FILGOTINIB MALEATE

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H23N5O3S.C4H4O4
Molecular Weight	541.576
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.O=C(NC1=NN2C(C=CC=C2C3=CC=C(CN4CCS(=O)(=O)CC4)C=C3)=N1)C5CC5

InChI

InChIKey=BFENHEAPFWQJFL-BTJKTKAUSA-N

InChI=1S/C21H23N5O3S.C4H4O4/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;5-3(6)1-2-4(7)8/h1-7,17H,8-14H2,(H,23,24,27);1-2H,(H,5,6)(H,7,8)/b;2-1-

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

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
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 39 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8504	10.0 nM [IC50]
Tyrosine-protein kinase JAK2 59 Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8504	28.0 nM [IC50]
Tyrosine-protein kinase JAK3 28 Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8504	810.0 nM [IC50]
Tyrosine-protein kinase TYK2 13 Target ID: CHEMBL3553 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8504	116.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Crohn's disease 64 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 665	Unknown Approved Use Unknown
Ulcerative colitis 125 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 665	Unknown Approved Use Unknown
Rheumatoid arthritis 320 Sources: http://adisinsight.springer.com/drugs/800032685 https://www.ncbi.nlm.nih.gov/pubmed/25681059 http://www.glpg.com/filgotinib	Primary	Phase III 665	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
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
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
565 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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

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
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
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
1743 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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

T_1/2

Value	Dose	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
4.91 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25681059	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
42.5% EXPERIMENT https://ard.bmj.com/content/78/Suppl_2/331.1			FILGOTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

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

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	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/31797578

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 879 UGT1A1 246 UGT1A4 98 UGT1A6 136 CYP1A2 2153 CYP2B6 926 CYP2E1 1060 UGT1A9 148 CYP3A4/5 296 CYP2C8 1057 CYP2C19 2057 UGT2B7 197 P-gp 1741 OCT2 779 OCT1 620 OAT3 747 OAT1 725 OATP1B3 961 OCT3 159 BSEP 550 OATP1B1 1079 BCRP 910 MATE1 415 OAT2 153 MATE2-K 77	CES1b 4 CES1c 4 CES2 33 P-gp 2052 BCRP 697 OATP1B1 503 OATP1B3 435	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Metabolite
OATP1B1 1095	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 110 uM]
OCT1 656	inhibitor 4027 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 656	inhibitor 4027 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 970	inhibitor 4027 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 970	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 168 uM]
OCT3 161	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 188 uM]
OATP1B1 1095	inhibitor 4027 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 730	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
OAT3 749	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
CYP2A6 911	inhibitor 4027 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 554	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >170 uM]
BCRP 985	inhibitor 4027 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 1932	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
CYP1A2 2333	inhibitor 4027 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 911	inhibitor 4027 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 1160	inhibitor 4027 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 2141	inhibitor 4027 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 1117	inhibitor 4027 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 2497	inhibitor 4027 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 2546	inhibitor 4027 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 1146	inhibitor 4027 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
CYP3A4/5 357	inhibitor 4027 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 416	inhibitor 4027 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 730	inhibitor 4027 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 155	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]
OAT2 155	inhibitor 4027 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 749	inhibitor 4027 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 161	inhibitor 4027 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 1932	inhibitor 4027 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 985	inhibitor 4027 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 554	inhibitor 4027 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 303	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A4 100	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A6 171	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A9 155	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT2B7 210	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
CYP2C19 2141	inhibitor 4027 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 1117	inhibitor 4027 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 2497	inhibitor 4027 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 1146	inhibitor 4027 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 303	inhibitor 4027 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 100	inhibitor 4027 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 171	inhibitor 4027 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 155	inhibitor 4027 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 210	inhibitor 4027 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 2333	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP2B6 1160	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP3A4 2633	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP1A2 2333	inhibitor 4027 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 1160	inhibitor 4027 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 2546	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP3A4/5 357	inhibitor 4027 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 77	inhibitor 4027 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 782	inhibitor 4027 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 77	inhibitor 4027 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 416	inhibitor 4027 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 782	inhibitor 4027 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 33	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	major
CES1b 4	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
CES1c 4	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
BCRP 697	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B1 503	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B3 435	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
P-gp 2052	substrate 4014 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 2263	inhibitor 2237 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.	2013-10-01	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 `Tue Apr 01 21:30:14 GMT 2025` Edited by `admin` on `Tue Apr 01 21:30:14 GMT 2025`
Record UNII	JG8OB4UL9Y
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FILGOTINIB MALEATE

Official Name

English

GS-6034

Preferred Name

English

FILGOTINIB MALEATE [JAN]

Common Name

English

Filgotinib maleate [WHO-DD]

Common Name

English

CYCLOPROPANECARBOXAMIDE, N-(5-(4-((1,1-DIOXIDO-4-THIOMORPHOLINYL)METHYL)PHENYL)(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)-, (2Z)-2-BUTENEDIOATE (1:1)

Common Name

English

FILGOTINIB MALEATE [USAN]

Common Name

English

N-(5-{4-[(1,1-Dioxo-?6-thiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide (2Z)-2-butenedioate (1:1)

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

588017