All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

leniolisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics	5715	1354690-24-6

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: leniolisib leniolisib phosphate joenja CDZ173-NX CDZ-173 CDZ173

Leniolisib inhibits PI3K-delta by blocking the active binding site of PI3K-delta. In cell-free isolated enzyme assays, leniolisib was selective for PI3K-delta over PI3K-alpha (28-fold), PI3K-beta (43-fold), and PI3K-gamma (257-fold), as well as the broader kinome. In cell-based assays, leniolisib reduced pAKT pathway activity and inhibited proliferation and activation of B and T cell subsets. Gain-of-function variants in the gene encoding the p110-delta catalytic subunit or loss of function variants in the gene encoding the p85-alpha regulatory subunit each cause hyperactivity of PI3K-delta. Leniolisib inhibits the signalling pathways that lead to increased production of PIP3, hyperactivity of the downstream mTOR/AKT pathway, and to the dysregulation of B and T cells. Molecular weight: 450.47 Formula: C21H25F3N6O2 CLOGP: 2.88 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 83.48 ALOGS: ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	EIF2AK3,GRK2,PDK1,PDK2,PDK4,PIK3CD,PRKDC	7
pfas-class	PFAS structural alert (1 = True, 0 = False)	1

Approvals:

Date	Agency	Company	Orphan
March 24, 2023	FDA	PHARMING

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L03AX22	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSTIMULANTS IMMUNOSTIMULANTS Other immunostimulants
MeSH PA	D000081082	Phosphoinositide-3 Kinase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182138	Cytochrome P450 1A2 Inhibitors
FDA MoA	N0000190107	Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA	N0000190108	Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000194054	Phosphoinositide 3-Kinase delta Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:50846	immunomodulator
CHEBI has role	CHEBI:229651	EC 2.7.1.153 (phosphatidylinositol-4,5-bisphosphate 3-kinase) inhibitor

Related Drugs by ATC class:

L03AX Other immunostimulants 15 drugs

cridanimodelapegademaseglatiramer acetatehistaminelentinanmavorixaformifamurtidemotixafortidepegademasepidotimodplerixaforroquinimex show all 15 →

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Activated PI3K delta syndrome (APDS)	indication	711480000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 70MG BASE	JOENJA	PHARMING	N217759	March 24, 2023	RX	TABLET	ORAL	March 24, 2028	NEW CHEMICAL ENTITY
EQ 70MG BASE	JOENJA	PHARMING	N217759	March 24, 2023	RX	TABLET	ORAL	March 24, 2030	TREATMENT OF ACTIVATED PHOSPHOINOSITIDE 3-KINASE DELTA (PI3K DELTA) SYNDROME (APDS) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Kinase	O00329	PK3CD_HUMAN	INHIBITOR	IC50	7.25		DRUG LABEL	DRUG LABEL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D	Enzyme	Q08499	PDE4D_HUMAN		IC50	5.33		CHEMBL
DNA-dependent protein kinase catalytic subunit	Kinase	P78527	PRKDC_HUMAN		IC50	6.06		CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Kinase	P48736	PK3CG_HUMAN		IC50	6.04		CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		IC50	5.11		CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN	INHIBITOR	IC50	5.79		DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Kinase	P42338	PK3CB_HUMAN	INHIBITOR	IC50	5.63		DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Kinase		PK3CG_MOUSE		IC50	5.39		CHEMBL

External reference:

ID	Source
CHEBI:229649	CHEBI
9NQ	PDB_CHEM_ID
CHEMBL3643413	ChEMBL_ID
C000625376	MESH_SUPPLEMENTAL_RECORD_UI
9424	IUPHAR_LIGAND_ID
DB16217	DRUGBANK_ID
933450921000036101	SNOMEDCT_US
4042147	VANDF
C4547202	UMLSCUI
CHEMBL3989909	ChEMBL_ID
10255	INN_ID
1354691-97-6	SECONDARY_CAS_RN
57495353	PUBCHEM_CID
365867	MMSL
41353	MMSL
d10028	MMSL
019356	NDDF
019357	NDDF
D11158	KEGG_DRUG
L22772Z9CP	UNII
2633005	RXNORM
L22772Z9CP	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Joenja	HUMAN PRESCRIPTION DRUG LABEL	1	71274-170	TABLET, FILM COATED	70 mg	ORAL	NDA	29 sections