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Zanubrutinib

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Also known as Bgb-3111BrukinsaUS9447106, 27b (peak 2)ZanubrutinlbZanubrutinib(S)-Zanubrutinib

Summary

Zanubrutinib (CHEMBL3936761) is an approved small molecule (ATC L01EL03) targeting BTK; indicated across 23 conditions including waldenstrom macroglobulinemia and mantle cell lymphoma.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EL03
  • Targets: 1 (BTK)
  • Indications: 23 conditions
  • Clinical trials: 162
  • Chemistry: 471.5 Da · C27H29N5O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3936761
NameZanubrutinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID135565884
ATCL01EL03
Molecular formulaC27H29N5O3
Molecular weight471.5
InChIKeyRNOAOAWBMHREKO-QFIPXVFZSA-N

SMILES: C=CC(=O)N1CCC(CC1)[C@@H]2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N

IUPAC name: (7S)-2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide

Also known as: Bgb-3111, BGB-3111, Brukinsa, Zanubrutinib, US9447106, 27b (peak 2), ZANUBRUTINIB, Zanubrutinlb, Zanubrutinib; Brukinsa, (S)-Zanubrutinib

Patent coverage: 1,037 distinct patent families (2,484 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
BTKBruton tyrosine kinaseInhibition8.70.7%Q06187

Broader ChEMBL bioactivity targets: 19 (assay-derived). Sample: Receptor tyrosine-protein kinase erbB-2, Epidermal growth factor receptor, Tyrosine-protein kinase JAK3, Tyrosine-protein kinase Blk, Tyrosine-protein kinase Lck, Tyrosine-protein kinase ITK/TSK, Receptor tyrosine-protein kinase erbB-4, Platelet glycoprotein VI, Cytochrome P450 2C9, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 79 potent at pChembl ≥ 5 of 83 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
BTK9.52IC500.3nMCHEMBL_ACT_19305904
BTK9.52IC500.3nMCHEMBL_ACT_24788459
BTK9.52IC500.3nMCHEMBL_ACT_24954234
BTK9.52IC500.3nMCHEMBL_ACT_25066888
BTK9.48IC500.33nMCHEMBL_ACT_26868700
BTK9.3IC500.5nMCHEMBL_ACT_24703138
BTK9.3IC500.5nMCHEMBL_ACT_24805897
BMX9.21IC500.62nMCHEMBL_ACT_19306062
BMX9.21IC500.62nMCHEMBL_ACT_24954236
BTK9.04IC500.92nMCHEMBL_ACT_19306050
BLK8.95IC501.13nMCHEMBL_ACT_19306060
BLK8.95IC501.13nMCHEMBL_ACT_24954235
ERBB48.8IC501.58nMCHEMBL_ACT_19306066
ERBB48.8IC501.58nMCHEMBL_ACT_24954237
TEC8.77IC501.7nMCHEMBL_ACT_25066953
BTK8.74IC501.8nMCHEMBL_ACT_19305855
BTK8.74IC501.8nMCHEMBL_ACT_24872439
BTK8.74IC501.8nMCHEMBL_ACT_24953974
BTK8.74IC501.8nMCHEMBL_ACT_25066994
BTK8.7IC502nMCHEMBL_ACT_17795785
TEC8.7IC502nMCHEMBL_ACT_19306054
TEC8.7IC502nMCHEMBL_ACT_24958604
BTK8.66IC502.2nMCHEMBL_ACT_23299051
BTK8.66IC502.2nMCHEMBL_ACT_23309949
EGFR8.62IC502.4nMCHEMBL_ACT_24805906
BTK8.62EC502.4nMCHEMBL_ACT_24805909
EGFR8.59IC502.6nMCHEMBL_ACT_19305953
EGFR8.59IC502.6nMCHEMBL_ACT_24958595
EGFR8.59IC502.6nMCHEMBL_ACT_25066924
TXK8.53IC502.95nMCHEMBL_ACT_19306074

Target pathways

Aggregated over 1 target gene(s): BTK.

Top Reactome pathways

45 total, by targets touching each:

PathwayTargetsGenes
ER-Phagosome pathway1BTK
Antigen processing-Cross presentation1BTK
Adaptive Immune System1BTK
Signal Transduction1BTK
Disease1BTK
Toll Like Receptor 4 (TLR4) Cascade1BTK
MyD88:MAL(TIRAP) cascade initiated on plasma membrane1BTK
Toll Like Receptor TLR1:TLR2 Cascade1BTK
Toll Like Receptor TLR6:TLR2 Cascade1BTK
Innate Immune System1BTK
Immune System1BTK
Toll-like Receptor Cascades1BTK
Toll Like Receptor 2 (TLR2) Cascade1BTK
Signaling by Rho GTPases1BTK
RHO GTPase Effectors1BTK
Fcgamma receptor (FCGR) dependent phagocytosis1BTK
Regulation of actin dynamics for phagocytic cup formation1BTK
DAP12 interactions1BTK
DAP12 signaling1BTK
Fc epsilon receptor (FCERI) signaling1BTK
FCERI mediated Ca+2 mobilization1BTK
Signaling by GPCR1BTK
GPCR downstream signalling1BTK
G-protein beta:gamma signalling1BTK
G alpha (q) signalling events1BTK
G alpha (12/13) signalling events1BTK
Diseases of Immune System1BTK
Diseases associated with the TLR signaling cascade1BTK
MyD88 deficiency (TLR2/4)1BTK
IRAK4 deficiency (TLR2/4)1BTK

Dominant GO biological processes

GO termTargets
neutrophil homeostasis1
positive regulation of type III hypersensitivity1
positive regulation of type I hypersensitivity1
adaptive immune response1
B cell affinity maturation1
histamine secretion by mast cell1
positive regulation of immunoglobulin production1
regulation of B cell cytokine production1
MyD88-dependent toll-like receptor signaling pathway1
regulation of B cell apoptotic process1
mesoderm development1
peptidyl-tyrosine phosphorylation1
calcium-mediated signaling1
proteoglycan catabolic process1
negative regulation of B cell proliferation1

Indications & clinical

Indications

23 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
Waldenstrom macroglobulinemia4MONDO:0100280EFO:0009441
mantle cell lymphoma4MONDO:0018876EFO:1001469
neoplasm4MONDO:0005070EFO:0000616
B-cell chronic lymphocytic leukemia3MONDO:0004948EFO:0000095
neoplasm of mature B-cells3MONDO:0004949EFO:0000096
diffuse large B-cell lymphoma3MONDO:0018905EFO:0000403
follicular lymphoma3MONDO:0018906MONDO:0018906
non-Hodgkin lymphoma3MONDO:0018908EFO:0005952
lymphoma2MONDO:0005062EFO:0000574
lupus nephritis2MONDO:0005556EFO:0005761
Castleman disease2MONDO:0015564MONDO:0015564
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
neuromyelitis optica2MONDO:0019100EFO:0004256
autoimmune thrombocytopenic purpura2MONDO:0008558EFO:0007160
kidney disorder2MONDO:0005240EFO:0003086
marginal zone lymphoma2MONDO:0017604EFO:1000630
autoimmune hemolytic anemia2MONDO:0020108EFO:1001264
monoclonal gammopathy2MONDO:0004960EFO:0000203
lymphoid leukemia2MONDO:0005402EFO:0004289
leukemia1MONDO:0005059EFO:0000565

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 162.

Phase distribution

PhaseTrials
PHASE2101
PHASE124
PHASE316
Not specified10
PHASE1/PHASE28
PHASE42
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07169331PHASE4RECRUITINGA Study to Evaluate the Efficacy and Safety of Zanubrutinib in Chinese Adults With Treatment-Naive Waldenström Macroglobulinemia
NCT07270835PHASE4RECRUITINGZanubrutinib Combined With Rituximab in the Treatment of Secondary HLH in B-cell Lymphoma
NCT03336333PHASE3ACTIVE_NOT_RECRUITINGA Study Comparing Zanubrutinib With Bendamustine Plus Rituximab in Participants With Previously Untreated CLL or SLL
NCT04002297PHASE3ACTIVE_NOT_RECRUITINGA Study to Investigate the Efficacy of Zanubrutinib Plus Rituximab Compared With Bendamustine Plus Rituximab in Adults With Previously Untreated Mantle Cell Lymphoma Who Are Ineligible for Stem Cell Transplantation
NCT04170283PHASE3ACTIVE_NOT_RECRUITINGLong-term Extension Study of Zanubrutinib (BGB-3111) Regimens in Participants With B-cell Malignancies
NCT04662255PHASE3ACTIVE_NOT_RECRUITINGStudy of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)
NCT05100862PHASE3RECRUITINGA Study of Zanubrutinib Plus Anti-CD20 Versus Lenalidomide Plus Rituximab in Participants With Relapsed/Refractory Follicular or Marginal Zone Lymphoma
NCT05707377PHASE2/PHASE3ACTIVE_NOT_RECRUITINGA Study to Examine the Efficacy and Safety of Zanubrutinib Given to Adults With Primary Membranous Nephropathy
NCT05735834PHASE3ACTIVE_NOT_RECRUITINGComparison Between Rituximab Plus Zanubrutinib Versus Rituximab Monotherapy in Untreated SMZL Patients
NCT05976763PHASE3RECRUITINGTesting Continuous Versus Intermittent Treatment With the Study Drug Zanubrutinib for Older Patients With Previously Untreated Mantle Cell Lymphoma
NCT06073821PHASE3ACTIVE_NOT_RECRUITINGStudy of Sonrotoclax (BGB-11417) Plus Zanubrutinib (BGB-3111) Compared With Venetoclax Plus Obinutuzumab in Participants With Chronic Lymphocytic Leukemia (CLL)
NCT06742996PHASE3RECRUITINGA Study to Investigate the Efficacy and Safety of Sonrotoclax Plus Zanubrutinib Compared With Placebo Plus Zanubrutinib in Adults With Relapsed/Refractory Mantle Cell Lymphoma (CELESTIAL-RRMCL)
NCT07277231PHASE3RECRUITINGA Study to Investigate Sonrotoclax (BGB-11417) Plus Zanubrutinib (BGB-3111) Compared With Venetoclax Plus Acalabrutinib in Adults With Previously Untreated Chronic Lymphocytic Leukemia
NCT07321652PHASE3NOT_YET_RECRUITINGTesting the Addition of Anti-Cancer Drug Sonrotoclax, to the Standard Treatment Zanubrutinib, for Previously Untreated CLL/SLL
NCT07377578PHASE3RECRUITINGA Study of Rocbrutinib Versus Investigator’s Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma
NCT03053440PHASE3COMPLETEDA Study Comparing BGB-3111 and Ibrutinib in Participants With Waldenström’s Macroglobulinemia (WM)
NCT03734016PHASE3COMPLETEDA Study of Zanubrutinib (BGB-3111) Versus Ibrutinib in Participants With Relapsed/Refractory Chronic Lymphocytic Leukemia
NCT05164770PHASE3UNKNOWNStudy of Zanubrutinib, Rituximab and Combination Chemotherapy in Newly-diagnosed Aggressive B-cell Non-Hodgkin Lymphoma
NCT05320575PHASE3COMPLETEDZanubrutinib for HLH
NCT03824483PHASE2RECRUITINGStudy of Zanubrutinib, Obinutuzumab, and Venetoclax in Patients With Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Leukemia (SLL)
NCT04271956PHASE2RECRUITINGEfficacy and Safety of Zanubrutinib Plus Tislelizumab Treatment with or Without Sonrotoclax for Patients with Richter Transformation
NCT04458610PHASE2ACTIVE_NOT_RECRUITINGZanubrutinib and Rituximab for the Treatment of Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT04515238PHASE2ACTIVE_NOT_RECRUITINGSequential Regimen of Bendamustine Followed by Obinutuzumab (GA101), Zanubrutinib (BGB-3111) and Venetoclax (ABT-199) in Patients With Relapsed/Refractory CLL
NCT04624958PHASE2ACTIVE_NOT_RECRUITINGZanubrutinib and Rituximab Followed by R-DHAOx Then Maintenance with Zanubrutinib for Newly-Diagnosed MCL
NCT04840602PHASE2RECRUITINGTesting the Combination of Venetoclax and Rituximab, in Comparison to the Usual Treatment (Ibrutinib Plus Rituximab or Zanubrutinib Alone) for Waldenstrom’s Macroglobulinemia/Lymphoplasmacytic Lymphoma
NCT05168930PHASE2RECRUITINGZanubrutinib and Venetoclax in CLL (ZANU-VEN)
NCT05189197PHASE2ACTIVE_NOT_RECRUITINGA Study to Evaluate Efficacy and Safety of Zanubrutinib With R-CHOP in Newly Diagnosed Non-GCB DLBCL Patients With Double Expression
NCT05199909PHASE2RECRUITINGSafety and Efficacy of Zanubrutinib in the Treatment of Antiphospholipid Syndrome With Secondary Thrombocytopenia
NCT05202782PHASE2ACTIVE_NOT_RECRUITINGZanubrutinib and CAR T-cell Therapy for the Treatment of Recurrent or Refractory Aggressive B-cell Non-Hodgkin’s Lymphoma or Transformed Indolent B-cell Lymphoma
NCT05214391PHASE2RECRUITINGA Prospective, One-arm and Open Clinical Study of Zanubrutinib in the Treatment of Immune Thrombocytopenia
NCT05369364PHASE2NOT_YET_RECRUITINGThe Combination of Zanubrutinib and High-dose Dexamethasone as First-line Treatment in Adult Immune Thrombocytopenia
NCT05389293PHASE2RECRUITINGA Study of Mosunetuzumab Alone or With Zanubrutinib in People With Follicular Lymphoma
NCT05596097PHASE2NOT_YET_RECRUITINGZanubrutinib in Maintenance Therapy of DLBCL Patients With Initial Remission
NCT05635162PHASE2RECRUITINGZanubrutinib Plus Rituximab for Patients With Indolent Mantle Cell Lymphoma
NCT05650723PHASE2ACTIVE_NOT_RECRUITINGZanubrutinib and Venetoclax as Initial Therapy for Chronic Lymphocytic Leukemia (CLL) With Response-based Obinutuzumab
NCT05681195PHASE2RECRUITINGZanubrutinib With Pemetrexed to Treat Relapsed/Refractory Primary and Secondary Central Nervous System (CNS) Lymphomas
NCT05718869PHASE2ACTIVE_NOT_RECRUITINGTafasitamab and Zanubrutinib for the Treatment of Patients With Newly Diagnosed Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma, TaZA CLL Study
NCT05873712PHASE2RECRUITINGZanubrutinib and Lisocabtagene Maraleucel for the Treatment of Richter’s Syndrome
NCT05890352PHASE2RECRUITINGStudy Adding Drugs to Usual Treatment for Large B-Cell Lymphoma That Returned or Did Not Respond to Treatment
NCT05939037PHASE2ACTIVE_NOT_RECRUITINGZanubrutinib Treatment in Patients With IgM Monoclonal Gammopathy and Antri-MAG Related Polyneuropathy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

80 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)BTK
RITLECITINIBChEMBL + PubChemPhase 4 (approved)BTK
ACALABRUTINIBChEMBLPhase 4 (approved)BTK
BOSUTINIBChEMBLPhase 4 (approved)BTK
BRIGATINIBChEMBLPhase 4 (approved)BTK
CERITINIBChEMBLPhase 4 (approved)BTK
DASATINIBChEMBLPhase 4 (approved)BTK
ENTRECTINIBChEMBLPhase 4 (approved)BTK
FEDRATINIBChEMBLPhase 4 (approved)BTK
FUTIBATINIBChEMBLPhase 4 (approved)BTK
IBRUTINIBChEMBLPhase 4 (approved)BTK
MITOXANTRONEChEMBLPhase 4 (approved)BTK
NERATINIBChEMBLPhase 4 (approved)BTK
NINTEDANIBChEMBLPhase 4 (approved)BTK
OLMUTINIBChEMBLPhase 4 (approved)BTK
OSIMERTINIBChEMBLPhase 4 (approved)BTK
PIRTOBRUTINIBChEMBLPhase 4 (approved)BTK
PONATINIBChEMBLPhase 4 (approved)BTK
SUNITINIBChEMBLPhase 4 (approved)BTK
TIRABRUTINIBChEMBLPhase 4 (approved)BTK
VANDETANIBChEMBLPhase 4 (approved)BTK
ABIVERTINIBChEMBLPhase 3BTK
ALISERTIBChEMBLPhase 3BTK
CANERTINIBChEMBLPhase 3BTK
CEDIRANIBChEMBLPhase 3BTK
DOVITINIBChEMBLPhase 3BTK
ENTOSPLETINIBChEMBLPhase 3BTK
EVOBRUTINIBChEMBLPhase 3BTK
FENEBRUTINIBChEMBLPhase 3BTK
LESTAURTINIBChEMBLPhase 3BTK
NEMTABRUTINIBChEMBLPhase 3BTK
ORELABRUTINIBChEMBLPhase 3BTK
POZIOTINIBChEMBLPhase 3BTK
PYROTINIBChEMBLPhase 3BTK
REMIBRUTINIBChEMBLPhase 3BTK
RILZABRUTINIBChEMBLPhase 3BTK
ROCILETINIBChEMBLPhase 3BTK
SARACATINIBChEMBLPhase 3BTK
TESEVATINIBChEMBLPhase 3BTK
TOLEBRUTINIBChEMBLPhase 3BTK
APITOLISIBChEMBLPhase 2BTK
AT-9283ChEMBLPhase 2BTK
ATUZABRUTINIBChEMBLPhase 2BTK
BIIB-091ChEMBLPhase 2BTK
BMS-754807ChEMBLPhase 2BTK
BMS-919373ChEMBLPhase 2BTK
BMS-986142ChEMBLPhase 2BTK
BRANEBRUTINIBChEMBLPhase 2BTK
CENISERTIBChEMBLPhase 2BTK
CEP-11981ChEMBLPhase 2BTK
DANUSERTIBChEMBLPhase 2BTK
DEFOSBARASERTIBChEMBLPhase 2BTK
EDRALBRUTINIBChEMBLPhase 2BTK
ELSUBRUTINIBChEMBLPhase 2BTK
FORETINIBChEMBLPhase 2BTK
ILORASERTIBChEMBLPhase 2BTK
MILREBRUTINIBChEMBLPhase 2BTK
PELITINIBChEMBLPhase 2BTK
POSELTINIBChEMBLPhase 2BTK
R-406ChEMBLPhase 2BTK

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot