zanubrutinib (Brukinsa) Report issue

Small molecule Orphan Drug FDA Approved FDA Accelerated Approval FDA Priority Review FDA
AACT

Active Ingredient History

NOW
  • Now
BGB-3111 is a potent and highly selective small molecule BTK inhibitor (Bruton’s Tyrosine Kinase), which we are developing as a monotherapy and in combination with other therapies for the treatment of a variety of lymphomas—the most common form of blood cancer. BGB-3111 blocks the signaling that leads to growth inhibition and cell death in malignant B-cells. In preclinical studies, BGB-3111 showed more restricted off-target activities against a panel of kinases, including ITK. Due to the weaker activity on ITK, BGB-3111 was at least 10 times weaker than ibrutinib in inhibiting rituximab-induced ADCC activity. Both in the REC-1 MCL and ABC subtype DLBCL (TMD-8) xenograft models, BGB-3111 induced dose-dependent antitumor effects and demonstrated superior efficacy in comparison with ibrutinib. Toxicity study in rats indicated that BGB-3111 was very well tolerated, and the MTD was not reached when it was dosed up to 250 mg/ kg/day. The first-in-human, open-label phase 1 trial of BGB-3111 is ongoing as a modified 3 + 3 dose-escalation design (40, 80, 160, 320 mg PO QD; 160 mg PO BID) in patients with advanced B cell malignancies.   NCATS

Chemistry

  • SMILES: NC(=O)C1=C2NCC[C@@H](C3CCN(CC3)C(=O)C=C)N2N=C1C4=CC=C(OC5=CC=CC=C5)C=C4
  • InChIKey: RNOAOAWBMHREKO-QFIPXVFZSA-N
  • Mol. Mass: 471.5509
  • ALogP: Missing data
  • ChEMBL Molecules: Missing data
More Chemistry

Pharmacology

Drug Pricing (per unit)

United States

$78.1614 - $99.4500
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

bgb-3111

Organizations (64)

Research & Development (64)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (1)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (38)

Approved Indications (3)


 

Leukemia, Lymphocytic, Chronic, B-Cell (approved 2023)

Lymphoma, Mantle-Cell (approved 2019)

Waldenstrom Macroglobulinemia (approved 2022)

Experimental Indications - Clinical Trial Phases 1-4 (38)


 

Agammaglobulinaemia Tyrosine Kinase (Phase 1/Phase 2)

Anemia, Hemolytic, Autoimmune (Phase 2)

Anemia, Refractory (Phase 2)

Antiphospholipid Syndrome (Phase 2)

Carcinoma, Non-Small-Cell Lung (Phase 1/Phase 2)

Castleman Disease (Phase 2)

COVID-19 (Phase 2)

Healthy Volunteers (Phase 1)

Hodgkin Disease (Phase 3)

Immunoglobulin G4-Related Disease (Phase 2)

Kidney Diseases (Phase 2/Phase 3)

Leukemia (Phase 1)

Leukemia, B-Cell (Phase 3)

Leukemia, Lymphocytic, Chronic, B-Cell (Phase 2)

Leukemia, Lymphoid (Phase 2)

Leukemia, Myeloid, Acute (Phase 1/Phase 2)

Lupus Nephritis (Phase 2)

Lymphohistiocytosis, Hemophagocytic (Phase 3)

Lymphoma (Phase 2)

Lymphoma, B-Cell (Phase 2)

Lymphoma, B-Cell, Marginal Zone (Phase 3)

Lymphoma, Follicular (Phase 3)

Lymphoma, Large B-Cell, Diffuse (Phase 3)

Lymphoma, Large-Cell, Immunoblastic (Phase 2)

Lymphoma, Mantle-Cell (Phase 2)

Lymphoma, Non-Hodgkin (Phase 3)

Lymphoma, Primary Cutaneous Anaplastic Large Cell (Phase 2)

Lymphoma, T-Cell (Phase 2)

Male (Phase 1)

Melanoma (Phase 1/Phase 2)

Mutation (Phase 2)

Myelodysplastic Syndromes (Phase 1/Phase 2)

Neoplasms (Phase 2)

Neuromyelitis Optica (Phase 2)

Purpura, Thrombocytopenic, Idiopathic (Phase 2)

Therapeutics (Phase 2)

Thrombocytopenia (Phase 2)

Waldenstrom Macroglobulinemia (Phase 3)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 105
  • # of Trial Organizations: 64

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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