20th NovHas with the T315I mutation, however, the 20th November 2007, Merck registration up to a comprehensive analysis of the efficacy and safety after a patient had exposed QTc prolongation.90 Phase II study of VX 680 was planned in small cell lung cancer and colorectal cancers.84 AZD1152 AZD1152 is not a selective inhibitor of Aurora B is currently being tested in phase CYT997 I studies with different doses. Neutropenia was the main dose-limiting toxicity t reported.91 A phase I II is underway in chemistry myeloid leukemia With acute Relapse. In acute leukemia Mie cells in vitro and in vivo has been found to synergistically enhance the AZD1152 antiproliferative agent of microtubules and a topoisomerase II inhibitor. There are four known members of this family of serine-threonine kinases mitotic people: PLK1, and PLK2 PLK3 PLK4.
PLK1 has been studied most extensively and is overexpressed in many tumor types.83 Elevated PLK1 Andarine expression has lead histological grade and poor prognosis with a variety of small molecules or siRNA inhibition of Plk1 to tumors.93 M G2 arrest and apoptosis correlated with inadequate production of spindle p the tensile forces cytokinesis.94 and break, 95 In addition, although the PLK1 depletion type t Harmful to cancer cells, normal cells showed little or no cytotoxicity t in response to Ersch shrinkage. Thus, PLK1 is an attractive target for anti-mitotic cancer therapies. The first small molecule inhibitor of Plk1 was reported marine natural product compounds scytonemin.96 ON01910.Na BI 2536 and are currently in clinical development. BI 2536 BI 2536 is highly selective for PLK1.
Investigated in Phase I trial in 104 patients 2 different regimens evaluated.97, 98 The main dose-limiting toxicity of t The two calendars was neutropenia. With the addition of thrombocytopenia on the lists Other side effects were fatigue, nausea and vomiting. The phase II trials evaluating BI 2536 are underway in metastatic or recurrent non-small cell lung cancer and small cell lung cancer as second-line therapy. ON 01910.Na 01910.Na is a competitive inhibitor of ATP PLK1, the st with the F Ability, substrates bind PLK Rt. It has nanomolar potency against ABL, FLT1 and PDGFR.84 In phase I studies, three different treatments were evaluated and the results pr in abstract form Presents on these.99 2, 100 events events were mild to moderate Mie, leukopenia erh hte liver enzymes, the symptom My stomach and fatigue.
KSP kinesin spindle protein inhibitors is a motor protein kinesin which then causes it the separation of the centrosome and is required to produce the bipolar spindle. There is evidence that increased CSF expression in tumor cells compared to normal cells Ht. 101 inhibition of KSP causes mitotic arrest with monopolar spindle no effect on proliferating cells.84 KSP absent in differentiated neurons. First page