General
Preferred name
leniolisib
Synonyms
CDZ173 ()
CDZ173 (phosphate) ()
CDZ-173 ()
Leniolisib (phosphate) ()
CDZ-173 FREE BASE ()
CDZ-173-NX ()
CDZ173 FREE BASE ()
CDZ173-NX ()
leniolisib (CDZ 173) ()
Joenja ()
Leniolisib monophosphate ()
CDZ173-AZ ()
CDZ-173-AZ ()
LENIOLISIB PHOSPHATE ()
P&D ID
PD053925
CAS
1354690-24-6
1354691-97-6
Tags
available
drug
probe
Approved by
FDA
First approval
2023
Drug indication
Sjogren syndrome
Drug Status
investigational
approved
Max Phase
4.0
Probe info
Probe selectivity
protein-selective
Probe type
P&D approved
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
19
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Leniolisib is an orally active, potent phosphatidylinositol 3-kinase inhibitor (PI3K) inhibitor, with selectivity for the PI3Kδ isoform. Novartis originally developed CDZ173 as a treatment for autoimmune diseases, but has rapidly repurposed it for its potential in patients with Activated PI3K Delta Syndrome (APDS, a.k.a. p110 delta activating mutation causing senescent T cells, lymphadenopathy and immunodeficiency, or PASLI). APDS is a rare genetic immunodeficiency disease characterised by lymphoproliferation, recurrent infections from childhood, and an increased risk of EBV-associated lymphoma. APDS is known to be caused by autosomal dominant, gain-of-function mutations in the PIK3CD gene which encodes the PI3Kδ protein .
DESCRIPTION
Leniolisib (CDZ173) is an orally bioavailable, potent phosphatidylinositol 3-kinase inhibitor (PI3K) inhibitor, with selectivity for the PI3Kδ isoform . Novartis originally developed CDZ173 as a treatment for autoimmune diseases, but has rapidly repurposed it for its potential in patients with Activated PI3K Delta Syndrome (APDS, a.k.a. p110 delta activating mutation causing senescent T cells, lymphadenopathy and immunodeficiency, or PASLI). APDS is an ultra-rare genetic immunodeficiency disease characterised by lymphoproliferation, recurrent infections from childhood, and an increased risk of EBV-associated lymphoma. APDS is known to be caused by autosomal dominant, gain-of-function mutations in the PIK3CD gene which encodes the PI3Kδ protein .
(GtoPdb)
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
On March 2023, FDA approved Leniolosib to treat activated phosphoinositide 3-kinase delta syndrome
(PKIDB)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
7
Organisms
2
Compound Sets
21
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
29
Molecular Weight
450.2
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
2
cLogP
2.88
TPSA
83.48
Fraction CSP3
0.52
Chiral centers
1.0
Largest ring
6.0
QED
0.75
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
PI3K/Akt/mTOR signaling
DNA Damage/DNA Repair
PI3K/Akt/mTOR
Target
PI3K??
DNA-PK
PI3K¦Ä
PIK3CD
MOA
PI3K
PI3K Delta inhibitor
PI3K inhibitor
Member status
virtual
Target class
Kinase
Target subclass
PI3/PI4
Recommended Cell Concentration
1 µM
Source data
