We are focused on advancing the development of tecarfarin, a Phase 3-ready, anticoagulant designed using a retrometabolic drug design process that targets a different pathway than the most commonly prescribed drugs used in the treatment of rare cardiovascular conditions.
The FDA has granted orphan drug designation (ODD) for heart failure patients with left ventricular assist devices (LVADs) as well as both ODD and fast track designation for the prevention of systemic thromboembolism of cardiac origin in patients with end-stage kidney disease (ESKD) plus atrial fibrillation (AFib).
Tecarfarin has been evaluated in 11 human clinical trials in over 1,000 individuals. In Phase 1, Phase 2 and Phase 2/3 clinical trials, tecarfarin has generally been well-tolerated in healthy adults and patients with ESKD and chronic kidney disease (CKD).
Key milestones
Tecarfarin is Phase 3-ready with a positive safety profile.
We have established that tecarfarin has a well-established and reversible mechanism of action and demonstrated that tecarfarin’s elimination from the body was not affected by severe kidney dysfunction.
Tecarfarin has been evaluated in 11 clinical trials in over 1.000 subjects: 269 patients were treated for at least 6 months and 129 patients were treated for one year or more.
In Phase 1, Phase 2, and Phase 2/3 clinical trials, tecarfarin has generally been well tolerated in both healthy adult subjects and patients with ESKD.
Clinical Trials
In a Phase 2/3 randomized and blinded trial, 607 patients with indications for chronic anticoagulation were treated with either tecarfarin or warfarin. The Time in Therapeutic Range, or TTR, with tecarfarin was similar to that with well-managed warfarin and tecarfarin appeared to have a favorable safety profile and be well tolerated with only 1.6% of the blinded tecarfarin subjects suffering from major bleeding and no thrombotic events. When thrombotic and major bleeding events during the blinded period were combined, a numerical imbalance favoring tecarfarin over warfarin was seen (warfarin 11 subjects, 3.6 %; tecarfarin 5 subjects, 1.6 %).
In a subsequent Phase 1 study with 23 patients with chronic kidney disease, the metabolism of warfarin was inhibited, but not tecarfarin. The safety of repeated dosing of tecarfarin in CKD patients remained unknown. However, if the pharmacokinetic findings of this single-dose study are present with repeated dosing, tecarfarin may lead to dosing that is more predictable than warfarin in CKD patients who require anticoagulation therapy.
