Drug intelligence / Profile preview

ralpancizumab

Development stage
Phase 1
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Subcutaneous, Intravenous
01

Overview

Ralpancizumab (PF-05335810) is a specifically engineered, pH-sensitive, humanized monoclonal antibody that targets proprotein convertase subtilisin/kexin type 9 (PCSK9). Developed by Pfizer for the treatment of hypercholesterolemia and dyslipidemia, it functions as a PCSK9 inhibitor. By binding to PCSK9 protein, ralpancizumab prevents its interaction with low-density lipoprotein receptors (LDLR), thereby increasing LDLR availability on hepatocyte surfaces and enhancing clearance of LDL cholesterol from the bloodstream. Ralpancizumab demonstrated a longer half-life and greater bioavailability compared to bococizumab in clinical studies. The drug was well tolerated in phase I trials but its development was discontinued after phase I[1][2][3][4][5][9].

Other names
ralpancizumabRN317RN-317RN 317
02

Targets

PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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