SAR443809: a selective inhibitor of the complement alternative pathway, targeting complement factor Bb.

ABSTRACT: Dysregulated activation of the complement system is implicated in the onset or progression of several diseases. Most clinical-stage complement inhibitors target the inactive complement proteins present at high concentrations in plasma, which increases target-mediated drug disposition and necessitates high drug levels to sustain therapeutic inhibition. Furthermore, many efforts are aimed at inhibiting only terminal pathway activity, which leaves opsonin-mediated effector functions intact. We describe the discovery of SAR443809, a specific inhibitor of the alternative pathway C3/C5 convertase (C3bBb). SAR443809 selectively binds to the activated form of factor B (factor Bb) and inhibits alternative pathway activity by blocking the cleavage of C3, leaving the initiation of classical and lecti

SUBMITTER: Rajagopal V 

PROVIDER: S-EPMC10424147 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature