zanubrutinib   Click here for help

GtoPdb Ligand ID: 9861

Synonyms: BGB-3111 | BGB3111 | Brukinsa® | compound 27b [US9447106]
Approved drug Immunopharmacology Ligand
zanubrutinib is an approved drug (FDA (2019), EMA (2021))
Compound class: Synthetic organic
Comment: Zanubrutinib (BGB-3111) is a potent, selective and irreversible BTK inhibitor that was developed by BeiGene for utility in the treatment of B cell cancers, such as non-Hodgkin's lymphoma and chronic lymphocytic leukemia (CLL) [1,4].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 7
Topological polar surface area 102.48
Molecular weight 471.23
XLogP 4.5
No. Lipinski's rules broken 0
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Canonical SMILES C=CC(=O)N1CCC(CC1)[C@@H]1CCNc2n1nc(c2C(=O)N)c1ccc(cc1)Oc1ccccc1
Isomeric SMILES C=CC(=O)N1CCC(CC1)[C@@H]1CCNc2n1nc(c2C(=O)N)c1ccc(cc1)Oc1ccccc1
InChI InChI=1S/C27H29N5O3/c1-2-23(33)31-16-13-18(14-17-31)22-12-15-29-27-24(26(28)34)25(30-32(22)27)19-8-10-21(11-9-19)35-20-6-4-3-5-7-20/h2-11,18,22,29H,1,12-17H2,(H2,28,34)/t22-/m0/s1
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Summary of Clinical Use Click here for help
Zanubrutinib was evaluated for efficacy in a large number of clinical trials, across a range of hematological cancers. Click here to link to's full list of zanubrutinib/BGB-3111 studies.
The FDA first approved zanubrutinib in November 2019 for the treatment of mantle cell lymphoma (MCL; in adult patients who have received at least one prior therapy). In June 2020, the drug was approved in China for the treatment of adult patients with CLL/SLL who have received at least one prior therapy, and for patients with MCL who have received at least one prior therapy. In the EU, zanubrutinib holds orphan designation for lymphoplasmacytic lymphoma, which was granted in May 2019. In April 2021, the The FDA accepted a supplemental new drug application (sNDA) for zanubrutinib for the treatment of adults with Waldenström macroglobulinemia, and approval followed in August that year. FDA approval was expanded in early 2023, to include treatment of CLL, based on evidence from the phase 3 SEQUOIA study (NCT03336333) [2-3]. A further expansion by the FDA in March 2024 added the treatment of relapsed/refractory follicular lymphoma to zanubrutinib's indication list.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03053440 A Study Comparing BGB-3111 and Ibrutinib in Participants With Waldenström's Macroglobulinemia (WM) Phase 3 Interventional BeiGene
NCT03332173 Study of BTK Inhibitor BGB-3111 in Chinese Participants With Relapsed/Refractory Waldenström's Macroglobulinemia (WM) Phase 2 Interventional BeiGene
NCT03336333 A Study Comparing Zanubrutinib With Bendamustine Plus Rituximab in Participants With Previously Untreated CLL or SLL Phase 3 Interventional BeiGene