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THE DEVELOPMENT OF NEW BLOOD CLOTTING INHIBITORS BASED ON PHARMACOLOGICAL AGENTS ADJUSTING THE ENZYMATIC ACTIVITY OF THROMBIN AND FACTOR XA


Purpose of the development: Proposed development of therapeutic agents that control blood clotting during surgery or extensive burns and selectively directed to the inhibition of activated Factor Xa and thrombin.

Recommended application field: Drugs capable of regulating blood clotting, are widely used in military medicine, the specifics of which are largely connected with the violation of the integrity of the body and burns a large body surface.

Advantages over analogues: Compared to heparin and its analogues direct thrombin inhibitors have important advantages which make it advisable to use these expensive drugs (3-day course of therapy stoet US $ 1000) in the treatment of pathological states for which heparin therapy is not effective.

The development stage readiness: Finishing off is required

Description of the development:
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Any injury and related surgery leads to significant activation of the blood coagulation system. A large number of patients die as a result of development of thrombotic complications. Even more, this picture is shown in burns. Violation of the blood coagulation system leads to the development of intra-vascular blood microcoagulation (ECC syndrome), which is accompanied by the activation of the blood coagulation system, followed by coagulopathy and organ failure. Therefore, any surgery is not without agents that are capable of regulating both blood coagulation during it, and in the postoperative period. The most commonly used drugs are heparin and further vitamin K antagonists (warfarin, coumarin et al.). However, these drugs have a number of drawbacks that limit the frequency of use, effectiveness and safety of the action: the need for constant laboratory control, a large number of drugs and metabolic interactions narrow therapeutic range and the associated danger of severe bleeding complications. The new drug will have a set of specific properties: controllability anticoagulation (absence of bleeding complications, decrease the required level of laboratory monitoring); the presence of the dosage form for internal use; a convenient mode of application (the smallest multiplicity results in improving compliance with recommendations and reduce the likelihood of missing the next dose); flexibility (simplified definition of an adequate dose); accessibility (low cost). Due to the performance in 2012 was created a library of thrombin inhibitors and factor Xa (more than 4000 connections), a list of recommendations on the synthesis of potential inhibitors of these enzymes, carried out their sampling of existing collections, and held more than 1,000 chemical synthesis of new chemical compounds. In general, more than 5,000 obtained prototypes of chemical compounds in an amount of 10-100 mg of which at the beginning of 2014 in 33 revealed inhibitory properties against thrombin enzymatic activity at 10 degrees -7 - 10 -9 mol degree, and 43 inhibitor factor Xa activity with a 10 degree -6 - 10 -7 mol degree. Type of partner sought - a medical facility, based on which will be carried out medical tests, the result of which will be prepared by the protocols of medical tests and developed guidelines for the medical use of the complex, which will provide the certificate of state registration, which authorizes the use of the product in medical practice and introducing it into production.

Information about newness of the development:


ноу-хау--
1 шт.

corresponds technical description
Reguires revision

Possibility of transfer abroad:
Creation of joint enterprise

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Country Ukraine

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