zanubrutinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors 5353 1691249-45-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • zanubrutinib
  • BGB-3111
  • brukinsa
BRUKINSA (zanubrutinib) is a Bruton’s tyrosine kinase (BTK) inhibitor. Zanubrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. In B-cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. In nonclinical studies, zanubrutinib inhibited malignant B-cell proliferation and reduced tumor growth.
  • Molecular weight: 471.56
  • Formula: C27H29N5O3
  • CLOGP: 2.85
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 102.48
  • ALOGS: -4.66
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 14, 2019 FDA BEIGENE USA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EL03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Bruton's tyrosine kinase (BTK) inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D047428 Protein Kinase Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Mantle cell lymphoma indication 443487006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.85 acidic
pKa2 2.64 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Nov. 14, 2024 NEW CHEMICAL ENTITY
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Nov. 14, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA (MCL) WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR IC50 9.52 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4038969 VANDF
C4727614 UMLSCUI
BA0 PDB_CHEM_ID
CHEMBL3936761 ChEMBL_ID
D11422 KEGG_DRUG
C000629551 MESH_SUPPLEMENTAL_RECORD_UI
135565884 PUBCHEM_CID
10555 INN_ID
AG9MHG098Z UNII
9861 IUPHAR_LIGAND_ID
DB15035 DRUGBANK_ID
2262435 RXNORM
326780 MMSL
37672 MMSL
d09435 MMSL
018195 NDDF
830103007 SNOMEDCT_US
830162004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRUKINSA HUMAN PRESCRIPTION DRUG LABEL 1 72579-011 CAPSULE, GELATIN COATED 80 mg ORAL NDA 30 sections