UVI5008: the first reversible, non-covalent Bruton's tyrosine kinase epi-inhibitor for B-cell malignancies - PubMed
9 hours ago
- #epi-inhibitor
- #CLL treatment
- #BTK inhibitor
- UVI5008 is the first reversible, non-covalent Bruton's tyrosine kinase (BTK) epi-inhibitor for B-cell malignancies.
- It targets both wild-type BTK and the C481S mutated BTK isoform, addressing resistance in chronic lymphocytic leukemia (CLL).
- UVI5008 shows superior efficacy compared to ibrutinib by reducing BTK protein levels and downstream signaling, leading to increased apoptosis.
- The inhibitor has demonstrated potent anti-tumor efficacy in relapsed/refractory CLL cells, including those with the C481S BTK mutation.
- In vivo and ex vivo studies support UVI5008's potential as a promising therapeutic agent for B-cell malignancies.