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
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)
DescriptionSources: http://www.glpg.com/filgotinibCurator'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
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 | Condition | Potency |
---|---|---|---|
10.0 nM [IC50] | |||
Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460 |
10.0 nM [IC50] | ||
Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460 |
28.0 nM [IC50] | ||
Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460 |
810.0 nM [IC50] | ||
Target ID: CHEMBL3553 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460 |
116.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | 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 | Co-administered | 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 |
T1/2
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: Page: p.6 |
healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: Page: p.6 |
Disc. AE: Skin rash... AEs leading to discontinuation/dose reduction: Skin rash (grade 1, 2.1%) Sources: 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: Page: p.6 |
healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: Page: p.6 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0 |
major | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0 |
minor | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0 |
minor | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0 |
no | |||
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 |
---|---|---|---|---|
Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=9 Page: 9.0 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25681059
Daily dose range up to 200 mg
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460
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.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C129825
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NCI_THESAURUS |
C1967
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C155799
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CHEMBL3301607
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3XVL385Q0M
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SUB182273
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DTXSID80152935
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49831257
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Filgotinib
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BC-110
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1206161-97-8
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100000168720
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9720
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DB14845
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ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE LESS ACTIVE (PARENT)
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)