fasitibant (MEN 16132) / Menarini - LARVOL DELTA

Non-peptide bradykinin B2 receptor ligands possessing the substituted quinolinyl moiety: pharmacological properties and prospective clinical uses. (PubMed, Peptides) - "FR173657, fasitibant, anatibant, deucrictibant and Compound 3 (the non-deuterated version of deucrictibant) are examples of competitive antagonists of the human B2 receptor, some of which having reached the stage of clinical trials. Other compounds structurally related to the common moiety, such as FR190997 and Compound 47a, are partial or nearly full agonists of the B2 receptor. The ongoing clinical development of deucrictibant for the treatment of hereditary angioedema is a first step in clarifying the therapeutic potential of orally bioavailable B2 receptor antagonists."

Journal • Review • Cardiovascular • Complement-mediated Rare Disorders • Hereditary Angioedema

Involvement of Bradykinin B2 Receptor in Pathological Vascularization in Oxygen-Induced Retinopathy in Mice and Rabbit Cornea. (PubMed, Int J Mol Sci) - "...Blockade of B2R signaling by the antagonist fasitibant delayed retinal vascularization in mouse pups, indicating that the retinal endothelium is a target of the BK/B2R system...In agreement with these results, in the OIR model, a blockade of B2R signaling significantly reduced retinal neovascularization, as determined by the area of retinal tufts, and, in the retinal vessel, it also reduced vascular endothelial growth factor and fibroblast growth factor-2 expression. All together, these findings show that B2R blockade reduces retinal neovascularization and inhibits the expression of proangiogenic and pro-inflammatory cytokines, suggesting that targeting B2R signaling may be an effective strategy for treating ischemic retinopathy."

Journal • Preclinical • Age-related Macular Degeneration • Biosimilar • Cardiovascular • Immunology • Ophthalmology • Reperfusion Injury

The BDKRB2 +9/-9 Polymorphisms Influence Pro-Inflammatory Cytokine Levels in Knee Osteoarthritis by Altering TLR-2 Expression: Clinical and in Vitro Studies. (PubMed) - Cell Physiol Biochem - "The data suggested that the BDKRB2 +9/-9 polymorphisms influence pro-inflammatory cytokine levels in knee osteoarthritis by altering TLR-2 expression."

Journal • Biosimilar • Immunology • Osteoarthritis • Pain