leniolisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics 5715 1354690-24-6

Description:

MoleculeDescription

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:
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 83.48
  • ALOGS:
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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:

None

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

DiseaseRelationSNOMED_IDDOID
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase INHIBITOR IC50 7.25 DRUG LABEL DRUG LABEL
DNA-dependent protein kinase catalytic subunit Kinase IC50 6.06 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase IC50 6.04 CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Enzyme IC50 5.33 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase INHIBITOR IC50 5.79 DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform Kinase INHIBITOR IC50 5.63 DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase IC50 5.39 CHEMBL

External reference:

IDSource
9NQ PDB_CHEM_ID
CHEMBL3643413 ChEMBL_ID
C000625376 MESH_SUPPLEMENTAL_RECORD_UI
9424 IUPHAR_LIGAND_ID
DB16217 DRUGBANK_ID
019356 NDDF
019357 NDDF
4042147 VANDF
C4547202 UMLSCUI
CHEMBL3989909 ChEMBL_ID
10255 INN_ID
1354691-97-6 SECONDARY_CAS_RN
57495353 PUBCHEM_CID
2633005 RXNORM
D11158 KEGG_DRUG
L22772Z9CP UNII
365867 MMSL
41353 MMSL
d10028 MMSL

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Joenja HUMAN PRESCRIPTION DRUG LABEL 1 71274-170 TABLET, FILM COATED 70 mg ORAL NDA 27 sections