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Exelixis Announces Phase II Trial Programs for Most Advanced Internally Developed Compounds

Posted on: Monday, 15 August 2005, 06:00 CDT

SOUTH SAN FRANCISCO, Calif., Aug. 15 /PRNewswire-FirstCall/ -- Exelixis, Inc. today announced plans for Phase II programs for its three most advanced internally generated development compounds, XL999, XL647, and XL784. XL999 and XL647 are anticancer compounds, currently in late Phase I trials and the company intends to begin a Phase II program for each of these compounds before the end of the year. XL784 has completed a single dose Phase I trial as well as additional toxicology and formulation development in preparation for a Phase II program to test its utility in diabetic nephropathy.

Based on the specific targets of each compound, preclinical data, and insights gained during the Phase I trials, the company intends to carry out expanded Phase II programs for each of the compounds. XL999 and XL647 each will be tested in multiple tumor types, and XL784 will be moved forward in diabetic nephropathy. All of these trials will be funded through the financing that the company obtained from Symphony Capital during the second quarter of 2005. The company expects that Phase II data for XL999 and XL647 will be available in 2006, and that the Phase II trial for XL784 in diabetic nephropathy will take fifteen to eighteen months to complete.

XL999 is a potent inhibitor in vitro of the FGFR, VEGFR and PDGFR receptor tyrosine kinases (RTKs), implicated in the development and maintenance of tumor vasculature. In addition, it inhibits Flt3, implicated in the etiology of certain leukemias. The company intends to advance XL999 in Phase II trials in multiple solid tumor types: renal cell carcinoma, colorectal, non-small cell lung, and ovarian cancers. In addition, the company intends to investigate XL999 in hematological malignancies: acute myelogenous leukemia and multiple myeloma. For each of these malignancies, XL999 will be studied as a single agent, looking for responses in patients who have failed prior therapies. Some of the studies are also designed to evaluate single-agent activity of XL999 in previously untreated patients for whom conventional therapy is not appropriate. Additionally, the company is considering combination trials of XL999 either in combination with other anti-angiogenic compounds or with cytotoxic chemotherapy.

XL647 simultaneously inhibits the EGFR, HER2, and VEGFR RTKs in vitro. The compound is orally bioavailable in humans and a tablet dosage form has been developed for use in Phase II studies. XL647 is expected to enter initially into Phase II trials in patients with non-small cell lung cancer and breast cancer, tumors where the kinases inhibited by XL647 are known to play a role. Additionally, the company is considering combination trials of XL647 with other anticancer treatments to test the ability of the combination therapy to prolong progression free survival.

Exelixis plans to advance XL784 into a Phase II trial for the treatment of patients with kidney disease resulting from diabetes. Prior to starting the Phase II trial, a repeated dose Phase I study will be conducted in healthy volunteers. A previous Phase I study demonstrated that XL784 is orally bioavailable and that single doses were tolerated up to 1700 mg per patient, the highest dose studied. The planned study will evaluate the safety, pharmacokinetics and pharmacodynamics of XL784 administered daily for 2 weeks using a newly-developed capsule formulation. After successful completion of the multi-dose Phase I trial, the company plans to initiate a Phase II study to test the ability of XL784 to treat patients with proteinuria associated with diabetic kidney disease. The trial will employ a double-blind, placebo-controlled design that will begin as soon as possible after completion of the Phase I trial.

The company anticipates that publications describing XL999 and XL647 will be submitted to the AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics meeting to be held in Philadelphia in November, at which point the Phase I data will be described.

About Exelixis

Exelixis, Inc. is a leading genomics-based drug discovery company dedicated to the discovery and development of novel therapeutics across various disease areas. The company is leveraging its fully integrated gene-to-drug platform to fuel the growth of its proprietary drug pipeline. Exelixis' development pipeline covers cancer and metabolism and is comprised of the following compounds: XL119 (becatecarin), for which a multinational Phase III clinical trial in bile duct tumor is ongoing and which has been exclusively licensed to Helsinn Healthcare S.A. with rights to reacquire commercial rights for North America; XL784, initially an anticancer compound, which completed a Phase I clinical trial and is being advanced as a treatment for renal disease; XL647, XL999, XL880 and XL820, anticancer compounds currently in Phase I clinical trials; XL844 and XL184, anticancer compounds for which investigational new drug applications (INDs) have been filed; and multiple compounds in preclinical development for diseases including cancer and various metabolic and cardiovascular disorders. Exelixis has established broad corporate alliances with major pharmaceutical and biotechnology companies including GlaxoSmithKline (GSK) and Bristol-Myers Squibb Company. Pursuant to a product development and commercialization agreement between Exelixis and GSK, GSK has the option, after completion of Phase IIa clinical trials by Exelixis, to elect to develop a certain number of compounds in Exelixis' product pipeline, which may include the cancer compounds identified in this press release (other than XL119 but including XL784), thus potentially triggering milestone payments and royalties from GSK and co-promotion rights by Exelixis. For more information, please visit the company's web site at http://www.exelixis.com/.

This press release contains forward-looking statements, including without limitation all statements related to Exelixis' clinical development plans for XL647, XL999 and XL784, which include the anticipated timing and design of such trials; and the therapeutic and commercial potential of XL119, XL784, XL647, XL999, XL880, XL820, XL844 and XL184, other compounds in the Exelixis preclinical pipeline and its program in metabolic diseases. Words such as "believes,""anticipates,""plans,""expects,""intends,""will,""slated,""goal" and similar expressions are intended to identify forward-looking statements. These forward-looking statements are based upon Exelixis' current expectations. Forward-looking statements involve risks and uncertainties. Exelixis' actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of these risks and uncertainties, which include, without limitation, the ability to successfully conduct the clinical trials for XL119, XL784, XL647, XL999, XL880, XL820, XL844 and XL184; the ability of the company to advance additional preclinical compounds into clinical development; the uncertainty of the FDA approval process; and the therapeutic and commercial value of the company's compounds. These and other risk factors are discussed under "Risk Factors" and elsewhere in our quarterly report on Form 10-Q for the quarter ended June 30, 2005 and other filings with the Securities and Exchange Commission. Exelixis expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein to reflect any change in the company's expectations with regard thereto or any change in events, conditions or circumstances on which any such statements are based.

NOTE: Exelixis and the Exelixis logo are registered U.S. trademarks.

Exelixis, Inc.

CONTACT: Charles Butler, Associate Director, Corporate Communications,of Exelixis, Inc., +1-650-837-7277, or cbutler@exelixis.com

Web site: http://www.exelixis.com/

Source: PRNewswire-FirstCall

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