Hybrigenics Files Patent Application For High-yield Inecalcitol Production

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-based chemotherapy for the hormone-refractory stage.

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.” The new and inventive chemical process is now protected by a worldwide patent application procedure.

Rémi Delansorne, CEO of Hybrigenics, said: “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. Our strategy is to optimize all components of inecalcitol development and to build several intellectual property barriers around it.”