Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials.[A32299] Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval;[L12228] however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US.[L45894] Ibrutinib was approved by the EMA in October 2014 [L45884] and by Health Canada in November 2014.[L45889] It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenstr?m's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017.[L12228] Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.[L43020]
Ibrutinib is indicated for the treatment of the following conditions. **Chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL)** - In the US, it is used in adult patients with or without 17p deletion.[L42980, L45884] - In Europe and Canada, it is used as a single agent or combined with [rituximab], [obinutuzumab], or [venetoclax] in previously untreated CLL patients. In patients who have received at least one prior therapy, it is used as a single agent or in combination with [bendamustine] and [rituximab].[L45884, L45889] **Waldenstr?m's macroglobulinemia** - It is used alone [L42980, L45884, L45889] or with [rituximab].[L45884, L45889] - In Europe, it is approved for patients who have received at least one prior therapy or in first-line treatment for patients unsuitable for chemoimmunotherapy.[L45884] **Chronic graft-versus-host disease (cGVHD)** - In the US, it is approved in patients aged one year and older after the prior failure of one or more lines of systemic therapy.[L42980] - In Canada, it is approved in adults with steroid-dependent or refractory cGVHD.[L45889] **Mantle cell lymphoma (MCL)** - In Europe and Canada, ibrutinib is also indicated to treat relapsed or refractory MCL in adults.[L45884, L45889] **Marginal zone lymphoma (MZL)** - In Canada, it is approved for adults who require systemic therapy and have received at least one prior anti-CD20-based therapy.[L45889]
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