World-Class Drug

Development Capabilities

Bexotegrast (PLN-74809) is an oral small-molecule dual-selective inhibitor of α_vβ₆ and α_vβ₁ integrins for the treatment of IPF and PSC.

While present at very low levels in healthy tissues, these integrins are upregulated in the lungs of IPF patients and the bile ducts of PSC patients where they activate TGF-β, a key driver of the fibrotic process. Blocking these integrins is designed to stop TGF-β activation, potentially halting the growth of scar tissue.

Bexotegrast (PLN-74809) is an oral small-molecule dual-selective inhibitor of α_vβ₆ and α_vβ₁ integrins for the treatment of IPF and PSC.

While present at very low levels in healthy tissues, these integrins are upregulated in the lungs of IPF patients and the bile ducts of PSC patients where they activate TGF-β, a key driver of the fibrotic process. Blocking these integrins is designed to stop TGF-β activation, potentially halting the growth of scar tissue.

Our oncology program focuses on selective inhibition of α_vβ₈, an integrin that can activate TGF-β in the tumor microenvironment, causing an anti-inflammatory effect and potential resistance to immuno-oncology therapeutics such as checkpoint inhibitors.

Muscular dystrophy comprises a group of inherited diseases, all characterized by inborn errors in dystrophin, a protein that anchors muscle cells to the extracellular matrix and facilitates contraction.  The lack of dystrophin results in muscle cell damage upon contraction, causing a progressive loss of muscle function over time.

Our second product candidate, PLN-1474, is a small-molecule selective inhibitor of α_vβ₁ for the treatment of late stage liver fibrosis associated with nonalcoholic steatohepatitis (NASH). The integrin α_vβ₁ activates TGF-β in the liver, leading to fibrosis and, potentially, liver failure.