Drug intelligence / Profile preview

famitinib + dalpiciclib + fulvestrant

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

Overview

famitinib + dalpiciclib + fulvestrant is a combination therapy being investigated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer. The regimen consists of dalpiciclib (SHR6390), a selective small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6); famitinib, a multi-targeted tyrosine kinase inhibitor that targets VEGFR2, PDGFR, and c-Kit; and fulvestrant, a selective estrogen receptor degrader (SERD). Dalpiciclib works by arresting the cell cycle in the G1 phase, while famitinib inhibits angiogenesis and tumor cell proliferation, and fulvestrant blocks estrogen-mediated signaling. This triplet combination is being evaluated in Phase 1b/2 clinical trials, such as those conducted at Henan Cancer Hospital, to improve outcomes in patients with heavily pretreated or advanced breast cancer.

Brand names
AiRuikangFaslodex
Other names
famitinib + dalpiciclib + fulvestrantSHR6390 + SHR1020 + fulvestrantdalpiciclib + famitinib + fulvestrant
02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)VEGFR2 (Vascular endothelial growth factor receptor 2)

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