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Table 1 Approved drugs with targets in the kallikrein-kinin system

From: Recent advances in the discovery and development of drugs targeting the kallikrein-kinin system

Drug

Class

Approved indication

Ref

C1 esterase inhibitor

 Human C1 esterase inhibitor

Protein replacement therapy

Hereditary angioedema (on-demand and prophylaxis)

[110,111,112]

 Conestat alfa

Protein replacement therapy

Hereditary angioedema (on-demand)

[117]

Coagulation factor XII

 Garadacimab/CSL312

Monoclonal antibody (fully human)

Hereditary angioedema (prophylaxis)

[27]

Plasma (P) and tissue (T) kallikrein

 Berotralstat (P)

Small molecule inhibitor

Hereditary angioedema (prophylaxis)

[57, 58]

 Ecallantide (P)

Inhibitor, protein

Hereditary angioedema (on-demand)

[53, 54]

 Lanadelumab (P)

Monoclonal antibody (fully human)

Hereditary angioedema (prophylaxis)

[55, 56]

 Aprotinin (P, T)

Inhibitor, protein

Reduction of perioperative blood loss

[87,88,89,90,91,92]

 Ulinastatin (P, T)

Inhibitor, protein

Sepsis, pancreatitis

[95, 96]

 Human urinary kallidinogenase (T)

Enzyme replacement therapy

Acute ischemic stroke

[101]

Bradykinin B2 receptor

 Icatibant

Peptide antagonist

Hereditary angioedema (on-demand)

[121, 122]

  1. (P) and (T) indicate whether plasma (P) or tissue (T) kallikrein is the drug target