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. 2023 Jul 29;30(9):2035–2052. doi: 10.1038/s41418-023-01196-z

Table 1.

Clinically relevant cell cycle kinase inhibitors.

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

NCT03242382NR

NCT01209598 [252254]

Phase 2

Phase 2

Recruiting

Completed

Solid tumors (CDK4/6 amp)

Abemaciclib

Palbociclib

NCT03310879

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

NCT02981940 [256]

NCT01227434 [257]

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]

NCT04545710 [261]

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.