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Ref Type Journal Article
PMID (30724426)
Authors Long F, He Y, Fu H, Li Y, Bao X, Wang Q, Wang Y, Xie C, Lou L
Title Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models.
Journal Cancer science
Vol 110
Issue 4
Date 2019 Apr
Abstract Text Inhibition of the cyclin-dependent kinase (CDK) 4/6-retinoblastoma (RB) pathway is an effective therapeutic strategy against cancer. Here, we performed a preclinical investigation of the antitumor activity of SHR6390, a novel CDK4/6 inhibitor. SHR6390 exhibited potent antiproliferative activity against a wide range of human RB-positive tumor cells in vitro, and exclusively induced G1 arrest as well as cellular senescence, with a concomitant reduction in the levels of Ser780-phosphorylated RB protein. Compared with the well-known CDK4/6 inhibitor palbociclib, orally administered SHR6390 led to equivalent or improved tumor efficacy against a panel of carcinoma xenografts, and produced marked tumor regression in some models, in association with sustained target inhibition in tumor tissues. Furthermore, SHR6390 overcame resistance to endocrine therapy and HER2-targeting antibody in ER-positive and HER2-positive breast cancer, respectively. Moreover, SHR6390 combined with endocrine therapy exerted remarkable synergistic antitumor activity in ER-positive breast cancer. Taken together, our findings indicate that SHR6390 is a novel CDK4/6 inhibitor with favorable pharmaceutical properties for use as an anticancer agent.


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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
SHR6390 SHR6390 4 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
SHR6390 SHR 6390|SHR-6390|Dalpiciclib CDK4/6 Inhibitor 13 SHR6390 (dalpiciclib) inhibits CDK4/6, which may lead to cell cycle arrest and tumor growth inhibition (PMID: 30724426).
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
RB1 negative breast cancer no benefit SHR6390 Preclinical - Cell culture Actionable In a preclinical study, SHR6390 (dalpiciclib) demonstrated little cytotoxic activity against a RB1-negative breast cancer cell line in culture (PMID: 30724426). 30724426
RB1 dec exp Advanced Solid Tumor no benefit SHR6390 Preclinical - Cell culture Actionable In a preclinical study, SHR6390 (dalpiciclib) demonstrated limited cytotoxic activity against tumor cell lines with low Rb1 expression in culture (PMID: 30724426). 30724426
RB1 positive Advanced Solid Tumor sensitive SHR6390 Preclinical - Cell culture Actionable In a preclinical study, SHR6390 (dalpiciclib) inhibited CDK4/6-RB pathway signaling, leading to cell cycle arrest and inhibition of proliferation in a panel of RB1-positive tumor cell lines in culture, and tumor growth inhibition in cell line xenograft models (PMID: 30724426). 30724426
RB1 positive colon cancer sensitive SHR6390 Preclinical - Cell line xenograft Actionable In a preclinical study, SHR6390 (dalpiciclib) inhibited CDK4/6-RB pathway activation, leading to growth inhibition in an RB1-positive colon cancer cell line in culture, and tumor regression in a cell line xenograft model (PMID: 30724426). 30724426