Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C23H14ClF3N6O |
Molecular Weight | 482.845 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][N+]1=CC=CC(=C1)C2=NC3=C(C=CC=C3Cl)C=C2[C@@H](NC4=NC=NC5=C4N=CC=C5)C(F)(F)F
InChI
InChIKey=LNLJHGXOFYUARS-OAQYLSRUSA-N
InChI=1S/C23H14ClF3N6O/c24-16-6-1-4-13-10-15(18(31-19(13)16)14-5-3-9-33(34)11-14)21(23(25,26)27)32-22-20-17(29-12-30-22)7-2-8-28-20/h1-12,21H,(H,29,30,32)/t21-/m1/s1
Seletalisib (UCB-5857) is a potent, ATP-competitive, and selective phosphoinositide 3-kinase (PI3K) delta inhibitor. Findings from cellular assays of adaptive immunity demonstrated that seletalisib blocks human T-cell production of several cytokines from activated T-cells. Additionally, seletalisib inhibited B-cell proliferation and cytokine release. In human whole blood assays, seletalisib inhibited CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation. Seletalisib safety, tolerability and pharmacokinetic/pharmacodynamic profiles support its continued clinical development in immune-inflammatory diseases. UCB Pharma is developing Seletalisib for the treatment of immune and inflammatory diseases including Activated PI3K delta Syndrome (APDS), Sjogren's syndrome and psoriasis.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3130 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28442583 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28160012
The phase I, randomised, double-blind, placebo-controlled, single-centre studies (NCT02303509, NCT02207595) evaluated single and multiple oral doses of seletalisib (5-90 mg QD and 30 mg BID) in healthy adults and subjects with mild-to-moderate psoriasis (Study-1). Seletalisib was well tolerated at doses ≤15 mg (Study-1) and ≤45 mg QD (Study-2) for 14 days. No safety concerns or dose-limiting toxicities were identified (Study-1).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28442583
Curator's Comment: Findings from cellular assays of adaptive immunity demonstrated that seletalisib blocks human T-cell production of several cytokines from activated T-cells. Additionally, seletalisib inhibited B-cell proliferation and cytokine release. In human whole blood assays, seletalisib inhibited CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation.
Unknown
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
EU-Orphan Drug |
EU/3/18/1986
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
||
|
FDA ORPHAN DRUG |
596517
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
||
|
FDA ORPHAN DRUG |
579917
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
||
|
NCI_THESAURUS |
C1404
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DB12706
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
56928390
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
C152320
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
100000170923
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
SUB185136
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
1362850-20-1
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
10023
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY | |||
|
64CW205BDD
Created by
admin on Sat Dec 16 09:44:28 GMT 2023 , Edited by admin on Sat Dec 16 09:44:28 GMT 2023
|
PRIMARY |
ACTIVE MOIETY