Table 1. Strategies to inhibit FXI or... | American Society of Hematology

Table 1.

Strategies to inhibit FXI or FXII

Agents	Target
Agents	FXI	FXII
ASOs	Reduce hepatic synthesis of FXI by inducing catalytic degradation of FXI mRNA (eg, IONIS-416858)*^,†	Reduce hepatic synthesis of FXII by inducing catalytic degradation of FXII mRNA
Monoclonal antibodies	Suppress FXIa generation and/or inhibit FXIa activity (eg, BAY1213790 (osocimab),^,† BAY1831865, MAA868, AB023)	Bind to FXII and block its activation (eg, 9A2, 15H8, AB052)
Monoclonal antibodies		Bind to FXIIa and blocks its activity (eg, CSL312,* 3F7)
Small peptidomimetic or peptide inhibitors	Bind to catalytic domain (eg, BMS-986177,*^,† EP-7041, ONO-5450598)	Bind to catalytic domain (eg, rHA-infestin 4, FXII618, 3-carboxamide coumarins)
Aptamers	Bind to FXI and/or FXIa and block its activity (eg, 11.16, 12.7)	Bind to FXII and/or FXIIa and block FXI activation (eg, R4cXII-1)

Agents	Target
Agents	FXI	FXII
ASOs	Reduce hepatic synthesis of FXI by inducing catalytic degradation of FXI mRNA (eg, IONIS-416858)*^,†	Reduce hepatic synthesis of FXII by inducing catalytic degradation of FXII mRNA
Monoclonal antibodies	Suppress FXIa generation and/or inhibit FXIa activity (eg, BAY1213790 (osocimab),^,† BAY1831865, MAA868, AB023)	Bind to FXII and block its activation (eg, 9A2, 15H8, AB052)
Monoclonal antibodies		Bind to FXIIa and blocks its activity (eg, CSL312,* 3F7)
Small peptidomimetic or peptide inhibitors	Bind to catalytic domain (eg, BMS-986177,*^,† EP-7041, ONO-5450598)	Bind to catalytic domain (eg, rHA-infestin 4, FXII618, 3-carboxamide coumarins)
Aptamers	Bind to FXI and/or FXIa and block its activity (eg, 11.16, 12.7)	Bind to FXII and/or FXIIa and block FXI activation (eg, R4cXII-1)

mRNA, messenger RNA.

Under evaluation in phase 2 clinical trials.

Discussed in text.