(RTTNews) – Biopharmaceutical company ArQule, Inc. (ARQL) announced Tuesday that the first patient has been dosed in a phase 1a/b trial with its BTK inhibitor, ARQ 531, in patients with B-cell malignancies refractory to other approved therapies.
The trial can enroll up to 120 patients. ARQ 531 is an investigational, orally bioavailable, potent and reversible inhibitor of both wild type and C481S-mutant Bruton’s tyrosine kinase or BTK.
The company said the phase 1 trial is designed to enroll patients with B-cell malignancies including B-cell lymphomas, chronic lymphocytic leukemia, and Waldenstrom’s macroglobulinemia. The phase 1a portion of the trial will be a dose escalation study open to all refractory patients, with the aim of establishing a recommended dose.
Upon completion of the phase 1a trial, the company plans to begin the phase 1b portion of trial that will consist of a number of expansion cohorts including patients with the C481S mutation who are refractory to other approved therapies. The goal of the phase 1b portion would be to establish proof of concept and early signs of activity.
B-cell malignancies, like chronic lymphocytic leukemia, Waldenstrom’s macroglobulinemia, diffuse large B-cell lymphoma and mantle cell lymphoma are driven by BTK. The only approved BTK inhibitor, ibrutinib, is irreversible and makes a covalent bond with the C481 residue of the targeted protein.
Brian Schwartz, Head of Research and Development and Chief Medical Officer at ArQule, said, “There is a clear clinical need to address the refractory population in B-cell malignancies, particularly those with the BTK C481S mutation. Our clinical strategy is to rapidly identify a recommended dose and then begin to enroll a number of expansion cohorts including one dedicated to patients with the C481S mutation.”
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