Modified relaxin polypeptides comprising a pharmacokinetic enhancer and pharmaceutical compositions thereof
The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
1. An isolated modified relaxin polypeptide comprising the structure:
wherein said AQ1-Relaxin comprises a relaxin A chain polypeptide of SEQ ID NO: 35 and a relaxin B chain polypeptide of SEQ ID NO: 6, wherein the modified para-acetyl-L-phenylalanine depicted in Formula III is located at the N-terminus of said relaxin A chain polypeptide.
2. A pharmaceutical composition comprising the isolated modified relaxin polypeptide of claim 1 , wherein said pharmaceutical composition is suitable for parenteral administration.