Serenex Announces Initiation Of Second Phase 1 Trial For Oral Hsp90 Inhibitor, SNX-5422
Durham, NC - Serenex, Inc., a leader in the discovery and development of small molecule Heat Shock Protein 90 (Hsp90) inhibitors, recenhtly announced the initiation of a second phase 1 trial, in hematological malignancies, for SNX-5422, its novel heat shock protein 90 (Hsp90) inhibitor. SNX-5422 is a totally synthetic small molecule delivered orally and was discovered internally using Serenex's proprietary chemoproteomics technology platform.
"We are extremely excited to be starting our phase 1 hematological trial for SNX-5422," said Richard Kent, M.D., president and chief executive officer of Serenex. "Our first phase 1 trial for SNX-5422 began in May for solid tumors and based on results from early dosing cohorts, the compound has shown to be well tolerated by patients, with excellent oral bioavailability and pharmacokinetic properties. The hematology trial will enable us to take a closer look at biomarkers and early signals of anti-tumor activity in patients fighting hematological cancers."
The phase 1 study will be a dose escalation trial involving up to 50 patients with hematological malignancies. The trial will evaluate safety, pharmacokinetic and pharmacodynamic properties of SNX-5422. This clinical trial will be conducted at Vanderbilt University in Nashville, TN and at the University of Pittsburg Cancer Institute in Pittsburg, PA.
"Inhibition of Hsp90 promises to be a key tool in our fight against a number of hematological malignancies. If SNX-5422 can demonstrate a wider therapeutic window than the geldanamycin class of Hsp90 inhibitors, this could be very exciting indeed," said Merrill Egorin, Co-Director of the Molecular Therapeutic, Drug Discovery Program at the University of Pittsburg Cancer Institute.
"Hsp90 has become a very important oncology target. We are excited to be studying SNX-5422 in patients with hematological malignancies and assessing the safety and therapeutic potential of this orally available Hsp90 inhibitor," said Mace Rothenberg, M.D., Ingram Professor of Cancer Research at Vanderbilt University.
About Hsp90
Hsp90 is an important molecular chaperone protein that regulates the folding and degradation of key signaling molecules (client proteins) involved in cell growth and survival. Inhibition of Hsp90 is an attractive drug target for oncology because many of the client proteins are key mediators in pathways disrupted in cancer. Hsp90 is specifically activated in tumor cells where it controls multiple oncogenic proteins (e.g., Her2, Raf), and their downstream signaling molecules (e.g., Akt, Erk) that are critical to the proliferation and survival of tumors. Hsp90 stabilizes mutated proteins (e.g. v-Src) as well as fusion proteins resulting from chromosomal translocations (e.g., Bcr-Abl). Inhibition of Hsp90 leads to degradation of the client proteins, loss of signaling, and inhibition of cell growth.
About SNX-5422
SNX-5422 is a novel, synthetic, orally bioavailable small molecule discovered using the company's proprietary chemoproteomics discovery platform. In early clinical studies, SNX-5422 has been shown to have excellent oral bioavailability and pharmacokinetic properties. In pre-clinical studies SNX-5422 has demonstrated strong efficacy in multiple tumor models as a single agent and in combination with other cancer therapies. SNX-5422 exhibits slow, tight-binding characteristics, a property that has been recognized as important in other targeted therapeutics. SNX-5422 is positioned as a break-through targeted therapy with broad applicability across a wide range of solid and hematological cancers.
SOURCE: Serenex, Inc.