Drug intelligence / Profile preview

trimeric apolipoprotein A-I

Development stage
Discontinued
Lead developer
Roche
Modality
Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

Trimeric apolipoprotein A-I (TripA-I) is a recombinant biologic drug candidate engineered to treat atherosclerosis and cardiovascular disease. It consists of human apolipoprotein A-I (apoA-I) fused to the trimerization domain of human tetranectin, resulting in a trimeric structure with a higher molecular weight than native monomeric apoA-I. This protein engineering approach extends the plasma half-life to approximately 36 hours (compared to 16 hours for monomeric apoA-I) by reducing renal filtration. TripA-I mimics the anti-atherogenic functions of native apoA-I, specifically promoting reverse cholesterol transport (RCT) through ABCA1-dependent and independent pathways and stimulating lecithin-cholesterol acyltransferase (LCAT) to facilitate cholesterol esterification. The drug was designed to reduce atherosclerotic plaque progression and provide anti-inflammatory benefits. Originally developed by Borean Pharma, the program was acquired by Roche in 2006 during the preclinical lead optimization stage.

Other names
trimerized apolipoprotein A-IapoA-I-tetranectin fusion protein
02

Targets

LCAT (Lecithin-cholesterol acyltransferase)ABCA1 (ATP-binding cassette transporter A1)

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