ASH 2024 | Updates on the Phase I trial of rocbrutinib (LP-168), a novel BTKi, for the treatment of CLL

Rocrutinib or LP-168 is a novel fourth generation covalent and non-covalent inhibitor of BTK. It’s an extremely selective inhibitor, so it has very few off-target effects, so expected to be very well tolerated. And based on preclinical data, we know that rocrutinib binds irreversibly to CLL or non-Hodgkin’s lymphoma cells that have wild type BTK or non-C41S BTK mutations and can bind reversibly or non-covalently when BTK is mutated at the cysteine 41 site. We showed some data last year showing preliminary safety and efficacy in this patient population and we extend this this year. 

For the entire cohort of CLL patients, we see a very high response rate of over 70 percent. Many patients actually remain on treatment some at two and approaching three years. We also treated a cohort of patients who had gatekeeper mutations, so T474 mutations, that are frequently seen in patients who develop resistance to pirtobrutinib, a non-covalent inhibitor. In this cohort the patients did extremely well. We had an overall response rate of 78 percent. And with a median follow up of 14 months, all of the patients remain on treatment. Safety continues to look good as well. We see very low rates of things like neutropenia and other hematologic toxicities. We’ve seen no evidence of atrial fibrillation and fairly low rates of bruising as well.

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