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- Title
Third generation PCSK9-inhibitors.
- Authors
Laufs, Ulrich; Blüher, Matthias; Isermann, Berend
- Abstract
Graph: Graphical Abstract Strategies to inhibit the proprotein convertase subtilisin/kexin type 9 (PCSK9). Targeting the proprotein convertase subtilisin/kexin type 9 (PCSK9) by monoclonal fully human antibodies (AB) and small interfering RNA (siRNA) has revolutionized the pharmocological armamentarium for lowering LDL-cholesterol (LDL-C)[1],[2] (Graphical Abstract). Third generation PCSK9 inhibitors in phase 2 and 3 of their clinical development programmes are lerodalcibep, a fusion protein that consists of a synthetic anti-PCSK9-binding domain (adnectin) bound to human serum albumin and MK-0616, a macrocyclic peptide that binds to PCSK9 and is orally bioavailable.
- Subjects
PILLS; LDL cholesterol; SYNTHETIC proteins; PYROPHOSPHATES
- Publication
European Heart Journal, 2023, Vol 44, Issue 40, p4281
- ISSN
0195-668X
- Publication type
Article
- DOI
10.1093/eurheartj/ehad566