angioedema

Fexofenadine hydrochloride (Terfenidine carboxylate hydrochloride) is a second generation antihistamine that is used for the treatment of allergic rhinitis, angioedema and chronic urticaria.

LSP-249 is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.

Avoralstat (BCX4161) is an oral plasma kallikrein (PKK) inhibitor. Which is used for the treatment of hereditary angioedema.

Berotralstat (BCX7353) is a second-generation, synthetic, and orally active plasma kallikrein inhibitor with low toxicity. It is highly specific and effectively used in the research of hereditary angioedema (HAE) attacks. Berotralstat functions by inhibiting the enzymatic activity of plasma kallikrein, which is responsible for the release of bradykinin. This blocking mechanism targets the major biologic peptide involved in the promotion of swelling and pain associated with HAE attacks[1][2].

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

Icatibant Acetate, an antagonist of the bradykinin B2 receptor, is used in the treatment of hereditary angioedema.

KKI-5 acetate is a serine protease inhibitor that inhibits kallikrein and plasmin. KKI 5 may exhibit anticancer chemotherapeutic benefit and may also be used as a treatment for angioedema.

Ecallantide (DX-88), a recombinant inhibitor targeting plasma kallikrein, impedes bradykinin synthesis and is used to prevent acute episodes of angioedema [1].

KKI 5 is a serine protease inhibitor that inhibits kallikrein and plasmin. KKI 5 may exhibit anticancer chemotherapeutic benefit and may also be used as a treatment for angioedema.

Lanadelumab (SHP643), a humanized IgG1 monoclonal antibody, targets plasma kallikrein (pKal) with a K i value of 0.12 nM, effectively inhibiting both its free form and its interaction with high molecular weight kininogen (HMWK)-bound pKal. This compound shows promise for hereditary angioedema research [1] [2].

Carbinoxamine, an anticholinergic and antihistamine agent, is used for hay fever, angioedema, vasomotor rhinitis, mild urticaria, dermatographism and allergic conjunctivitis. It is a histamine antagonist, specifically an H1-antagonist.

Ecallantide (DX-88) TFA, a specific recombinant plasma kallikrein inhibitor, directly inhibits bradykinin production and is indicated for the prevention of acute angioedema attacks [1].

Plasma kallikrein-IN-2, a potent inhibitor of plasma kallikrein (PKal) with an inhibitory concentration (IC) 50 value of 0.1 nM, is utilized in research targeting hereditary angioedema, diabetic macular edema, and diabetic retinopathy.

Garadacimab (CSL312) is a potent whole-human IgG4 monoclonal antibody targeting activation factor XII (FXIIa). Garadacimab can be used to study hereditary angioedema.