techandprod

Pipeline

A new class of drugs

Inositec is building a pipeline of first-in-class drugs based on inositol phosphate (IP6), with lead programs targeting cardiovascular and renal calcification disorders, as well as Clostridium difficile infection (CDI). These Inositune™ molecules have been fine-tuned to address specific therapeutic indications.

Calcification Inhibitors

Inositec is developing drug candidates based on IP6 that have been designed specifically to possess superior potency and pharmacokinetics that will provide significant patient benefit.

The build-up of calcium and/or phosphate in the blood can lead to mineral deposits, particularly in the cardiovascular system. This is due to a loss in control of factors in the blood that regulate mineral balance in the body.

These deposits lead to a stiffening and/or occlusion of arterial walls and heart valves, ultimately leading to:

  • stenosis
  • left ventricular hypertrophy
  • reduced coronary blood flow
  • compromised endothelial function
  • damage to the microcirculation in various organs

This dysfunctional cardiovascular system causes symptoms such as shortness of breath, reduced exercise capacity, fainting, heart rhythm disturbances and chest pain. Moreover, cardiovascular events and all-cause mortality increases with progression of calcifications. These effects are particularly marked in patients with chronic kidney disease or diabetes.

In the kidneys, the build-up of calcium oxalate crystals damages the renal epithelium and excessive crystal growth can result in the formation of kidney stones. This can result in severe pain and/or loss of kidney function.

There is a significant unmet need for therapeutic agents capable of reducing pathological crystallization processes regardless of their root cause. To date, there is no approved therapy for treating calcification-dependent cardiovascular disease. The therapeutics developed by Inositec are being designed to potently inhibit the crystallization process in soft tissues.

INS-3001

The lead vascular calcification inhibitor, INS-3001, is being developed to treat a number of diseases driven by cardiovascular calcification:

  • Aortic valve stenosis, for which no pharmacological treatment exists and patients must wait for the severity of their condition to degrade until risky valve replacement is necessary.
  • Arterial stiffness in stage 3-4 chronic kidney disease patients, a population of over 100 million patients globally, leading to left ventricular hypertrophy, reduced coronary perfusion and chronic heart failure.

INS-6015

The InosituneTM platform has generated molecules with potential to treat renal calcification disorders, characterized by the production of recurrent kidney stones. Inositec will initially target the unmet medical need faced by patients suffering from recurrent kidneys stones caused by rare conditions, which are considered orphan indications.

Clostridium difficile inhibitors

Inostitec has discovered orally active, small molecule compounds, in particular INS-5010, that irreversibly inhibit Clostridium difficile toxins.

The symptoms C. difficile infection (CDI) causes are mainly produced by two highly similar protein toxins (toxin A and toxin B) that are secreted by the bacterium once it arrives in the colon. Inhibiting the action of these toxins reduces inflammation and damage to the colon. Alleviating these symptoms also helps promote a more rapid regeneration of the intestinal microbiota. This could lead to reduced infection recurrence rates, since individuals with a healthy microbiota generally do not show symptoms from C. difficile carriage.

Inositec is seeking partners for further development of the CDI program.