zanubrutinib 🐶 Veterinary Use | 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: 2.58
  • 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:

DoseUnitRoute
0.32 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 2021 EMA BEIGENE IRELAND LTD
Nov. 14, 2019 FDA BEIGENE USA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cytokine increased 129.91 67.04 14 470 50 63488488
Cytokine release syndrome 84.74 67.04 20 464 14294 63474244
Hypophosphataemia 78.38 67.04 18 466 11408 63477130
Lymphocyte count decreased 69.89 67.04 20 464 30237 63458301
Hypoalbuminaemia 67.24 67.04 16 468 11789 63476749

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myelosuppression 90.49 54.78 25 439 19240 34937227
Cytokine increased 87.37 54.78 10 454 35 34956432

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cytokine increased 207.35 61.57 24 939 107 79743318
Myelosuppression 128.83 61.57 38 925 40258 79703167
Cytokine release syndrome 102.20 61.57 31 932 35967 79707458
Hypophosphataemia 96.35 61.57 26 937 19887 79723538
Lymphocyte count decreased 93.88 61.57 31 932 47258 79696167
Hypoalbuminaemia 90.00 61.57 25 938 21272 79722153
Blood immunoglobulin G decreased 79.58 61.57 16 947 3393 79740032
Platelet count decreased 76.46 61.57 40 923 194624 79548801
White blood cell count decreased 74.83 61.57 39 924 188249 79555176
Neutrophil count decreased 73.14 61.57 31 932 93928 79649497
Hypokalaemia 69.36 61.57 34 929 144006 79599419
N-terminal prohormone brain natriuretic peptide increased 68.66 61.57 15 948 4740 79738685

FDA Adverse Event Reporting System (Pediatric)

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
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000193934 Brutons Tyrosine Kinase Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Waldenström macroglobulinemia indication 190818004 DOID:0050747
Mantle cell lymphoma indication 443487006
Marginal zone lymphoma indication 447100004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 FOR THE TREATMENT OF PATIENTS WITH WALDENSTROMS MACROGLOBULINEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 10570139 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 FOR THE TREATMENT OF PATIENTS WITH WALDENSTROMS MACROGLOBULINEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11142528 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 FOR THE TREATMENT OF PATIENTS WITH WALDENSTROMS MACROGLOBULINEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 9447106 April 22, 2034 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 FOR THE TREATMENT OF PATIENTS WITH WALDENSTROMS MACROGLOBULINEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL 11591340 Aug. 15, 2037 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Aug. 31, 2024 TREATMENT OF ADULT PATIENTS WITH WALDENSTROM’S MACROGLOBULINEMIA (WM)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Sept. 14, 2024 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE ANTI-CD20-BASED REGIMEN
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 Jan. 19, 2026 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
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
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Aug. 31, 2028 TREATMENT OF ADULT PATIENTS WITH WALDENSTRӦM’S MACROGLOBULINEMIA (WM)
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Sept. 14, 2028 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE ANTI-CD20-BASED REGIMEN
80MG BRUKINSA BEIGENE N213217 Nov. 14, 2019 RX CAPSULE ORAL Jan. 19, 2030 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR IC50 9.52 SCIENTIFIC LITERATURE DRUG LABEL
Epidermal growth factor receptor Kinase IC50 8.22 CHEMBL
Tyrosine-protein kinase Lck Kinase IC50 6.73 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 7.12 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase IC50 8.80 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase IC50 8.27 CHEMBL
Tyrosine-protein kinase Fgr Kinase IC50 6.81 CHEMBL
Tyrosine-protein kinase JAK3 Kinase IC50 6.24 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase IC50 7.18 CHEMBL
Protein-tyrosine kinase 6 Kinase IC50 7.48 CHEMBL
Tyrosine-protein kinase Tec Kinase IC50 8.70 CHEMBL
Tyrosine-protein kinase TXK Kinase IC50 8.53 CHEMBL
Tyrosine-protein kinase Blk Kinase IC50 8.95 CHEMBL
Platelet glycoprotein VI Unclassified IC50 6.29 CHEMBL
Tyrosine-protein kinase FRK Kinase IC50 6.42 CHEMBL

External reference:

IDSource
AG9MHG098Z UNII
C4683810 UMLSCUI
BA0 PDB_CHEM_ID
CHEMBL3936761 ChEMBL_ID
135565884 PUBCHEM_CID
DB15035 DRUGBANK_ID
D11422 KEGG_DRUG
10555 INN_ID
9861 IUPHAR_LIGAND_ID
018195 NDDF
830103007 SNOMEDCT_US
830162004 SNOMEDCT_US
4038969 VANDF
2262435 RXNORM
326780 MMSL
37672 MMSL
d09435 MMSL
C000629551 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRUKINSA HUMAN PRESCRIPTION DRUG LABEL 1 72579-011 CAPSULE, GELATIN COATED 80 mg ORAL NDA 31 sections
BRUKINSA HUMAN PRESCRIPTION DRUG LABEL 1 72579-011 CAPSULE, GELATIN COATED 80 mg ORAL NDA 31 sections
BRUKINSA HUMAN PRESCRIPTION DRUG LABEL 1 72579-011 CAPSULE, GELATIN COATED 80 mg ORAL NDA 31 sections
BRUKINSA HUMAN PRESCRIPTION DRUG LABEL 1 72579-011 CAPSULE, GELATIN COATED 80 mg ORAL NDA 31 sections