Table 1 Current CDK4/6 inhibitors in clinical development
From: Targeting the cyclin-dependent kinases (CDK) 4/6 in estrogen receptor-positive breast cancers
Compound | Manufacturer | Phase | CDK4/6 in vitro inhibition profile (IC50, nM) |
|---|---|---|---|
Palbociclib (PD-0332991) | Pfizer, Inc. | Approved | CDK4 (cyclinD1): 11 |
CDK4 (cyclinD3): 9 | |||
CDK6 (cyclinD2): 15 | |||
Ribociclib (LEE011) | Novartis | III | CDK4 (cyclinD1): 10 |
CDK6 (cyclinD2): 40 | |||
Abemaciclib (LY2835219) | Eli Lilly | III | CDK4 (cyclinD1): 2 |
CDK6 (cyclinD1): 9.9 |