Biochem/physiol Actions

CPHPC (Miridesap; Ro 63-8695) is an orally active serum amyloid P (SAP) blocker that targets the ligand-binding site on the SAP planar binding (B) face with each of its two D-proline moieties (up to two SAP per CPHPC), being able to crosslink and dimerize two SAP pentamers to form B face-to-B face decamers. CPHPC potently inhibits SAP binding to amyloid fibrils in vitro (IC50 = 0.9 µM using AD Aβ amyloid fibrils) and exhibits in vivo efficacy toward liver & circulating SAP clearance as well as SAP removal from tissue amyloid deposits (1-5 mg/mL in drinking water; human SAP transgenic mice).