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Ref Type Journal Article
PMID (30194564)
Authors Rahaman MH, Yu Y, Zhong L, Adams J, Lam F, Li P, Noll B, Milne R, Peng J, Wang S
Title CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.
Journal Investigational new drugs
Vol 37
Issue 4
Date 2019 08
Abstract Text Acute myeloid leukemia (AML) is the most common form of acute leukemia with dismal long-term prognosis with age. The most aggressive subtype of AML is MLL-AML that is characterized by translocations of the mixed-lineage leukemia gene (MLL) and resistance to conventional chemotherapy. Cyclin dependent kinase 9 (CDK9) plays a crucial role in the MLL-driven oncogenic transcription, and hence, inhibiting activity of CDK9 has been proposed as a promising strategy for treatment of AML. We investigated the therapeutic potential of CDKI-73, one of the most potent CDK9 inhibitors, against a panel of AML cell lines and samples derived from 97 patients. CDKI-73 induced cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it was relatively low toxic to the bone marrow cells of healthy donors. In MV4-11 xenograft mouse models, oral administration of CDKI-73 resulted in a marked inhibition of tumor growth (p < 0.0001) and prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities. The study suggests that CDKI-73 can be developed as a highly efficacious and orally deliverable therapeutic agent for treatment of AML.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
CDKI-73 CDK1 Inhibitor 13 CDK2 Inhibitor 23 CDK9 Inhibitor 19 CDKI-73 is a kinase inhibitor that blocks CDK9, CDK1, and CDK2 activity, which may lead to apoptotic activity and inhibition of cell proliferation and tumor growth (PMID: 30194564, PMID: 24495868, PMID: 32368391).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KMT2A fusion acute myeloid leukemia sensitive CDKI-73 Preclinical - Cell line xenograft Actionable In a preclinical study, CDKI-73 treatment inhibited Cdk9 kinase activity and viability, and induced apoptosis in acute myeloid leukemia cell lines harboring KMT2A fusions in culture, and inhibited tumor growth and induced regression in a cell line xenograft model (PMID: 30194564). 30194564