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An established Slovak research institute and Slovak university have developed Cemtirestat disulfide – a new prodrug of an inhibitor of aldo-keto reductases and are looking for a licensee/ investor/buyer

Summary

Profile Type
  • Technology offer
POD Reference
TOSK20240610007
Term of Validity
10 June 2024 - 10 June 2025
Company's Country
  • Slovakia
Type of partnership
  • Commercial agreement with technical assistance
  • Investment agreement
Targeted Countries
  • All countries
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General information

Short Summary
A team of inventors from an established Slovak scientific and research institute and an established Slovak university have developed a new pharmaceutically usable prodrug (cemtirestat disulfide) of a pharmacologically active compound, which is an inhibitor of aldo-keto reductases, in particular aldose reductase. The novel prodrug can be used in the treatment of cancer that originates in chronic inflammation.
The preferred cooperation type are commercial agreement or investment agreement.
Full Description
Aldo-keto reductases are NAD(P)H-dependent oxidoreductases that are best characterized as glucose reducing agents. They are involved in the pathophysiology of diabetic complications. These enzymes also metabolize products of lipid peroxidation, thus contributing in certain circumstances to an inflammatory response. Aldose reductase (AR, AKR1B1), besides being involved in diabetic complications through glucose reduction, effectively reduces aldehydes formed by lipid peroxidation, as well as their conjugates with glutathione, to the corresponding alcohols, which mediate inflammatory signals in the body. It is very well documented that chronic inflammation is associated with cancer progression. Epidemiological studies suggest that more than 25% of all cases of cancer are closely related to chronic infection and chronic inflammation. Increased expression of aldo-keto reductases in tumors of lung, breast, prostate, cervix, testes and colon has been observed, and the role of aldo-keto reductases in the etiology of colorectal carcinoma has been confirmed. Although cemtirestat exhibits effective inhibition of aldo-keto reductases AKR1B1 and AKR1B10, it would be advantageous to improve its pharmacokinetic properties when administered orally and parenterally.
A team of inventors from an established Slovak scientific and research institute and an established Slovak university has managed to solve the above mentioned shortcomings by using a therapeutic strategy based on the administration of a prodrug (cemtirestat disulfide) of the active drug (cemtirestat). In this strategy (prodrug strategy), the release of the active drug occurs 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. Cemtirestat disulfide was synthesized and tested to obtain a prodrug of an effective inhibitor of aldose reductase. Given the key role of aldo-keto reductases AKR1B1 and AKR1B10 in the etiology of several types of cancer associated with chronic inflammation, it is assumed that the release of cemtirestat within tumor cells by reduction of its prodrug would increase the efficiency and especially the selectivity of the drug.
The institutions are looking for a partner to cooperate with via commercial agreement or investment agreement.
Advantages and Innovations
• 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
Stage of Development
  • Lab tested
Sustainable Development Goals
  • Goal 17: Partnerships to achieve the Goal
  • Goal 9: Industry, Innovation and Infrastructure
IPR status
  • IPR granted
IPR notes
Granted patent in Slovak republic
Patent pending in Europe, China & India

Partner Sought

Expected Role of a Partner
The present invention can be used in the field of treatment of cancer originating in chronic inflammation, namely cancer of colon, lung, breast, liver, prostate, pancreas, endometrium and cervix. The present invention can be also used for the treatment of cancer as an adjuvant therapeutic in combination with clinically used chemotherapeutics that are substrates of aldo-keto reductases.
The institute and the Slovak university are looking for a partner to cooperate with via commercial agreement (an investor to further develop this technology is sought or a partner to sell this technology to is sought) or investment agreement (a partner for licensing of this technology is sought).
Type and Size of Partner
  • Big company
  • SME 50 - 249
Type of partnership
  • Commercial agreement with technical assistance
  • Investment agreement

Dissemination

Technology keywords
  • 06001003 - Cytology, Cancerology, Oncology
Market keywords
  • 05005014 - Oncology
Targeted countries
  • All countries