Table 2.
Clinical trials on CDK inhibitors with synthetic lethality potential.
| Inhibitor | Inhibition of CDK | Clinical applicability | Status | Ref. |
|---|---|---|---|---|
| Palbociclib (combination with letrozole, an aromatase inhibitor) | CDK4/6 | ER+ and HER– breast cancer | FDA approved | 89,90 |
| Palbociclib (combination with cetuximab, an inhibitor of EGFR) | CDK4/6 | Head and neck squamous-cell carcinomas (HNSCCs) | Phase II | 91 |
| Palbociclib (combination with cetuximab, an inhibitor of EGFR) | CDK4/6 | K-RAS, N-RAS and BRAF wild-type metastatic colorectal cancer (CRC) | Phase II | 92 |
| Palbociclib (combination with MEK162, an inhibitor of MEK) | CDK4/6 | K-RAS and N-RAS mutant metastatic colorectal cancers (CRC) | Phase II | 93 |
| Palbociclib (combination with gedatolisib, a mTOR inhibitor) | CDK4/6 | Lung cancer squamous cell, cancers of head, neck and pancreas | Phase I | 94 |
| Dinaciclib (MK-7965) (combination with MK2206, an AKT inhibitor) | CDK1/2/5/9 | Pancreatic cancer | Phase I | 95 |
| Dinaciclib (combination with pembrolizumab, a monoclonal anti-PD-L1) | CDK1/2/5/9 | Hematologic malignancies | Phase I | 96 |
| Dinaciclib (combination with ofatumumab, a monoclonal anti-CD20) | CDK1/2/5/9 | Relapsed/refractory CLL | Phase III | 87 |
| Alvocidib (combination with venetoclax, a BCL-2 inhibitor) | CDK1/2/4/9 | AML | Phase I | 97,98 |