Phase I-II Study to Determine the Maximum Tolerated Dose (MTD) of AUY922 in Advanced Solid Malignancies, and Efficacy in HER2+ or ER+ Locally Advanced or Metastatic Breast Cancer Patients.

Phase I-II Study to Determine the Maximum Tolerated Dose (MTD) of AUY922 in Advanced Solid Malignancies, and Efficacy in HER2+ or ER+ Locally Advanced or Metastatic Breast Cancer Patients.

Solid Tumors

Ongoing, but not recruiting

1

Start Date 07/15/2007

Age of Trial (yrs) 17.8

Gleevec-resistant

HSP90 inhibitor

Destroy KIT

GIST not specified. GIST patients known to be enrolled.

CAUY922A2101

Novartis

Novartis Pharmaceuticals 1 800 340-6843

IV Intravenous

AUY922 is a potent Hsp90 inhibitor from Novartis. The phase I portion of this trial allows adults with advanced solid tumors. The trial will then expand into a phase II with expansion arms in patients with either HER2 Positive or ER Positive locally advanced or metastatic breast cancer.
Drug Class: HSP90 inhibitors
Heat Shock Protein 90 (Hsp90) is a protein that has several functions in cells. It is an emerging therapeutic target of interest for the treatment of cancer. Proteins are the mainstay of structural and signaling elements of all cells. Hsp90 is a molecule that maintains the conformation and activity of specific proteins in the cell, also called "client proteins" of Hsp90. KIT is one of the client proteins of Hsp90. Hsp90 enables cancer cell survival by maintaining the function of their mutated client proteins including the KIT and PDGFRA proteins in GIST. Inhibition of Hsp90 therefore has the potential to destroy the activated KIT/PDGFRA proteins resulting in a therapeutic effect in GIST. Since the target of these drugs are Hsp90 and not KIT or PDGFRA, they should be unaffected by the secondary mutations that commonly cause resistance to Gleevec. In fact, preliminary work has suggested that the stronger KIT is activated, the better they work.
Drugs in this class include both oral and intravenous drugs. Some of the intravenous drugs are also being developed as an oral version.