Successful proof-of-concept for Inositec's lead candidate

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06.02.2020
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Results from multiple preclinical studies for Inositec's lead candidate INS-3001, a novel cardiovascular calcification inhibitor, showed that the drug candidate significantly reduced the effects of cardiovascular calcification. The treatment could be a potential alternative for patients suffering from the deleterious effects of cardiovascular calcification.

Inositec, a spinoff from the ETH Zurich, is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable Inositune technology to adjust the chemical and physical properties of inositol phosphate (IP6) analogs, the startup is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders.

Calcification, particularly in arterial walls and cardiac valves, leads to an increase in cardiac events. Its lead candidate, INS-3001, aims at addressing a number of cardiovascular indications caused by calcification, including aortic valve stenosis.

In its preclinical studies, a small library of IP6 analogs was synthesized and screened for their ability to inhibit calcification and for their resistance towards hydrolysis. INS-3001 displayed superior efficacy, as well as more favourable pharmacokinetics and tolerability profiles than IP6. It potently stabilized calciprotein particle growth and consistently demonstrated low micromolar activity in different in-vitro models of cardiovascular calcification. INS-3001 also largely abolished the development of cardiovascular calcification in rodent models, without causing toxicity related to serum calcium chelation.

Consequently, Inositec ascertained that its INS-3001 was a potent and well-tolerated inhibitor of pathological soft tissue calcification and a pharmacokinetic profile that could make it a potential treatment alternative for a wide variety of patients suffering from the harmful effects of cardiovascular calcification.

The data was published in Nature Communications, hence validating the efficacy of Inositec's treatment.

“We have rigorously validated the scientific foundations supporting the role of INS-3001 in several potential therapeutic indications, the first of which that Inositec will be targeting is aortic valve stenosis,” stated Mattias Ivarsson, CEO of Inositec.

(Press release/ran)

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