Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases

Our integrated drug discovery efforts on the Relaxin-2 peptide hormone, in collaboration with our collaborators at global life sciences company Sanofi, has produced a paper just published in the Journal of Medicinal Chemistry.
The natural peptide hormone human relaxin-2 has a complex heterodimeric insulin-like structure that makes its chemical synthesis tractability quite challenging.
The goal of our collaboration was to reduce the chemical complexity and optimize the hormone to a highly potent single B-chain Relaxin-2, with sustained duration of action and an improved half-life suitable for once daily administration.
The new class of RXFP1 agonists described in J.Med. Chem. paper have long-lasting properties that are compatible with once daily sub-cutaneous administration in patients. This approach opens the door to new treatments for chronic fibrosis and cardiovascular diseases.