Table 3.
Factor XI inhibitors in phase 2 and 3 clinical trials
| Type of drug | Drug | Mechanism of action | Administration route | Population, comparator (acronym, NCT) |
|---|---|---|---|---|
| Antisense oligonucleotides | Fesomersen (IONIS-FXI-LRx/ISIS 416858/BAY2306001) | Inhibits FXI mRNA | s.c. (weekly) | • ESKD on chronic haemodyalisis vs. placebo (NCT02553889; EMERALD, NCT03358030)**• TKA vs. enoxaparin (NCT01713361)** |
| FXI-LICA (BAY2976217) | Same RNA sequence as IONIS-FXIRX conjugated with GalNAc | • ESRD on haemodialysis (RE-THINc), ESRD (NCT04534114)** | ||
| Monoclonal antibodies | Abelacimab (MAA868) | Binds and inhibits FXI and FXIa | s.c. (monthly) | • AF vs. rivaroxaban (AZALEA-TIMI 71, NCT04755283)**• CAT vs. apixaban (ASTER, NCT05171049)*** or dalteparin (MAGNOLIA, NCT05171075)***• Postoperative VTE after TKA vs. enoxaparin (EudraCT number, 2019-003756-37)** |
| Osocimab (BAY 1213790) | Binds and inhibits FXIa | i.v./s.c. (monthly) | • ESKD on chronic haemodyalisis vs. placebo (CONVERT, NCT04523220)**• Postoperative VTE after TKA vs. enoxaparin or apixaban (FOXTROT, NCT03276143)** | |
| Xisomab 3G3 (AB023) | Binds FXI and blocks its activation by FXIIa | i.v. (single dose) | • ESKD on chronic haemodyalisis vs. placebo (NCT03612856)**• Prevention of CAT in patients with cancer receiving chemotherapy (NCT04465760)** | |
| MK-2060 | Binds and inhibits FXIa | i.v. once a week | • ESRD receiving haemodyalisis (NCT05027074)** | |
| REGN9933 | Binds and inhibits FXIa | i.v. | • TKA vs. enoxaparin and apixaban (NCT05618808)** | |
| Small molecules | Asundexian (BAY 2433334) | Binds and inhibits FXIa | Oral, daily | • AF vs. apixaban (PACIFIC-AF, NCT04218266)**• Post-AMI vs. placebo (PACIFIC-AMI, NCT04304534)**• Brain infarcts and recurrent symptomatic ischaemic stroke vs. DAPT (PACIFIC-STROKE, NCT04304508)** |
| Milvexian (BMS-986177/JNJ‐70033093) | Binds and inhibits FXIa | Oral, daily | • TKA vs. enoxaparin (AXIOMATIC-TKR, NCT03891524)**• Post-acute ischaemic stroke or high-risk transient ischaemic attack vs. SAPT/DAPT (LIBREXIASTROKE, NCT05702034)***• Stroke prevention in patients receiving aspirin and clopidogrel (AXIOMATIC-SSP, NCT03766581)** |
**Phase 2 clinical development. ***Phase 3 clinical development.
AMI, acute myocardial infarction; AF, atrial fibrillation; CAT, cancer-associated thromboembolism; CRT, catheter-related thrombosis in cancer patients; DAPT, dual antiplatelet therapy (aspirin plus clopidogrel); ESKD, end-stage kidney disease; F, coagulation factor; i.v., intravenous; mRNA, messenger RNA; SAPT, single antiplatelet therapy; s.c., subcutaneous; TKA, total knee arthroplasty; VTE, venous thromboembolism.