ARIAD Pharmaceuticals, Inc. (NASDAQ: ARIA) today announced that the scientific journal, Cancer Cell, has published a comprehensive paper describing the design and preclinical characterization of AP24534, ARIAD’s investigational, multi-targeted kinase inhibitor. The paper, “AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance,” is co-authored by scientists from ARIAD, and collaborating investigators from the Oregon Health & Science University Knight Cancer Institute and the Howard Hughes Medical Institute.
The publication describes for the first time the chemical structure of AP24534 and its activity against all known BCR-ABL mutants, including the T315I mutant that is resistant to currently marketed therapies for chronic myeloid leukemia (CML). The paper provides a comprehensive description of the activity of AP24534 in a range of established cell-based and animal models of CML. AP24534 was discovered by ARIAD scientists and is now in a Phase 1 dose-escalating clinical trial in patients with refractory CML, acute myeloid leukemia (AML) and other hematological malignancies.
“These data support the ongoing clinical study of AP24534 to develop a potential much-needed treatment option for patients with resistant mutations such as T315I, that could complement the currently available tyrosine kinase inhibitors,” said Timothy P. Clackson, Ph.D., senior vice president and chief scientific officer at ARIAD and senior author of the paper. “Longer term, a pan-BCR-ABL inhibitor such as AP24534 may offer important advantages by minimizing the development of mutation-based drug resistance.”