Study Safety and Preliminary Efficacy of DCC-2036 in Patients With Leukemias

Rationale: DCC-2036 is a potent broad spectrum inhibitor of BCR-ABL kinase. Inhibition of
BCR-ABL has been validated for effective treatment of chronic myelogenous leukemia and
Philadelphia chromosome positive (Ph+) acute lymphoblastic leukemia. The emergence of
mutant forms of BCR-ABL which resist inhibition by imatinib, dasatinib, and nilotinib is
associated with loss of efficacy in treatment of the disease. DCC-2036 is a potent inhibitor
of resistant mutants of BCR-ABL including the T315I mutation, and would therefore be
expected to effectively treat patients who fail to respond to other BCR-ABL inhibitors.

Purpose: to assess the safety and tolerability in patients after continuous administration
of DCC-2036 and to determine recommended doses for the conduct of a Phase 2 efficacy trial.