Table 3

Factor XI inhibitors in phase 2 and 3 clinical trials

Type of drugDrugMechanism of actionAdministration routePopulation, comparator (acronym, NCT)
Antisense oligonucleotidesFesomersen (IONIS-FXI-LRx/ISIS 416858/BAY2306001)Inhibits FXI mRNAs.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 antibodiesAbelacimab (MAA868)Binds and inhibits FXI and FXIas.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 FXIai.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 FXIIai.v. (single dose)• ESKD on chronic haemodyalisis vs. placebo (NCT03612856)**• Prevention of CAT in patients with cancer receiving chemotherapy (NCT04465760)**
MK-2060Binds and inhibits FXIai.v. once a week• ESRD receiving haemodyalisis (NCT05027074)**
REGN9933Binds and inhibits FXIai.v.• TKA vs. enoxaparin and apixaban (NCT05618808)**
Small moleculesAsundexian (BAY 2433334)Binds and inhibits FXIaOral, 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 FXIaOral, 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)**
Type of drugDrugMechanism of actionAdministration routePopulation, comparator (acronym, NCT)
Antisense oligonucleotidesFesomersen (IONIS-FXI-LRx/ISIS 416858/BAY2306001)Inhibits FXI mRNAs.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 antibodiesAbelacimab (MAA868)Binds and inhibits FXI and FXIas.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 FXIai.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 FXIIai.v. (single dose)• ESKD on chronic haemodyalisis vs. placebo (NCT03612856)**• Prevention of CAT in patients with cancer receiving chemotherapy (NCT04465760)**
MK-2060Binds and inhibits FXIai.v. once a week• ESRD receiving haemodyalisis (NCT05027074)**
REGN9933Binds and inhibits FXIai.v.• TKA vs. enoxaparin and apixaban (NCT05618808)**
Small moleculesAsundexian (BAY 2433334)Binds and inhibits FXIaOral, 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 FXIaOral, 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.

Table 3

Factor XI inhibitors in phase 2 and 3 clinical trials

Type of drugDrugMechanism of actionAdministration routePopulation, comparator (acronym, NCT)
Antisense oligonucleotidesFesomersen (IONIS-FXI-LRx/ISIS 416858/BAY2306001)Inhibits FXI mRNAs.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 antibodiesAbelacimab (MAA868)Binds and inhibits FXI and FXIas.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 FXIai.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 FXIIai.v. (single dose)• ESKD on chronic haemodyalisis vs. placebo (NCT03612856)**• Prevention of CAT in patients with cancer receiving chemotherapy (NCT04465760)**
MK-2060Binds and inhibits FXIai.v. once a week• ESRD receiving haemodyalisis (NCT05027074)**
REGN9933Binds and inhibits FXIai.v.• TKA vs. enoxaparin and apixaban (NCT05618808)**
Small moleculesAsundexian (BAY 2433334)Binds and inhibits FXIaOral, 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 FXIaOral, 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)**
Type of drugDrugMechanism of actionAdministration routePopulation, comparator (acronym, NCT)
Antisense oligonucleotidesFesomersen (IONIS-FXI-LRx/ISIS 416858/BAY2306001)Inhibits FXI mRNAs.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 antibodiesAbelacimab (MAA868)Binds and inhibits FXI and FXIas.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 FXIai.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 FXIIai.v. (single dose)• ESKD on chronic haemodyalisis vs. placebo (NCT03612856)**• Prevention of CAT in patients with cancer receiving chemotherapy (NCT04465760)**
MK-2060Binds and inhibits FXIai.v. once a week• ESRD receiving haemodyalisis (NCT05027074)**
REGN9933Binds and inhibits FXIai.v.• TKA vs. enoxaparin and apixaban (NCT05618808)**
Small moleculesAsundexian (BAY 2433334)Binds and inhibits FXIaOral, 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 FXIaOral, 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.

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