A VX-680 (an Aurora Kinase Inhibitor) Study in Patients With Advanced Cancer
Summary
The purpose of this trial is to study an investigational drug in patients with recurrent or non-responsive solid tumors, or cancers for which standard therapy does not exist.
Study Design
Allocation: Non-Randomized, Control: Uncontrolled, Endpoint Classification: Safety/Efficacy Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment
Conditions
Cancer
Intervention
VX-680 (an Aurora Kinase Inhibitor)
Status
Terminated
Source
Merck
Results (where available)
Links
- Source: http://clinicaltrials.gov/show/NCT00104351
- Information obtained from ClinicalTrials.gov on July 15, 2010
Medical and Biotech [MESH] Definitions
Cyclin-dependent Kinase Inhibitor P19
An INK4 cyclin-dependent kinase inhibitor containing five ANKYRIN REPEATS. Aberrant expression of this protein has been associated with TESTICULAR CANCER.
Cyclin-dependent Kinase 2
A key regulator of CELL CYCLE progression. It partners with CYCLIN E to regulate entry into S PHASE and also interacts with CYCLIN A to phosphorylate RETINOBLASTOMA PROTEIN. Its activity is inhibited by CYCLIN-DEPENDENT KINASE INHIBITOR P27 and CYCLIN-DEPENDENT KINASE INHIBITOR P21.
Cyclin-dependent Kinase Inhibitor P15
An INK4 cyclin-dependent kinase inhibitor containing four ANKYRIN-LIKE REPEATS. INK4B is often inactivated by deletions, mutations, or hypermethylation in HEMATOLOGIC NEOPLASMS.
Cyclin-dependent Kinase Inhibitor P27
A cyclin-dependent kinase inhibitor that coordinates the activation of CYCLIN and CYCLIN-DEPENDENT KINASES during the CELL CYCLE. It interacts with active CYCLIN D complexed to CYCLIN-DEPENDENT KINASE 4 in proliferating cells, while in arrested cells it binds and inhibits CYCLIN E complexed to CYCLIN-DEPENDENT KINASE 2.
Cyclin-dependent Kinase Inhibitor P18
An INK4 cyclin-dependent kinase inhibitor containing five ANKYRIN-LIKE REPEATS. Aberrant expression of this protein has been associated with deregulated EPITHELIAL CELL growth, organ enlargement, and a variety of NEOPLASMS.
Clinical Trials
RATIONALE: Aurora A kinase inhibitor MLN8237 and bortezomib may stop the growth of cancer cells by blocking some of the enzymes needed for cell growth. PURPOSE: This phase I/II trial is s...
Aurora B/C Kinase Inhibitor GSK1070916A in Treating Patients With Advanced Solid Tumors
RATIONALE: Aurora B/C kinase inhibitor GSK1070916A (GSK1070916A) may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. PURPOSE: This phase I trial is...
Study with an investigational drug in patients with recurrent or non-responsive colorectal cancer or other advanced solid tumors. This is an early phase trial and some specific protocol i...
A Study of MLN8237, a Novel Aurora A Kinase Inhibitor, in Patients With Advanced Solid Tumors
To determine the dose-limiting toxicity (DLT) and maximum tolerated dose (MTD) of MLN8237 when given by mouth (PO) for a minimum of 7 and a maximum of 21 consecutive days, followed by a 14...
This is a phase I study of an investigational cancer drug, CYC116, in patients with advanced solid tumors.
PubMed Articles
Aurora kinases are key regulators of cell division and important targets for cancer therapy. We report that Binucleine 2 is a highly isoform-specific inhibitor of Drosophila Aurora B kinase, and we id...
Aurora kinases, frequently detected to be over-expressing in human tumors, regulate many essential events during mitosis progression and have been regarded as potentially important targets for cancer...
Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imida...
Crystal Structure of Human Aurora B in Complex with INCENP and VX-680.
We present the structure of human Aurora B kinase domain in complex with the C-terminal Aurora-binding region of human INCENP, and the Aurora kinase inhibitor VX-680. The structure unexpectedly reveal...
Mutants of protein kinase A that mimic the ATP-binding site of Aurora kinase.
We describe here mutations of the catalytic subunit α of protein kinase A (PKA) that introduce amino acid side chains into the ATP binding site and progressively transform the pocket to mimic that of...
