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Avacopan (CCX168) is an oral small-molecule antagonist of the complement C5a receptor 1 (C5aR1). It is used in combination with standard immunosuppressive therapies—specifically cyclophosphamide or rituximab, and glucocorticoids—for the treatment of severe active ANCA-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis). By blocking C5aR1, avacopan inhibits C5a-mediated neutrophil activation and migration, which are central to the pathogenesis of vasculitis. This combination regimen was specifically evaluated in the Phase 2 CLASSIC trial to assess the safety and efficacy of adding avacopan to standard-of-care regimens, with the goal of maintaining disease control while potentially reducing high-dose glucocorticoid exposure.
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