2 24	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	major
CES1b 4	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
CES1c 4	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
BCRP 545	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B1 389	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B3 333	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
P-gp 1491	substrate 3264 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1603	inhibitor 1584 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=9 Page: 9.0

PubMed

Title	Date	PubMed
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.	2013 Oct 1	24006460

Patents

Sample Use Guides

In Vivo Use Guide

Daily dose range up to 200 mg

Route of Administration: Oral

In Vitro Use Guide

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 `Sat Dec 17 17:32:21 UTC 2022` Edited by `admin` on `Sat Dec 17 17:32:21 UTC 2022`
Record UNII	3XVL385Q0M
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

FILGOTINIB

Official 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

G-146034

Code

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