DCC-2036 (Rebastinib) CML Chronic Myeloid Leukemia
"DCC-2036 is a new tyrosine kinase inhibitor that overcomes imatinib resistance by binding to a different domain on the BCR-ABL protein thus avoiding interaction with the mutated regions most commonly associated with resistance. DCC-2036 retained full potency against the T315I mutant kinase in preclinical studies and therefore warrants testing in patients who have failed prior TKI therapies or who have the T315I mutation and are diagnosed with either Ph+ CML or Ph+ ALL. DCC-2036 is also active against wild type BCR-ABL and other mutants commonly seen after imatinib failure."
Extract from MD Anderson Cancer Center
"Although clinical activity was observed, clinical benefit was insufficient to justify continued development in chronic or acute myeloid leukemia."
Extract of https://haematologica.org/article/view/8003
ARTICLES
Phase 1 Dose-Finding Study Of Rebastinib (DCC-2036) In Patients With Relapsed Chronic Myeloid Leukemia And Acute Myeloid Leukemia
March 2017, Haematologica
Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia
December 7, 2016, PubMed
A Phase 1 Study of DCC-2036, a Novel Oral Inhibitor of BCR-ABL Kinase, in Patients with Philadelphia Chromosome Positive (Ph+) Leukemias Including Patients with T315I Mutation
December 12, 2011, ASH 2011
The Gatekeeper T315I Versus the Switch-Control Inhibitor DCC-2036: The Last Title Fight in CML?
July 1, 2011, The Hematologist
New Drug Shows Potential for Treatment-Resistant Leukemia
April 13, 2011, Science Daily
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Apr 12, 2011, Cancer Cell
Phase 1 Dose-Finding Study Of Rebastinib (DCC-2036) In Patients With Relapsed Chronic Myeloid Leukemia And Acute Myeloid Leukemia
March 2017, Haematologica
Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia
December 7, 2016, PubMed
A Phase 1 Study of DCC-2036, a Novel Oral Inhibitor of BCR-ABL Kinase, in Patients with Philadelphia Chromosome Positive (Ph+) Leukemias Including Patients with T315I Mutation
December 12, 2011, ASH 2011
The Gatekeeper T315I Versus the Switch-Control Inhibitor DCC-2036: The Last Title Fight in CML?
July 1, 2011, The Hematologist
New Drug Shows Potential for Treatment-Resistant Leukemia
April 13, 2011, Science Daily
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Apr 12, 2011, Cancer Cell