FILGOTINIB MALEATE

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	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

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 38 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 8297	10.0 nM [IC50]
Tyrosine-protein kinase JAK1 38 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8297	10.0 nM [IC50]
Tyrosine-protein kinase JAK2 55 Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8297	28.0 nM [IC50]
Tyrosine-protein kinase JAK3 27 Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8297	810.0 nM [IC50]
Tyrosine-protein kinase TYK2 16 Target ID: CHEMBL3553 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8297	116.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Crohn's disease 42 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 656	Unknown Approved Use Unknown
Ulcerative colitis 123 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 656	Unknown Approved Use Unknown
Rheumatoid arthritis 316 Sources: http://adisinsight.springer.com/drugs/800032685 https://www.ncbi.nlm.nih.gov/pubmed/25681059 http://www.glpg.com/filgotinib	Primary	Phase III 656	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 781	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 707 UGT1A1 204 UGT1A4 77 UGT1A6 108 CYP1A2 1524 CYP2B6 810 CYP2E1 882 UGT1A9 116 CYP3A4/5 278 CYP2C8 911 CYP2C19 1478 UGT2B7 146 P-gp 1461 OCT2 647 OCT1 512 OAT3 642 OAT1 599 OATP1B3 706 OCT3 150 BSEP 402 OATP1B1 788 BCRP 699 MATE1 306 OAT2 145 MATE2-K 9	CES1b 4 CES1c 4 CES2 28 P-gp 1537 BCRP 561 OATP1B1 406 OATP1B3 350	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity	Metabolite
OATP1B1 803	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 110 uM]
OCT1 543	inhibitor 3277 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 543	inhibitor 3277 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 715	inhibitor 3277 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 715	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 168 uM]
OCT3 150	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 188 uM]
OATP1B1 803	inhibitor 3277 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 603	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
OAT3 644	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
CYP2A6 739	inhibitor 3277 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 403	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >170 uM]
BCRP 773	inhibitor 3277 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 1650	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
CYP1A2 1692	inhibitor 3277 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 739	inhibitor 3277 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 1001	inhibitor 3277 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 1553	inhibitor 3277 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 965	inhibitor 3277 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 1819	inhibitor 3277 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 1891	inhibitor 3277 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 970	inhibitor 3277 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
CYP3A4/5 335	inhibitor 3277 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 308	inhibitor 3277 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 603	inhibitor 3277 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 147	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]
OAT2 147	inhibitor 3277 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 644	inhibitor 3277 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 150	inhibitor 3277 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 1650	inhibitor 3277 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 773	inhibitor 3277 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 403	inhibitor 3277 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 254	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A4 80	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A6 141	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A9 121	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT2B7 157	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
CYP2C19 1553	inhibitor 3277 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 965	inhibitor 3277 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 1819	inhibitor 3277 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 970	inhibitor 3277 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 254	inhibitor 3277 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 80	inhibitor 3277 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 141	inhibitor 3277 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 121	inhibitor 3277 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 157	inhibitor 3277 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 1692	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP2B6 1001	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP3A4 1925	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP1A2 1692	inhibitor 3277 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 1001	inhibitor 3277 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 1891	inhibitor 3277 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP3A4/5 335	inhibitor 3277 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 3277 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 648	inhibitor 3277 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 3277 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 308	inhibitor 3277 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 648	inhibitor 3277 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 28	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	major
CES1b 4	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
CES1c 4	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
BCRP 561	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B1 406	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B3 350	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
P-gp 1537	substrate 3367 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 1647	inhibitor 1626 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 16 13:50:22 GMT 2023` Edited by `admin` on `Sat Dec 16 13:50:22 GMT 2023`
Record UNII	JG8OB4UL9Y
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

FILGOTINIB MALEATE

Official 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

GS-6034

Code

English

FILGOTINIB MALEATE [USAN]

Common Name

English

N-(5-{4-[(1,1-Dioxo-λ6-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