Zanubrutinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2019
- First approval year
- 2019
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Zanubrutinib
- Molecular weight
- 471.56
- Structure (SMILES)
- C=CC(=O)N1CCC([C@@H]2CCNc3c(C(N)=O)c(-c4ccc(Oc5ccccc5)cc4)nn32)CC1
- brukinsa
- Brukinsa
- bgb 3111
- Bgb-3111
- BGB-3111
- BGB-3111 (Arm A)
- BGB-3111 (Arm B)
- zanubrutinib
- Zanubrutinib
- zanubrutinib [INN]
- ZANUBRUTINIB [MI]
- ZANUBRUTINIB [ORANGE BOOK]
- ZANUBRUTINIB [USAN]
- Zanubrutinib [WHO-DD]
- Zanubrutinib 80 MG
- zanubrutinib inn
- zanubrutinib mi
- Zanubrutinib Oral Capsule
- zanubrutinib orange book
- zanubrutinib usan
- zanubrutinib who dd
- ATC classification codes
- L01EL03
Sources for recorded values
- CAS registry numbers
- 1691249-45-2
- ChEMBL ID
- CHEMBL3936761
- InChIKey
- RNOAOAWBMHREKO-QFIPXVFZSA-N
- PubChem compound IDs
- 135565884
- RxNorm IDs (RxCUI)
- 2262435
- FDA ingredient codes (UNII)
- AG9MHG098Z
- Applicant
- BEONE MEDICINES USA
- Approval date
- 14 Nov 2019
- Application number
- NDA213217
- Status
- Authorised
- Status date
- 22 Nov 2021
- Authorisation date
- 22 Nov 2021
- Approved indications
- Brukinsa as monotherapy is indicated for the treatment of adult patients with Waldenström’s macroglobulinaemia (WM) who have received at least one prior therapy, or in first line treatment for patients unsuitable for chemo-immunotherapy. Brukinsa as monotherapy is indicated for the treatment of adult patients with marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based therapy. Brukinsa as monotherapy is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL). Brukinsa in combination with obinutuzumab is indicated for the treatment of adult patients with refractory or relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies.
- Product number
- EMEA/H/C/004978
- Authorisation holder
- BeOne Medicines Ireland Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Waldenstrom Macroglobulinemia
European medicines record
- Patents
- 25
- Designations
- 6
- Earliest recorded loss of exclusivity
- 19 Jan 2043
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- zanubrutinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Bruton tyrosine kinase
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Median affinity
- 8.7
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase BTK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase BTK
- Protein identifier
- Q06187
Open Targets mechanisms
- Mechanism
- Tyrosine-protein kinase BTK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase BTK
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Lymphoma, Follicular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000096
- Subject identifier
- D008224
- Condition
- Paraproteinemias
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000203
- Subject identifier
- D010265
- Condition
- Lymphoma, Large B-Cell, Diffuse
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000403
- Subject identifier
- D016403
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Kidney Diseases
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Neuromyelitis Optica
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004256
- Subject identifier
- D009471
- Condition
- Leukemia, Lymphoid
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004289
- Subject identifier
- D007945
- Condition
- Lupus Nephritis
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005761
- Subject identifier
- D008181
- Condition
- Lymphoma, Non-Hodgkin
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005952
- Subject identifier
- D008228
- Condition
- Purpura, Thrombocytopenic, Idiopathic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0007160
- Subject identifier
- D016553
- Condition
- Waldenstrom Macroglobulinemia
- Highest recorded phase
- 4
- Condition identifier
- EFO:0009441
- Subject identifier
- D008258
- Condition
- Lymphoma, B-Cell, Marginal Zone
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000630
- Subject identifier
- D018442
- Condition
- Anemia, Hemolytic, Autoimmune
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001264
- Subject identifier
- D000744
- Condition
- Lymphoma, Mantle-Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:1001469
- Subject identifier
- D020522
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Lymphohistiocytosis, Hemophagocytic
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0015540
- Subject identifier
- D051359
- Condition
- Castleman Disease
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0015564
- Subject identifier
- D005871
- Condition
- Immunoglobulin G4-Related Disease
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0017287
- Subject identifier
- D000077733
- Condition
- Lymphoma, Follicular
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0018906
- Subject identifier
- D008224
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0100096
- Subject identifier
- D045169
- Condition identifier
- EFO_0000095
- Condition identifier
- EFO_0000096
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000203
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000403
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000638
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004256
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005761
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005952
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007160
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009441
- Condition identifier
- EFO_1000157
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000630
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001264
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001469
- Condition identifier
- EFO_1001938
- Highest recorded phase
- 1
- Condition identifier
- HP_0001873
- Highest recorded phase
- 2
- Condition identifier
- HP_0002098
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000432
- Condition identifier
- MONDO_0000432
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0001824
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002083
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002571
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004948
- Highest recorded phase
- 4
And 28 more, listed on the interactive page.
- Event
- anaemia
- Reports
- 15
- Reporting signal score
- 12.2271
- Event
- blood cholinesterase decreased
- Reports
- 2
- Reporting signal score
- 9.88431
- Event
- chronic lymphocytic leukaemia recurrent
- Reports
- 2
- Reporting signal score
- 7.82464
- Event
- colorectal adenoma
- Reports
- 1
- Reporting signal score
- 6.90693
- Event
- contusion
- Reports
- 7
- Reporting signal score
- 8.24316
- Event
- cytokine release syndrome
- Reports
- 3
- Reporting signal score
- 6.27437
- Event
- cytomegalovirus colitis
- Reports
- 2
- Reporting signal score
- 5.97669
- Event
- cytopenia
- Reports
- 4
- Reporting signal score
- 9.02056
- Event
- disease progression
- Reports
- 8
- Reporting signal score
- 7.73028
- Event
- double hit lymphoma
- Reports
- 1
- Reporting signal score
- 6.33185
- Event
- febrile neutropenia
- Reports
- 10
- Reporting signal score
- 13.6607
- Event
- follicular lymphoma recurrent
- Reports
- 3
- Reporting signal score
- 23.7144
- Event
- globulins decreased
- Reports
- 2
- Reporting signal score
- 9.86891
- Event
- hydroa vacciniforme
- Reports
- 1
- Reporting signal score
- 8.41072
- Event
- hyperuricaemia
- Reports
- 3
- Reporting signal score
- 8.34103
- Event
- hypoalbuminaemia
- Reports
- 3
- Reporting signal score
- 6.66132
- Event
- hypocalcaemia
- Reports
- 4
- Reporting signal score
- 6.00877
- Event
- hypokalaemia
- Reports
- 8
- Reporting signal score
- 11.4984
- Event
- hypoproteinaemia
- Reports
- 5
- Reporting signal score
- 21.0095
- Event
- lung squamous cell carcinoma metastatic
- Reports
- 1
- Reporting signal score
- 6.27127
- Event
- lymphangitis
- Reports
- 2
- Reporting signal score
- 7.62707
- Event
- lymphocyte count decreased
- Reports
- 10
- Reporting signal score
- 24.559
- Event
- marginal zone lymphoma recurrent
- Reports
- 1
- Reporting signal score
- 6.90693
- Event
- myelosuppression
- Reports
- 11
- Reporting signal score
- 34.1387
- Event
- neutropenia
- Reports
- 10
- Reporting signal score
- 7.13856
And 13 more, listed on the interactive page.
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- NCT04172246
- NCT04277637
- NCT04551963
- NCT02795182
- NCT04899453
- NCT06067048
- NCT02914938
- NCT03145064
- NCT03520920
- NCT04460248
- NCT04668365
- NCT04705129
- NCT04835870
- NCT05068440
- NCT05179733
- NCT05189197
- NCT05200312
- NCT05290090
- NCT05290337
- NCT05348213
- NCT05428670
- NCT05527912
And 57 more, listed on the interactive page.
- Dose
- 160 mg
- Route
- Oral
- How often
- Twice daily
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 2
- Polar surface area
- 102.48
- Calculated partition coefficient (ALogP)
- 4.22
- Calculated partition coefficient (XLogP)
- 3.5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 35
- Molecular formula
- C27H29N5O3
- Monoisotopic mass
- 471.22703980
- Natural product
- No
- 72579-011
- 72579-122
- Recorded assays
- 388
- Active assays
- 101
- Confirmatory
- Other
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
- Hematologic Agents
These details could not be displayed.
Related records
Trials (248)
- A Clinical Study Evaluating the Safety and Efficacy of ZRMT Regimen in the Treatment of PCNSL
- A HR20031 BE Study on Healthy Subjects
- A Multicenter, Prospective, Phase II Study of Zanubrutinib for Maintenance in Patients With Mantle Cell Lymphoma
- A Pharmacokinetic Study to Assess Drug-drug Interaction Between Zanubrutinib and a Cocktail of Substrates in Healthy Subjects
- A Phase 2 Clinical Trial to Evaluate Zanubrutinib Combined With BR (Bendamustine/Rituximab) Regimen in Subjects With Newly-diagnosed Waldenström's Macroglobulinemia
- A Phase 2 Trial of Mosunetuzumab and Zanubrutinib for Patients With Relapsed/Refractory Marginal Zone Lymphoma
- A Phase 2 Trial Of The Combination Of Zanubrutinib, Sonrotoclax, And Obinutuzumab For Patients With Treatment-Naïve Chronic Lymphocytic Leukemia
- A Phase I Study to Evaluate Safety, Tolerability, and Immunogenicity of a PIKA COVID-19 Vaccine in Healthy Individuals
- A Phase II Clinical Study of Zanubrutinib Combined With Four Cycles of CD20 Monoclonal Antibody and Reduced-Dose Bendamustine in the Treatment of Untreated Waldenström Macroglobulinemia
- A Phase II Study of Rituximab, Chidamide, Zanubrutinib-induced and CHOP Therapy
- A Phase II Study of Zanubrutinib, Lenalidomide Plus R-CHOP as the First-line Treatment for Diffused Large B-cell Lymphoma
- A Phase II Study of Ziv-aflibercept in Combination With Capecitabine/Oxaliplatin (XELOX) Chemotherapy in the Front-Line Treatment of Patients With Metastatic Colorectal Cancer
- A Phase III Transition Study of DRL Rituximab to Reference Medicinal Products
- A Prospective, One-arm and Open Clinical Study of Zanubrutinib in the Treatment of Immune Thrombocytopenia
- A Randomized Phase II Study Of Bruton Tyrosine Kinase Inhibitor With Or Without Venetoclax In Veterans With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
- A Single-Arm, Expanded Access Study of Zanubrutinib in Participants With B-cell Malignancies
- A Single-arm, Single-center, Open-label Phase II Study of Zanubrutinib Combined With R-CHOP/R-DHAP in Newly Diagnosed Mantle CellLymphoma Patients
- A Study Comparing BGB-3111 and Ibrutinib in Participants With Waldenström's Macroglobulinemia (WM)
- A Study Comparing Obinutuzumab and BGB-3111 Versus Obinutuzumab Alone in Treating R/R Follicular Lymphoma
- A Study Comparing Zanubrutinib With Bendamustine Plus Rituximab in Participants With Previously Untreated CLL or SLL
Approved for (4)
In development for (21)
- Autoimmune hemolytic anemia Phase 2
- Autoimmune thrombocytopenic purpura Phase 2
- B-cell chronic lymphocytic leukemia Phase 3
- B-cell non-Hodgkin lymphoma Phase 1
- Castleman disease Phase 2
- COVID-19 Phase 2
- Diffuse large B-cell lymphoma Phase 3
- Follicular lymphoma Phase 3
- Hemophagocytic syndrome Phase 3
- Immunoglobulin G4-related sclerosing disease Phase 2
- Kidney disorder Phase 2
- Leukemia Phase 1
- Lupus nephritis Phase 2
- Lymphoid leukemia Phase 2
- Lymphoma Phase 2
- Marginal zone lymphoma Phase 2
- Monoclonal gammopathy Phase 2
- Neoplasm of mature B-cells Phase 3
- Neuromyelitis optica Phase 2
- Non-Hodgkin lymphoma Phase 3
Other linked conditions (1)
- Lymphoplasmacytic lymphoma
Targets (1)
- BTK Tyrosine-protein kinase BTK inhibitor