Fibrotic diseases lead to progressive loss of tissue function and organ failure and are estimated to contribute ~45% of deaths in the developed world. Idiopathic pulmonary fibrosis (IPF) is one of these and is poorly treated with a survival rate lower than that of most cancers. It is characterised by excessive scarring - unregulated wound healing - in the lung with transforming growth factor (TGF) thought to play a pivotal role. Integrins are cell surface receptors (involved in cell adhesion inter alia) involved in activating TGF and it is thought that their inhibition - and in particular the integrin αvβ6 - may have a therapeutic benefit in treating IPF. This presentation will focus on our work on the synthesis and properties of αvβ6 inhibitors which led to a clinical candidate.

The design, synthesis and optimization of αvβ6 antagonists as potential idiopathic pulmonary fibrosis agents

ACS Spring Meeting 2021

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