Drug intelligence / Profile preview

dalpiciclib + apatinib

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Dalpiciclib + apatinib is a combination therapy comprising two small-molecule targeted agents: dalpiciclib, a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), and apatinib, a tyrosine kinase inhibitor (TKI) specifically targeting vascular endothelial growth factor receptor-2 (VEGFR-2). Dalpiciclib induces cell cycle arrest in the G1 phase by preventing the phosphorylation of the retinoblastoma (Rb) protein, thereby inhibiting tumor cell proliferation. Apatinib acts as an anti-angiogenic agent by blocking VEGFR-2 signaling, which is critical for tumor-associated neoangiogenesis and vascular permeability. This combination is primarily developed by Jiangsu Hengrui Pharmaceuticals and is being evaluated in clinical trials, including those led by Peking University Third Hospital, for the treatment of advanced or refractory sarcomas and other solid tumors. The rationale for the combination lies in the potential synergy between cell cycle inhibition and the disruption of the tumor microenvironment through anti-angiogenesis.

Brand names
Dawu
Other names
SHR6390 + YN968D1dalpiciclib plus apatinib
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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