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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
Structure of SELETALISIB

SMILES

[O-][N+]1=CC=CC(=C1)C2=C(C=C3C=CC=C(Cl)C3=N2)[C@@H](NC4=C5N=CC=CC5=NC=N4)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

HIDE SMILES / InChI

Description

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

PubMed

PubMed

TitleDatePubMed
A Dual-Administration Microtracer Technique to Characterize the Absorption, Distribution, Metabolism, and Excretion of [14 C]Seletalisib (UCB5857) in Healthy Subjects.
2017 Dec
Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3Kδ.
2017 Jun
First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases.
2017 May

Sample Use Guides

In Vivo Use Guide
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
Name Type Language
SELETALISIB
INN   WHO-DD  
INN  
Official Name English
N-((R)-1-(8-CHLORO-2-(1-OXOPYRIDIN-3-YL)QUINOLIN-3-YL)-2,2,2-TRIFLUOROETHYL)PYRIDO(3,2-D)PYRIMIDIN-4-YLAMINE
Systematic Name English
SELETALISIB [INN]
Common Name English
SELETALISIB [WHO-DD]
Common Name English
UCB-5857
Code English
3-(8-CHLORO-3-((1R)-1-((PYRIDO(3,2-D)PYRIMIDIN-4-YL)AMINO)-2,2,2-TRIFLUOROETHYL)QUINOLIN-2-YL)PYRIDINE N-OXIDE
Systematic Name English
UCB5857
Code English
PYRIDO(3,2-D)PYRIMIDIN-4-AMINE, N-((1R)-1-(8-CHLORO-2-(1-OXIDO-3-PYRIDINYL)-3-QUINOLINYL)-2,2,2-TRIFLUOROETHYL)-
Systematic Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/18/1986
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
FDA ORPHAN DRUG 596517
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
FDA ORPHAN DRUG 579917
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
NCI_THESAURUS C1404
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
Code System Code Type Description
PUBCHEM
56928390
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
PRIMARY
NCI_THESAURUS
C152320
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
PRIMARY
EVMPD
SUB185136
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
PRIMARY
CAS
1362850-20-1
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
PRIMARY
INN
10023
Created by admin on Mon Oct 21 20:10:01 UTC 2019 , Edited by admin on Mon Oct 21 20:10:01 UTC 2019
PRIMARY