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Details

Stereochemistry ACHIRAL
Molecular Formula C22H23N5O2
Molecular Weight 389.4503
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SOLCITINIB

SMILES

CC1(C)CN(C1)C(=O)C2=CC=C(C=C2)C3=CC=CC4=NC(NC(=O)C5CC5)=NN34

InChI

InChIKey=MPYACSQFXVMWNO-UHFFFAOYSA-N
InChI=1S/C22H23N5O2/c1-22(2)12-26(13-22)20(29)16-10-6-14(7-11-16)17-4-3-5-18-23-21(25-27(17)18)24-19(28)15-8-9-15/h3-7,10-11,15H,8-9,12-13H2,1-2H3,(H,24,25,28)

HIDE SMILES / InChI

Molecular Formula C22H23N5O2
Molecular Weight 389.4503
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Solcitinib (also known as GSK2586184 or GLPG0778) is a selective Janus kinase 1 (JAK1) inhibitor, for the treatment of psoriasis, lupus, and ulcerative colitis. Galapagos NV's collaboration with GlaxoSmithKline has hit a roadblock. It was reported that its Big Pharma partner had hit the brakes on a Phase II study of GSK2586184 for lupus after a first look at the data failed to demonstrate a positive effect. And an exploratory Phase I/II of the same drug for ulcerative colitis was put on hold as investigators review the program.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Unknown

Approved Use

Unknown
Palliative
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
779.8 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1871.7 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4787.7 μg × h/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7546.1 μg × h/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
7656.32 ng × h/mL
400 mg 2 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
9.7 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.8 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLCITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Patents

Sample Use Guides

at doses of 50 mg twice daily (b.i.d), 100 mg b.i.d, 200 mg b.i.d, 400 mg b.i.d up to 12 weeks
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:00:29 GMT 2025
Edited
by admin
on Mon Mar 31 22:00:29 GMT 2025
Record UNII
3V7GQ1260K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SOLCITINIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
solcitinib [INN]
Preferred Name English
CYCLOPROPANECARBOXAMIDE, N-(5-(4-((3,3-DIMETHYL-1-AZETIDINYL)CARBONYL)PHENYL)(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)-
Systematic Name English
GLPG-0788
Code English
Solcitinib [WHO-DD]
Common Name English
GSK-2586184
Code English
GLPG-0778
Code English
G-154578
Code English
GLPG0778
Code English
GSK-2586184A
Code English
SOLCITINIB [USAN]
Common Name English
GSK2586184A
Code English
G154578
Code English
N-(5-(4-((3,3-DIMETHYL-1-AZETIDINYL)CARBONYL)PHENYL)(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)CYCLOPROPANECARBOXAMIDE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
NCI_THESAURUS C574
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
Code System Code Type Description
INN
10047
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
NCI_THESAURUS
C152385
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
FDA UNII
3V7GQ1260K
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
PUBCHEM
44603362
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
SMS_ID
100000174858
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
CAS
1206163-45-2
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
ChEMBL
CHEMBL3301606
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
USAN
BC-49
Created by admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
PRIMARY
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