Table 1.
Selected inhibitors of cell cycle regulators used in clinical trials for lung cancer therapy
Inhibitor | Main targets | Clinical trials |
Inhibitors of cyclin-dependent kinases | ||
Flavopiridol also known as alvocidib | CDK1, CDK2, CDK4, CDK6, CDK7 and CDK9 | Phase I: NSCLC in combination with paclitaxel and carboplatin (ref. 115) |
Aminothiazole SNS-032 also known as BMS-387032 (Sunesis) | CDK2, CDK7 and CDK9 (CDK1 and CDK4) | Phase I: NSCLC Sensitized radioresistant NSCLC cells to ionizing radiations (ref. 116) |
R-roscovitine also known as CYC202 and seliciclib (Cyclacel) | CDK1, CDK2, CDK5, CDK7 and CDK9 | Phase I–II: NSCLC (ref. 117) |
Indisulam, also known as E7070 | Not Assigned | Phase I: lung cancer in combination with irinotecan |
SCH 727965 | CDK1, CDK2, CDK5 and CDK9 | Phase II: NSCLC |
Inhibitors of mitotic checkpoint kinases | ||
VX-680, also known as MK-0457 | Pan-aurora | Phase I–II: NSCLC Trials discontinued owing to QT prolongation (ref. 118) |
Inhibitors of DNA Damage Checkpoint kinases | ||
7-hydroxy-staurosporine, also known as UCN-01 | CHK1 and MARK3 (PKC, PDK1, GSK3β, CDK1, CDK2 and CHK2) | Phase II: SCLC (with topotecan) |