Aptamer thrombin complex for use as an antidote to direct acting thrombin inhibitors

Simple SummaryContent extracted from patent full text and abstract with AI.

This invention describes a medical complex comprising thrombin (an enzyme involved in blood clotting) and a specially designed aptamer (a short nucleic acid sequence that binds to thrombin). When combined, the aptamer binds thrombin in such a way that the thrombin loses its normal clot-forming activity but remains reactive to direct acting thrombin inhibitors (DTIs), such as dabigatran and argatroban. This complex serves as a targeted antidote that can neutralize the effects of these anticoagulant drugs in cases of overdose or dangerous bleeding, without increasing the risk of blood clots.

Use CasesContent extracted from patent full text and abstract with AI.

• Emergency reversal of anticoagulant effects in patients treated with direct acting thrombin inhibitors (DTIs) during uncontrolled or life-threatening bleeding events.
• Preparation of patients on DTI therapy for urgent surgical or invasive procedures by safely neutralizing the anticoagulant effect.
• Treatment of DTI overdose to quickly restore hemostasis.
• Development of safer protocols for DTI use by providing a reliable reversal agent.
• Use in both therapeutic and prophylactic contexts where rapid neutralization of DTIs is required.

BenefitsContent extracted from patent full text and abstract with AI.

• Provides a universal, specific antidote for multiple DTIs (including dabigatran, argatroban, and others), improving patient safety.
• Reduces the risk of excessive bleeding or hemorrhage associated with DTI therapy by allowing immediate reversal.
• Avoids pro-thrombotic side effects seen with other reversal strategies as the thrombin in the complex is inactivated for clotting functions by the aptamer.
• Rapid onset of action demonstrated in trials (both in vitro and in vivo), enabling timely intervention.
• Does not require development of drug-specific antibodies, which can cause immune reactions or are limited to single drugs.
• Suitable for use in various pharmaceutical formulations and routes of administration.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to a complex formed by thrombin and a thrombin-binding aptamer, said complex is capable of neutralizing the activity of a direct acting thrombin inhibitor, and to a use as an antidote to blood anticoagulants selected from direct acting thrombin inhibitors.