Cemtirestat disulfid – a prodrug of an inhibitor of aldo-keto reductase

The solution uses a strategy based on the administration of a prodrug (cemtirestat disulfide) of the active drug (cemtirestat). In this strategy (prodrug strategy), the active drug is released after chemical or metabolic activation of the inactive prodrug at the site of desired effect. This approach can significantly increase the availability of the drug at the site of action and reduce toxicity compared to direct drug administration.

Competitive advantage

• targeted distribution of effective drug into cancer cells, which can lead to higher efficiency and reduced side effects (compared to cemtirestat);
• expected higher efficiency also with respect to the symmetry of cemtirestat disulfide and the provision of two molecules of effective AR inhibitor (cemtirestat) at once;
• increased selectivity of action, thanks to the effective conversion of the prodrug to cemtirestat bound to the naturally increased reducing environment of tumors;
• expected better absorbability of cemtirestat disulfide in the acidic environment of tumors (compared to cemtirestat), thanks to its higher lipophilicity.

Use of technology

• in the field of treatment of cancer originating in chronic inflammation, namely cancer of colon, lung, breast, liver, prostate, pancreas, endometrium and cervix;
• for the treatment of cancer as an adjuvant therapeutic in combination with clinically used chemotherapeutics that are substrates of aldo-keto reductases.

For download

• Marketing brief

Protection of intellectual property

• Patent application: (SK)