Phase I Dose Escalation Study to Determine the Safety and Pharmacokinetics of MSX-122 Administered Orally in Patients With Refractory Metastatic or Locally Advanced Solid Tumors
Primary Objectives:
To determine the maximum tolerated dose (MTD) and the recommended Phase II dose(s) and schedule of MSX-122
To characterize the dose limiting toxicities (DLTs) and determine the overall safety and tolerability of MSX-122
Secondary Objectives:
To determine the pharmacokinetics and pharmacodynamics of orally administered MSX-122
To evaluate the preliminary evidence for anti-tumor activity of MSX-122
To perform correlative studies to elucidate signaling pathways involved in CXCR4 activation in blood and optional tissue specimens by IHC (immunohistochemistry) and RPPA (reverse phase protein microarrays)
100 Clinical Results associated with Metastatix, Inc.
0 Patents (Medical) associated with Metastatix, Inc.
01 Oct 2009·Expert Opinion on Drug DiscoveryQ3 · MEDICINE
In vitro screening for chemokine antagonists
Q3 · MEDICINE
Article
Author: Ribeiro, Sofia ; Horuk, Richard
BACKGROUND:Chemokines play an important role in host defense coordinating the migration of immune cells. They do this by activating G-protein-coupled receptors and these proteins have attracted a huge investment in research and development by the pharmaceutical industry with the promise of new therapeutics for treating inflammatory diseases.
OBJECTIVE:Here, we provide a brief perspective of the in vitro assays that have been used in drug discovery for identifying potent and specific chemokine receptor antagonists. We outline the complexity of the chemokine system, give a historical perspective on the in vitro assays and types of assays used at different stages of discovery, followed by several examples of successes and failures in the clinic.
CONCLUSION:We discuss the rationale for continuing, after several failures, targeting chemokine receptors and how screening may change with the increasing evidence of dimerization of chemokine receptors.
100 Deals associated with Metastatix, Inc.
100 Translational Medicine associated with Metastatix, Inc.