Synonyms: BTK inhibitor 16 | Jaypirca® | LOXO-305 | LOXO305 | MCL-133 | MCL133 | RXC005
pirtobrutinib is an approved drug (FDA & EMA (2023))
Compound class:
Synthetic organic
Comment: Pirtobrutinib (LOXO-305, MCL-133) is a selective and reversible (non-covalent), oral Bruton's tyrosine kinase (BTK) inhibitor that was originally developed by LOXO oncology (now Lilly Oncology) for potential to treat B cell malignancies [3,5]. It binds within the BTK kinase pocket but its interaction does not rely on the C481 residue that is essential for the activity of earlier irreversible BTK inhibitors (ibrutinib, acalabrutinib, and zanubrutinib). Therefore, it is expected to be active in cancers with wild type BTK or with C481 resistance mutations.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Pirtobrutinib (LOXO-305) was progressed to clinical trial to determine efficacy in B cell malignancies. The FDA first approved its use in January 2023 [6], for the treatment of relapsed/refractory mantle cell lymphoma. EMA authorisation for this indication followed in April of the same year. FDA approval was expanded in late 2023 to include treatmant of chronic lymphocytic leukemia or small lymphocytic lymphoma (CLL/SLL; previously treated with ≥2 drugs, including a BTK inhibitor and a BCL-2 inhibitor). |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03740529 | A Study of Oral LOXO-305 in Patients With Previously Treated CLL/SLL or NHL | Phase 1/Phase 2 Interventional | Eli Lilly and Company | This study found that pirtobrutinib was safe and active in multiple B cell malignancies. It was effective in patients who had previously received treatment with covalent BTK inhibitors. | 4,7 |