Hybrigenics improves inecalcitol synthesis
French firm makes patent application for high-yield inecalcitol production
Hybrigenics has filed a new patent application protecting a crucial step in the synthesis of orally active agonist inecalcitol.
The French biopharmaceutical company focused on r&d of new cancer treatments and specialised in protein interactions, says 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 structure. During the scale-up of the chemical synthesis of inecalcitol, special conditions were found to improve the effectiveness of "14-epimerisation". This 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-epimerisation," said Remi Delansorne, Hybrigenics' ceo. "Our strategy is to optimise all components of inecalcitol development and to build several intellectual property barriers around it."
