Drugs Information:
Zanubrutinib
Basic Information
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ID | DDInter1959 | |
Drug Type | small molecule | |
Molecular Formula | C27H29N5O3 | |
Molecular Weight | 471.561 | |
CAS Number | 1691249-45-2 | |
Description | 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.[L10163] Mantle cell lymphoma is an aggressive mature B-cell non-Hodgkin lymphoma that is associated with early relapse, poor clinical outcomes, and long-term survival.[A187967] BTK is an enzyme that plays a role in oncogenic signalling pathways, where it promotes the survival and proliferation of malignant B cells.[A187985] Compared to the first-generation BTK inhibitor [ibrutinib], zanubrutinib displays higher potency and selectivity for BTK with fewer off-target effects.[A187958] 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,[L10166] which measures the proportion of patients in a trial whose tumour is entirely or partially destroyed by a drug.[L10169] 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.[L39030] This indication is valid in the US, Europe, and Canada.[L39367] 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.[L39025] 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 leukaemia.[L43737] | |
ATC Classification | L01EL03 | |
IUPAC Name | (7S)-2-(4-phenoxyphenyl)-7-[1-(prop-2-enoyl)piperidin-4-yl]-4H,5H,6H,7H-pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
InChI | RNOAOAWBMHREKO-QFIPXVFZSA-N | |
Canonical SMILES | NC(=O)C1=C2NCC[C@@H](C3CCN(CC3)C(=O)C=C)N2N=C1C1=CC=C(OC2=CC=CC=C2)C=C1 | |
Useful Links | DrugBank ChemSpider BindingDB Wikipedia ChEMBL ZINC |
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Zanubrutinib
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