Biology Reference
In-Depth Information
TABLE 1.5 Examples of Inhibitors of Cyclin-dependent Kinases in Clinical Trials
Main targets
(other targets)
Agent
Company
Indications
Trial status
Sanofi
e
Aventis
Alvocidib (flavopiridol)
CDK1, CDK2, CDK4,
CDK6, CDK7, CDK9
(GSK3
Various leukemias, multiple
myeloma, various lymphomas,
sarcoma, pancreatic,
gastroesophageal, solid tumors,
germ cell tumors
Phase 1, 2
b
)
Dinaciclib
(SCH 727965)
Schering Plough
CDK1, CDK2, CDK5,
CDK9
Advanced solid tumors, NHL,
ALL, CLL, MM, lymphoma,
advanced BC, NSCLC
Phase 2
Indisulam (E7070)
Esai
CDK2, cyclin E
Solid tumors, stage 4
melanoma, renal, colorectal,
MBC, pancreatic, lung, GI
Phase 1, 2
Seliciclib
(R-roscovitine, CYC202)
Cyclacel
CDK1, CDK2, CDK5,
CDK7 and CDK9 (CK1,
GSK3
NSCLC, advanced solid tumors
Phase 1, 2
, DYRK1A,
ERK1, ERK2, PDXK)
aeb
AT7519
Astex
CDK2, CDK4, CDK5 and
CDK9
(CDK1, CDK4, CDK6
and GSK3
Multiple myeloma, advanced
solid tumors, refractory NHL
Phase 1, 2
b
)
LEE011
Novartis AG
CDK4, CDK6
Solid tumors, lymphoma
Phase 1
P1446A-05
Nicholas Piramal
CDK4
Advanced refractory
malignancies
Phase 1
P276-00
Nicholas Piramal
CDK1, CDK4, CDK9
(CDK2, CDK6, CDK7)
MM, mantle cell lymphoma,
head and neck, pancreatic,
cyclin D1-positive melanoma,
advanced refractory
malignancies
Phase 1, 2
PD-0332991
Pfizer
CDK4, CDK6
Advanced cancers,
glioblastoma, mantle cell
lymphoma, MM, HR
Phase 1, 2
รพ
advanced BC
R547
(Ro-4584820)
Hoffmann La
Roche
CDK1, CDK2, CDK4,
CDK7
Advanced solid tumors
Phase 1
SNS-032
(BMS-387032)
Sunesis
CDK2, CDK7 and CDK9
(CDK1, CDK4)
B-lymphoid, CLL, MM,
lymphoma, advanced solid
tumors
Phase 1
Terameprocol
(EM-1421)
Erimos
CDK1, survivin, VEGFRs
Leukemia, refractory solid
tumors, lymphoma
Phase 1
UCN-01
Developmental
Therapeutics
Program, National
Cancer Institute
Chk1, MARK3, PKC,
PDK1, GSK3
Leukemia and MDS, solid
tumors, lymphoma
Renal, melanoma, lymphoma,
SCLC
Phase 1
Phase 2
, CDK1,
CDK2 and Chk2
b
ZK 304709
(MTGI, ZK-CDK)
Schering AG
CDK1, CDK2, CDK4,
CDK7, CDK9 (VEGFR1
VEGFR2, VEGFR3,
PDGFR)
Advanced solid tumors
Phase 1
Abbreviations: ALL, acute lymphoblastic leukemia; BC, breast cancer; CLL, chronic lymphocytic leukemia; MBC, metastatic breast cancer; MDS, myelodysplastic
syndrome; MM, multiple myeloma; NHL, non-Hodgkin's lymphoma; NSCLC, non-small-cell lung cancer.
