Overview
Zanubrutinib is a novel Bruton's tyrosine kinase (BTK) inhibitor used for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy. Mantle cell lymphoma is an aggressive mature B-cell non-Hodgkin lymphoma associated with early relapse, poor clinical outcomes, and long-term survival. BTK is an enzyme that plays a role in oncogenic signalling pathways, promoting the survival and proliferation of malignant B cells. Compared to the first-generation BTK inhibitor ibrutinib, zanubrutinib displays higher potency and selectivity for BTK with fewer off-target effects. Due to this enhanced selectivity towards BTK, zanubrutinib belongs to the second-generation BTK inhibitor drug group that also includes acalabrutinib, which was approved by the FDA in 2017. Zanubrutinib was granted accelerated approval by the FDA in November 2019 based on clinical trial results that demonstrated an 84% overall response rate from zanubrutinib therapy in patients with MCL, which measures the proportion of patients in a trial whose tumour is entirely or partially destroyed by a drug. It is currently marketed under the trade name BRUKINSA™ and is available as oral capsules. In August 2021, the FDA granted accelerated approval to zanubrutinib for the treatment of adults with Waldenström’s macroglobulinemia. This indication is valid in the US, Europe, and Canada. In September 2021, zanubrutinib was granted another accelerated approval for the treatment of relapsed or refractory marginal zone lymphoma who have received at least one anti-CD20-based regimen. In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended zanubrutinib be granted marketing authorization for the treatment of chronic lymphocytic leukemia.
Background
Zanubrutinib is a novel Bruton's tyrosine kinase (BTK) inhibitor used for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy. Mantle cell lymphoma is an aggressive mature B-cell non-Hodgkin lymphoma associated with early relapse, poor clinical outcomes, and long-term survival. BTK is an enzyme that plays a role in oncogenic signalling pathways, promoting the survival and proliferation of malignant B cells. Compared to the first-generation BTK inhibitor ibrutinib, zanubrutinib displays higher potency and selectivity for BTK with fewer off-target effects. Due to this enhanced selectivity towards BTK, zanubrutinib belongs to the second-generation BTK inhibitor drug group that also includes acalabrutinib, which was approved by the FDA in 2017. Zanubrutinib was granted accelerated approval by the FDA in November 2019 based on clinical trial results that demonstrated an 84% overall response rate from zanubrutinib therapy in patients with MCL, which measures the proportion of patients in a trial whose tumour is entirely or partially destroyed by a drug. It is currently marketed under the trade name BRUKINSA™ and is available as oral capsules. In August 2021, the FDA granted accelerated approval to zanubrutinib for the treatment of adults with Waldenström’s macroglobulinemia. This indication is valid in the US, Europe, and Canada. In September 2021, zanubrutinib was granted another accelerated approval for the treatment of relapsed or refractory marginal zone lymphoma who have received at least one anti-CD20-based regimen. In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended zanubrutinib be granted marketing authorization for the treatment of chronic lymphocytic leukemia.
Indication
Zanubrutinib is indicated for the treatment of:
Associated Conditions
- Chronic Lymphocytic Leukemia
- Mantle Cell Lymphoma (MCL)
- Refractory Marginal Zone Lymphoma
- Relapsed Marginal Zone Lymphoma
- Small Lymphocytic Lymphoma
- Waldenström's Macroglobulinemia (WM)
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/10 | Phase 2 | Not yet recruiting | Shanghai Zhongshan Hospital | ||
2025/06/04 | Phase 2 | Not yet recruiting | |||
2025/05/15 | Phase 2 | Not yet recruiting | |||
2025/04/24 | Not Applicable | Not yet recruiting | |||
2025/03/05 | Phase 1 | Not yet recruiting | City of Hope Medical Center | ||
2025/03/03 | Phase 2 | Not yet recruiting | Christine Ryan | ||
2025/02/27 | Phase 2 | Not yet recruiting | |||
2025/02/26 | Phase 2 | Recruiting | |||
2025/02/21 | Phase 2 | Recruiting | |||
2025/02/13 | Phase 1 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| BEIGENE USA, INC. | 72579-011 | ORAL | 80 mg in 1 1 | 3/8/2024 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
BeOne Medicines Ireland Limited,10 Earlsfort Terrace,Dublin 2,D02 T380,Co. Dublin,Ireland | Authorised | 11/22/2021 | |
Authorised | 11/22/2021 | ||
Authorised | 11/22/2021 | ||
BeOne Medicines Ireland Limited,10 Earlsfort Terrace,Dublin 2,D02 T380,Co. Dublin,Ireland | Authorised | 11/22/2021 | |
Authorised | 11/22/2021 | ||
Authorised | 11/22/2021 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| BRUKINSA™ CAPSULE 80MG | SIN16341P | CAPSULE | 80mg | 10/1/2021 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Zanubrutinib Capsules | 国药准字H20200005 | 化学药品 | 胶囊剂 | 6/2/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| BRUKINSA zanubrutinib 80 mg capsule bottle | 338475 | Medicine | A | 10/7/2021 |