zanubrutinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors | 5353 | 1691249-45-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.32 | g | O |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 22, 2021 | EMA | BEIGENE IRELAND LTD | |
| Nov. 14, 2019 | FDA | BEIGENE USA INC |
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 | 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Waldenström macroglobulinemia | indication | 190818004 | DOID:0050747 |
| Mantle cell lymphoma | indication | 443487006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.85 | acidic |
| pKa2 | 2.64 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 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 | 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 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 | 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 MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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 | 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 WALDENSTR¿M’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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase BTK | Kinase | INHIBITOR | IC50 | 9.52 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Platelet glycoprotein VI | Unclassified | IC50 | 6.29 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| AG9MHG098Z | UNII |
| C4683810 | UMLSCUI |
| BA0 | PDB_CHEM_ID |
| CHEMBL3936761 | ChEMBL_ID |
| 135565884 | PUBCHEM_CID |
| DB15035 | DRUGBANK_ID |
| D11422 | KEGG_DRUG |
| 9861 | IUPHAR_LIGAND_ID |
| 2262435 | RXNORM |
| 326780 | MMSL |
| 37672 | MMSL |
| d09435 | MMSL |
| 830103007 | SNOMEDCT_US |
| 830162004 | SNOMEDCT_US |
| 4038969 | VANDF |
| 018195 | NDDF |
| C000629551 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10555 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |