Table 1.
Targeted kinase | Tumor | Inhibitor | Clinical trials (NCT nUMBER) | Phase | Status |
---|---|---|---|---|---|
CDK4/6 | Liposarcoma (CDK4/6 amp) | Abemaciclib | NCT04967521 [251] | Phase 3 | Recruiting |
Sarcoma (CDK4 overexpression/amp) |
Palbociclib Palbociclib |
Phase 2 Phase 2 |
Recruiting Completed |
||
Solid tumors (CDK4/6 amp) |
Abemaciclib Palbociclib |
NCT01037790 [252, 255] |
Phase 2 Phase 2 |
Recruiting Completed |
|
Metastatic breast cancer (HR + ; HER2-) | Abemaciclib + Aromatase Inhibitor / Abemaciclib + Fulvestrant | NCT05362760 | Phase 4 | Recruiting | |
Glioblastoma (CDK4/6 amp) |
Abemaciclib Palbociclib |
Phase 2 Phase 2 |
Active Terminated |
||
Cancer with brain metastasis | Abemaciclib | NCT02308020 [258] | Phase 2 | Completed | |
Non-Small cell lung cancer |
Abemaciclib Abemaciclib + Osimertib |
NCT02152631 [259, 260] |
Phase 3 Phase 2 |
Active Unknown |
|
Squamous cell lung cancer (CDK4 amp) |
Palbociclib + Docetaxel | NCT02785939 | Phase 2/3 | Completed | |
Esophagogastric cancer (CDK6 amp) |
Abemaciclib | NCT03292250 | Phase 2 | Completed | |
CDK2 | Breast cancer and solid tumors | PF-07104091 | NCT05262400 | Phase 2 | Recruiting |
ATR | Solid tumors | Berzosertib | NCT03718091 [262] | Phase 2 | Completed |
Ovarian cancer | Berzosertib + gemcitabine | NCT02595892 [263] | Phase 2 | Active | |
Solid tumors (relapsed or refractory) | BAY1895344 | NCT05071209 | Phase 1/2 | Active | |
Non-small cell lung cancer | Ceralasertib | NCT05450692 | Phase 3 | Recruiting | |
Advanced solid tumors and Hematological Malignancies | ATG-018 | NCT05338346 | Phase 1 | Recruiting | |
DNA-PK | Rectal cancer | Peposertib | NCT03770689 | Phase 1/2 | Completed |
CHK1/2 | Solid tumors | LY3295368 | NCT02873975 | Phase 2 | Completed |
Small cell lung cancer | LY3295368 | NCT02735980 | Phase 2 | Completed | |
Ovarian Carcinoma, Endometrial Adenocarcinoma, and Urothelial Carcinoma | LY2606368 | NCT05548296 | Phase1/2 | Recruiting | |
WEE1 | Triple-negative Metastatic Breast Cancer | MK-1775 | NCT03012477 | Phase 2 | Completed |
Adenocarcinoma of the Pancreas | MK-1775 | NCT02037230 [264] | Phase 1/2 | Completed | |
Advanced solid tumors | Debio 0123 | NCT05109975 | Phase 1 | Recruiting | |
High-Grade Serous Ovarian, Fallopian Tube or Primary Peritoneal Cancer (CycE Driven) | ZN-C3 | NCT05128825 | Phase 2 | Recruiting | |
Uterine Serous Carcinoma | ZN-C3 | NCT04814108 | Phase 2 | Recruiting | |
PLK1 | Pancreatic cancer | Rigosertib + Gemcitabine | NCT01360853 [265] | Phase 3 | Completed |
Myelodysplastic Syndromes | Rigosertib | NCT01241500 [266] | Phase 3 | Completed | |
AURORA A | Prostate cancer | Alisertib | NCT01799278 [267] | Phase 2 | Completed |
Acute Myeloid Leukemia | Alisertib | NCT02560025 [268] | Phase 2 | Completed | |
Cancer Patients (KRAS G12C mutated) | LY2606368 | NCT04956640 | Phase 1 | Recruiting |
In a wide range of tumor malignancies, several kinase inhibitors that target cell cycle regulators are currently undergoing clinical trials for cancer therapy, both as single and combined treatment.