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Fluzoparib + dalpiciclib
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Fluzoparib + dalpiciclib is a combination of two orally administered small molecule drugs under clinical investigation for the treatment of advanced or metastatic cancers, including sarcoma and breast cancer. Fluzoparib is a selective inhibitor of poly(ADP-ribose) polymerase 1 and 2 (PARP1/2), which impairs DNA repair in homologous recombination-deficient tumor cells, leading to cell cycle arrest and apoptosis[6][7]. Dalpiciclib is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase by inhibiting phosphorylation of the retinoblastoma protein, thereby suppressing tumor cell proliferation[5][8]. The combination aims to exploit complementary mechanisms—DNA damage induction by PARP inhibition and cell cycle blockade by CDK4/6 inhibition—to enhance antitumor efficacy. Both drugs are developed primarily by Jiangsu Hengrui Medicine.
- Brand names
- AiRuiYi (for fluzoparib)AiRuiKang (for dalpiciclib)
- Other names
- Dalpiciclib Isethionate (for dalpiciclib)
02
Targets
CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)PARP2 (Poly (adp-ribose) polymerase 2)
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