Hybrigenics Improves Inecalcitol Synthesis

Paris, March 11, 2010 - Hybrigenics, a bio-pharmaceutical company with a focus on research and development of new cancer treatments and specialized in protein interactions, announced today that it has filed a new patent application protecting a crucial step in the synthesis of inecalcitol. The improved chemical process will allow higher yields and lower costs for future industrial batches. Inecalcitol is currently in Phase II clinical development for prostate cancer.

The originality of the chemical structure of inecalcitol resides in the so-called “14-epimer” conformation of the vitamin D backbone. The lack of hypercalcemic effect and, as a consequence, the excellent tolerance of high doses of inecalcitol, can be explained in part by this unique structural configuration. During the scale-up of the chemical synthesis of inecalcitol, special conditions were found to improve the effectiveness of “14-epimerization”. This new and inventive chemical process is now protected by a worldwide patent application procedure.

“We originally licensed the exclusive patent rights for inecalcitol itself and for part of its synthesis. Last year we filed a patent on the therapeutic use of high doses of inecalcitol, and now we have moved to protect 14-epimerization,” said Rémi Delansorne, Hybrigenics’ CEO. “Our strategy is to optimize all components of inecalcitol development and to build several intellectual property barriers around it.”

About Inecalcitol

Inecalcitol is an orally active agonist targeting the vitamin D receptor. The therapeutic rationale behind its development is to add its cytostatic potential to the established efficacy of the reference treatments of the two stages of prostate cancer: anti-hormonals (LH-RH agonists and anti-androgens) for the hormone-dependent stage and Taxotere(R)-based chemotherapy for the hormone-refractory stage.

About Hybrigenics

Hybrigenics (www.hybrigenics.com) is a bio-pharmaceutical company listed (ALHYG) on Alternext (NYSE-Euronext) in Paris, focusing its internal R&D programs on innovative targets and therapies for the treatment of cancer. Hybrigenics’ development program is based on inecalcitol, a vitamin D analogue, for the treatment of hormone-refractory prostate cancer in combination with Sanofi-Aventis’ Taxotere(R), which is the current gold-standard chemotherapeutic treatment for this indication. Hybrigenics’ research program explores the role of enzymes known as ubiquitin-specific proteases (USP) in the degradation of onco-proteins, and the effectiveness of proprietary USP inhibitors in treating various types of cancer.

Hybrigenics is also the market leader in Yeast-Two Hybrid (Y2H) and related services to identify, validate and inhibit protein interactions for researchers in all areas of life sciences, using its ISO 9001-certified high-throughput Y2H screening platform, its sophisticated bioinformatics tools and extensive database, along with its chemical library and chemical screening platform.

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