Abstract
The complement component C5 inhibitory peptide zilucoplan is currently in phase III clinical trials for myasthenia gravis (MG). Despite being at an advanced stage of clinical development, there have been no published reports in the literature detailing its chemical synthesis. In this work, we describe an approach for the chemical synthesis of zilucoplan and validate that the synthesised compound blocks LPS-induced C5a production from human blood.
Keywords:
C5; C5a; Complement; Peptide synthesis; Peptides; RA101495; Zilucoplan.
MeSH terms
-
Complement C5 / antagonists & inhibitors*
-
Complement C5 / chemical synthesis
-
Complement C5 / chemistry
-
Complement C5 / pharmacology
-
Complement Inactivating Agents / chemical synthesis*
-
Complement Inactivating Agents / chemistry
-
Complement Inactivating Agents / pharmacology
-
Humans
-
Inhibitory Concentration 50
-
Lipopolysaccharides / pharmacology
-
Molecular Structure
-
Peptides, Cyclic / chemical synthesis*
-
Peptides, Cyclic / chemistry
-
Peptides, Cyclic / pharmacology
-
Solid-Phase Synthesis Techniques
Substances
-
Complement C5
-
Complement Inactivating Agents
-
Lipopolysaccharides
-
Peptides, Cyclic
-
zilucoplan