ENMD-2076 for hematological malignancies.

Abstract

INTRODUCTION:

Aurora kinases are key regulators of mitosis and inhibition of Aurora kinase activity is a rational therapeutic strategy in the treatment of solid tumors and hematological malignancies.

AREAS COVERED:

This paper will provide an updated summary of preclinical and clinical experience with ENMD-2076 in hematological malignancies. The MEDLINE (OVID) (1980 through 31 January 2012) was searched with the term combinations including Aurora, multiple myeloma, leukemia, lymphoma, myelodysplastic syndrome and myeloproliferative neoplasms. In addition, the American Society of Clinical Oncology (ASCO) (1997 - 2011) and the American Society of Hematology (ASH) (1997 - 2011) conference proceedings were searched for reports of new or ongoing trials.

EXPERT OPINION:

ENMD-2076 is a multi-kinase inhibitor, with activity against Aurora A kinase, FLT3, c-KIT, c-FMS and VEGFR-2 and -3. It appears to be tolerable, exhibits favorable pharmacokinetic profiles and has activity in patients with acute myeloid leukemia and multiple myeloma. Further evaluation with cytotoxic chemotherapy and targeted agents, which affect different pathways and have non-overlapping toxicities, in patients with hematological malignancies are warranted.

• Authors: Jonathan How, Karen Yee
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 21 Issue 5 Pg. 717-32 (May 2012) ISSN: 1744-7658 [Electronic] England
• PMID: 22397360 (Publication Type: Journal Article, Review)

Chemical References

• Angiogenesis Inhibitors
• Antineoplastic Agents
• ENMD 2076
• Protein Kinase Inhibitors
• Pyrazoles
• Pyrimidines
• Aurora Kinases
• Protein Serine-Threonine Kinases

Topics

• Angiogenesis Inhibitors (therapeutic use)
• Animals
• Antineoplastic Agents (therapeutic use)
• Aurora Kinases
• Hematologic Neoplasms (drug therapy, metabolism)
• Humans
• Protein Kinase Inhibitors (pharmacology, therapeutic use)
• Protein Serine-Threonine Kinases (antagonists & inhibitors)
• Pyrazoles (therapeutic use)
• Pyrimidines (therapeutic use)