SAN DIEGO, March 10, 2021 /PRNewswire/ -- MEI Pharma, Inc. (NASDAQ: MEIP), a late-stage pharmaceutical company focused on advancing new therapies for cancer, today announced that the abstract, Voruciclib, a CDK9 inhibitor, downregulates MYC and inhibits proliferation of KRAS mutant cancers in preclinical models, was selected for an E-Poster Session presentation at the American Association for Cancer Research (AACR) Annual Meeting 2021 and will be available on April 10, 2021. Voruciclib is an orally available inhibitor of cyclin-dependent kinase 9 (CDK9), part of a family of regulatory enzymes important to cell cycle regulation associated with cell proliferation and increased survival.
KRAS mutated cancers are frequently associated with overexpression of MYC, a transcription factor regulating cell proliferation and growth. Inhibition of CDK9 leads to reduced transcription of MYC. As reported in the abstract to be presented at AACR 2021, voruciclib decreased cell viability among multiple KRAS mutant cancer cell lines in vitro and was associated with significant tumor growth inhibition in vivo. Voruciclib treatment was associated with rapid inhibition of MYC phosphorylation at Ser62 resulting in a decrease in MYC protein. The research presented suggests that voruciclib could be an attractive therapeutic target for cancers driven by KRAS mutated cancers.
MEI pharma is also engaged in additional pre-clinical studies to explore the potential synergistic activity in various cancers of voruciclib in combination with drug-candidates that directly inhibit KRAS.
Details of MEI's e-poster presentation at AACR Annual Meeting 2021:
Abstract Title: Voruciclib, a CDK9 inhibitor, downregulates MYC and inhibits proliferation of KRAS mutant cancers in preclinical models Poster Number: 1962 Poster Session Title: Cell Cycle Date: Saturday, April 10, 2021
About Voruciclib Voruciclib is an orally administered cyclin-dependent kinase (CDK) inhibitor differentiated by its potent in vitro inhibition of CDK9 in addition to CDK6, 4 and 1. The CDK family of proteins are important cell cycle regulators.
CDK9 is a transcriptional regulator of the myeloid leukemia cell differentiation protein ("MCL1"), a member of the family of anti-apoptotic proteins which, when elevated, may prevent the cell from undergoing cell death. Inhibition of CDK9 blocks the production of MCL1, which is an established resistance mechanism to the B-cell lymphoma ("BCL2") inhibitor venetoclax (marketed as Venclexta®).
CDK9 is also a transcriptional regulator of MYC proto-oncogene protein ("MYC"), a transcription factor regulating cell proliferation and growth which contributes to many human cancers and is frequently associated with poor prognosis and unfavorable patient survival. Targeting MYC directly has historically been difficult, but CDK9 is a transcriptional regulator of MYC and is a promising approach to target this oncogene.
Voruciclib is being currently evaluated in a Phase 1b trial evaluating dose and schedule in patients with acute myeloid leukemia ("AML") and B-cell malignancies.
About MEI Pharma MEI Pharma, Inc. (Nasdaq: MEIP) is a late-stage pharmaceutical company focused on developing potential new therapies for cancer. MEI Pharma's portfolio of drug candidates contains four clinical-stage assets, including zandelisib, currently in an ongoing Phase 2 clinical trial which may support accelerated approval applications with the U.S. Food and Drug Administration. Each of MEI Pharma's pipeline candidates leverages a different mechanism of action with the objective of developing therapeutic options that are: (1) differentiated, (2) address unmet medical needs and (3) deliver improved benefit to patients either as standalone treatments or in combination with other therapeutic options. For more information, please visit www.meipharma.com.
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