Regado Biosciences, Inc, a biopharmaceutical company focused on the discovery and development of actively controllable aptamer therapeutics for the acute care setting, announced the publication in the Journal of Thrombosis and Thrombolysis of data from a single escalating-dose Phase 1 clinical trial of the REG2 anticoagulation system. The published data demonstrates the dose and concentration-dependent attenuation of thrombin generation and subsequent restoration of thrombin following reversal associated with REG2.
REG2 is a two-component system consisting of a subcutaneous depot formulation of pegnivacogin, an anticoagulant aptamer specifically targeting coagulation Factor IXa, and its complementary intravenous injectable oligonucleotide active control agent, anivamersen. REG2 is being developed to be the preferred therapeutic option in high value sub-acute venous thrombosis indications such as DVT and VTE prophylaxis. REG2 will be an important part of the life cycle franchise strategy associated with Revolixys Kit which ultimately entails broad use throughout the hospital.
Christopher Rusconi, Ph.D., Regado's chief scientific officer and co-discoverer of the Regado controllable aptamer technology, commented, "These results support the choice of FIXa as an excellent target for anticoagulant therapy. In addition, the concentration-dependent inhibition of thrombin generation observed in this study further supports the pegnivacogin dose selected for the REGULATE-PCI Phase 3 study of the companion product candidate, Revolixys Kit."
The study included 32 healthy volunteers who were enrolled sequentially into four cohorts. Patients in cohorts 1-3 were randomized (3:1) to ascending doses of pegnivacogin, from 0.5 mg/kg to 3 mg/kg, and placebo, with no anivamersen administered. In cohort 4, all patients received 2 mg/kg open-label pegnivacogin and were randomised (1:1) to reversal by one dose or multiple doses over time of 1 mg/kg anivamersen. Parameters of the CAT assay included time to peak thrombin generation (PTm), endogenous thrombin potential, peak thrombin generation and velocity index (VIx).
REG2 is a clinical-stage product candidate comprising a subcutaneous depot formulation of pegnivacogin paired with an intravenous injection of anivamersen, the specific complementary control agent to pegnivacogin. Pegnivacogin and anivamersen are the same active moieties found in Regado's lead clinical programme, Revolixys Kit. REG2 is formulated to provide a controllable level of anticoagulation for up to two weeks for sub-acute uses, especially in cases where a patient may be unable to swallow an oral anticoagulant.
Regado is developing REG2 for potential uses in a variety of acute and sub-acute care cardiovascular indications such as venous thromboembolism prophylaxis in patients undergoing abdominal surgery, as treatment for transcatheter aortic valve implantation (TAVI) patients and for bridging patients who are unable to take oral anticoagulants for a period of time before or after a surgical procedure.