Table 2. Strategies to inhibit factor XI.
Agents | Mechanisms of action of FXI inhibitors |
---|---|
Antisense
oligonucleotides (ASO) |
Reduce hepatic synthesis of FXI by inducing catalytic degradation
of FXI mRNA (for example, IONIS-FXI Rx) a |
Monoclonal antibodies | Suppress FXIa generation and/or inhibit FXIa activity (for example,
BAY1213790 (osocimab) b, MAA868 (abelacimab), AB023) |
Small molecules | Bind to catalytic domain (for example, JNJ-70033093, BAY2433334,
EP-7041, ONO-5450598) |
Aptamers | Bind to FXI and/or FXIa and block its activity |
aFXI ASO for prevention of venous thromboembolism (evaluated in a phase 2 randomized controlled trial: NCT01717761).
bOsocimab (evaluated in a phase 2 randomized, active-comparator-controlled, multi-center study (NCT03276143) to assess the safety and efficacy of different doses of BAY1213790 for the Prevention of Venous Thromboembolism in Patients Undergoing Elective Primary Total Knee Arthroplasty, Open-label to Treatment and Observer-blinded to BAY1213790 Doses (FOXTROT) 36.