SGX PHARMACEUTICALS, INC.

SGX PHARMACEUTICALS, INC.

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Company Overview
SGX Pharmaceuticals, Inc. is a biotechnology company that focuses on the discovery, development, as well as commercialization of cancer therapeutics. The company was incorporated in 1998. The registered headquarters of the company is located in San Diego, California. It is publicly traded on the NASDAQ under the Ticker symbol SGXP.
SGX Pharmaceuticals develops an internal oncology product pipeline and lead compounds through the application of its proprietary drug discovery platform, Fragments of Active Structures (FAST). The company’s pre-clinical development programs include BCR-ABL Kinase Inhibitor Program that focuses on compounds, which inhibit wild-type and Gleevec-resistant mutant forms of BCR-ABL tyrosine kinase, the enzyme that is responsible for CML; and MET Tyrosine Kinase Receptor Inhibitor program that inhibits solid tumors. In addition, the company develops JAK2, a non-receptor tyrosine kinase protein; and RAS, that is in the lead identification stage, which regulates cell growth. The company has collaboration and license agreements with Novartis Institutes for Biomedical Research, Inc.; Cystic Fibrosis Foundation Therapeutics, Inc.; National Institutes of Health; and Eli Lilly and Company.
SGX Pharmaceuticals is dedicated to provide patients with life-changing therapies through the innovation, excellence and commitment of its employees.
Business Summary
SGX Pharmaceuticals, Inc. is a biotechnology company focused on the discovery, development and commercialization of targeted therapeutics directed at addressing unmet medical needs in oncology. The Company’s most advanced drug development programs target the c-MET receptor tyrosine kinase (MET), an enzyme implicated in an array of cancers, and the BCR-ABL tyrosine kinase enzyme, for treatment of Chronic Myelogenous Leukemia (CML), a cancer of the bone marrow. The Company’s earlier stage drug discovery activities are focused on a portfolio of other protein and enzyme targets that have been implicated in human cancers. In August 2008, Eli Lilly and Company completed the acquisition of SGX Pharmaceuticals, Inc.
Description and history
SGX Pharmaceuticals, Inc., incorporated in July 1998, is a biotechnology company focused on the discovery, development and commercialization of targeted therapeutics directed at addressing unmet medical needs in oncology. The Company’s most advanced drug development programs target the c-MET receptor tyrosine kinase (MET), an enzyme implicated in an array of cancers, and the BCR-ABL tyrosine kinase enzyme, for treatment of Chronic Myelogenous Leukemia (CML), a cancer of the bone marrow. The Company’s earlier stage drug discovery activities are focused on a portfolio of other protein and enzyme targets that have been implicated in human cancers. In August 2008, Eli Lilly and Company completed the acquisition of SGX Pharmaceuticals, Inc.

The Company’s approach to drug discovery combines a number of tools designed to enable the identification of high quality development candidates. At the core is FAST, its fragment based, protein structure-guided drug discovery technology, underpinned by a x-ray crystallographic platform for the determination of protein structures. SGX Pharmaceuticals utilizes small molecule scaffolds, drawing upon detailed three-dimensional information predicting how they will bind to the target protein. This approach typically provides multiple opportunities for lead optimization, from which to choose.

MET Development Program

SGX Pharmaceuticals has identified a number of low molecular weight, selective MET inhibitors, including SGX523 and SGX126, which have demonstrated potency in cell based assays, oral bioavailability in multiple animal species and potent anti-tumor effects in multiple in vivo mouse models of human cancer.

SGX523 is an internally developed, small molecule inhibitor of MET. In January 2008, SGX Pharmaceuticals initiated two parallel, multi-center Phase I clinical trials to establish the safety and tolerability of an oral, twice daily dosing of SGX523 in patients with solid tumor cancers. The first trial has been designed to examine twice daily, oral dosing on a continuous 28-day cycle and the second trial has been designed to examine interrupted dosing (a repeating 21 day cycle of 14 days on therapy followed by seven days off).

In November 2007, SGX Pharmaceuticals announced the nomination of a second MET development candidate, SGX126, for IND-enabling preclinical development, to broaden the Company’s MET program. SGX126 is an internally developed, orally bioavailable small molecule inhibitor of MET, with potent in vitro and in vivo activity. SGX Pharmaceuticals is assessing whether to conduct any supplemental preclinical studies of SGX126 in light of the recent developments in its SGX523 clinical studies.

BCR-ABL Development Program

The Company’s BCR-ABL development program is focused on a compound that inhibits both wild-type and drug-resistant mutant forms of the BCR-ABL kinase, the target for second-line treatment of CML. The goal of this program is to develop an oral therapy for the second-line treatment of CML, that is, patients that relapse while on Gleevec and those intolerant of Gleevec. The Company’s development candidate, SGX393, is in IND-enabling preclinical development. SGX393 is an internally developed, potent, selective, orally bioavailable small molecule that inhibits wild-type BCR-ABL and several drug-resistant mutant forms of BCR-ABL, including the T315I mutant.

SGX Pharmaceuticals plans to conduct a Phase I dose escalation trial in relapsed/refractory CML patients to assess safety and tolerability and establish the maximum tolerated dose (MTD) or biologically effective dose (BED; the dose at which BCR-ABL enzyme activity is reduced by more than 90%) followed by administration of SGX393 to a cohort of pre-qualified CML patients possessing the T315I mutation. Subsequent clinical trials will be designed once the results of the initial trial are available, but they likely would involve pre-qualified CML patients bearing the T315I mutation, other relapsed/refractory CML patients and those intolerant of Gleevec.

Oncology Drug Discovery Portfolio

The SGX drug discovery technologies are being applied to a portfolio of oncology targets, including JAK2, RAS, and three undisclosed tyrosine kinases. SGX Pharmaceuticals has been collaborating with Novartis Institutes for Biomedical Research, Inc., (Novartis) under a license and collaboration agreement that it entered to discover, develop and commercialize oral BCR-ABL inhibitors for the front-line treatment of CML. The research term of this agreement concluded in late March 2008. A number of compounds discovered within the collaboration is undergoing further evaluation at Novartis.

JAK2 is a non-receptor tyrosine kinase involved in cytokine-induced signaling and growth regulation, survival, and differentiation of cells. Enhanced JAK2 activation has been implicated in various blood disorders. The Company has identified JAK2 inhibitors that have good potency against both wild-type and mutant JAK2 in cell-based assays. Oral bioavailability and selectivity versus JAK3 have also been demonstrated and are aimed at optimizing the potency and drug-like properties of these compounds. This program is in the lead optimization stage

RAS is a protein that regulates cell growth. Applying its FAST platform, the Company has taken a approach to the modulation of RAS activity and it has identified inhibitors that have demonstrated cell-based activity. SGX Pharmaceuticals RAS program is in the lead identification stage.

SGX Pharmaceuticals is also pursuing lead identification/lead optimization for three additional undisclosed oncology targets, all of which are tyrosine kinases. Like MET, BCR-ABL, JAK2, and RAS, these targets have been chosen on the basis of their potential roles in human cancers.

The Company competes with Astex Therapeutics Limited, Plexxikon Inc., Evotec AG, Vernalis Plc., Sunesis Pharmaceuticals, Inc., and Active Site, Inc.

Business Line
Biotechnology company that focuses on the discovery, development, as well as commercialization of cancer therapeutics
Subsidiary
PROSPECT GENOMICS, INC
Advisor
ERNST & YOUNG LLP
IPO date
2/1/2006
US SIC Code
2834
Company Address
10505, Roselle Street

City province or state postal code
92121, SAN DIEGO, CA
Phone: +1 858 558 4850
Fax: +1 858 558 4859
Country address: UNITED STATES OF AMERICA
Website url: www.sgxpharma.com