Table 3: CDK inhibitors utilized in clinical trials for the treatment of various types of malignancies (http://www.clinicaltrials.gov).

Cdk inhibitors (Alias(es))GenerationPrincipal antikinase activityClinical trials for the treatment of tumors

Seliciclib (CYC-202;R-roscovitine)ICdk1, 2, 5, 7, 9; CK1; GSK3A; DIRK1A; ERK1Phases I-II for nonsmall cell lung cancer (NSCLC) and other solid tumors

Alvocidib (flavopiridol)ICdk1, 2, 4, 6, 7, 9; GSK3βPhases I-II for various types of cancers, such as multiple myeloma, leukemia, lymphomas, sarcoma, and solid tumors

Dinaciclib (SCH727965)ICdk1, 2, 5, 9Phases I-II for various solid tumors; phases I-II for acute myelogenous leukemia, acute lymphoblastic leukemia, mantle cell lymphoma, and B cell chronic lymphocytic leukemia

SNS-032 (BMS-387032)ICdk1, 2, 4, 7, 9Phases I-II for B-cell malignancies, nonsmall cell lung cancer (NSCLC), advanced breast cancer, and melanoma

AG-024322ICdk1, 2, 4, 7Phase I for non-Hodgkin’s lymphoma and advanced solid tumors

R547 (R0-4584820)ICdk1, 2, 4, 7Phase I for advanced solid tumors

P276-00IICdk1; Cdk4; Cdk9Phases I-II for multiple myeloma and various advanced refractory malignancies

PD-0332991IICdk4, Cdk6Phase I for non-Hodgkin’s lymphoma, mantle cell lymphoma, and other malignancies

AT-7519IICdk2, Cdk4, Cdk5, Cdk9; GSK3βPhases I-IIa for advanced and/or metastatic solid tumors and refractory non-Hodgkin’s lymphoma

RGB-286638IICdk1, Cdk2, Cdk4, Cdk5, Cdk7, Cdk9Entering a phase I clinical trial for the treatment of advanced solid tumors

ZK 304709IIICdk1, 2, 4, 7, 9; VEGFR1, 2, 3;
PDGFR-b; Flt-3
Phase I trials for refractory and/or relapsed solid tumors

GPC-286199 (RGB-286199)IIICdk1, 2, 3, 5, 7, 9; CRKsPreclinical stage

JNJ-7706621IIICdk1, 2, 3; Aurora A/BPreclinical stage