

Advancing Discoveries in Fibrosis
Our team has unmatched expertise in fibrosis biology and is focused on discovering and developing novel targeted therapies to address life-threatening fibrotic diseases. Our research in a variety of forums is regularly published and presented at medical and scientific conferences.
Papers
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Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF
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TGF-β as a driver of fibrosis: physiological roles and therapeutic opportunities
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Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness
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Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations
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The integrin αvβ6 binds and activates latent TGF beta 1: a mechanism for regulating pulmonary inflammation and fibrosis
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The αvβ1 integrin plays a critical in vivo role in tissue fibrosis
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Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs
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Epithelial-mesenchymal interactions in fibrosis and repair. Transforming growth factor-β activation by epithelial cells and fibroblasts
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Evaluation of integrin αvβ 6 cystine knot PET tracers to detect cancer and idiopathic pulmonary fibrosis
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Integrin αvβ6 is a marker of the progression of biliary and portal liver fibrosis and a novel target for antifibrotic therapies
Posters & Presentations
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Safety, Tolerability and Antifibrotic Activity of Bexotegrast: Phase 2a INTEGRIS-IPF Study (NCT04396756)
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Circulating ITGB6 Levels Are Elevated in Patients with Idiopathic Pulmonary Fibrosis and Reduced Following Lung Transplant
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Dual αvβ6/αvβ1 Integrin Inhibitor Bexotegrast Reduces Fibrogenesis in Pathological Cell Populations Present in the Fibrotic Human Lung
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INTEGRIS-PSC Phase 2a Study: Evaluating the Safety, Tolerability, and Pharmacokinetics of Bexotegrast (PLN-74809) in Participants with Primary Sclerosing Cholangitis
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Dual alpha-v/beta-6 and alpha-v/beta-1 Integrin Inhibitor Bexotegrast Attenuates Profibrogenic Gene Expression of Myofibroblasts in Human Liver Explant Tissue with Biliary Fibrosis
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Non-invasive Imaging Method Demonstrates Anti-fibrotic Efficacy of a Dual Integrin alpha-v/beta-6 and alpha-v/beta-1 Inhibitor in a Rat Model of Biliary Fibrosis
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Single nuclei RNA-seq profiling of fibrotic human precision-cut tissue slices: a model for evaluating anti-fibrotic therapies in lung and liver
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Dual αVβ6/αVβ1 Integrin Inhibitor PLN-74809 Attenuates Pathologic Fibroblasts in Human Fibrotic Lung Explant Tissue
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PLN-74809 Shows Favorable Safety and Tolerability and Indicates Antifibrotic Activity in a Phase 2a Study for the Treatment of Idiopathic Pulmonary Fibrosis
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INTEGRIS-PSC Phase 2a Study: Evaluating the Safety, Tolerability, and Pharmacokinetics of Bexotegrast (PLN-74809) in Participants with Primary Sclerosing Cholangitis
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Dual alpha-v/beta-6 and alpha-v/beta-1 Integrin Inhibitor Bexotegrast Attenuates Profibrogenic Gene Expression of Myofibroblasts in Human Liver Explant Tissue with Biliary Fibrosis
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Non-invasive Imaging Method Demonstrates Anti-fibrotic Efficacy of a Dual Integrin alpha-v/beta-6 and alpha-v/beta-1 Inhibitor in a Rat Model of Biliary Fibrosis
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Combining Dual αVβ6/αVβ1 Integrin Inhibitor, PLN-74809, With Standard-of-Care Therapies Has a Synergistic Effect on Reducing Fibrogenic Gene Expression in Fibrotic Human Lung Slices
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PLN-74809, A dual-selective inhibitor of integrins αvβ6 and αvβ1 shows dose-dependent target engagement in the lungs of patients with idiopathic pulmonary fibrosis (IPF)
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PLN-74809, an oral, dual-selective αvβ6/αvβ1 inhibitor in phase 2 clinical trials for idiopathic pulmonary fibrosis (IPF), sustainably reduces transforming growth factor-beta (TGF-β) activity in the lungs of healthy participants with once-daily dosing
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PLN-74809, a dual-selective inhibitor of αvβ6 and αvβ1, is well tolerated in over 280 healthy participants
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Therapeutic biomarker discovery in idiopathic pulmonary fibrosis (IPF) through proteomic analysis of precision-cut lung slice (PCLS) supernatants
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Pharmacological inhibitors of integrin αvβ6 that differentially modulate protein conformation are similarly effective at inhibiting TGF- β signaling in the fibrotic lung
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Profiling fibrosis regression in a rat model of non-alcoholic steatohepatitis
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PK/PD assessment of an oral, selective αVβ6 /αVβ1 integrin dual antagonist, PLN-74809, for the treatment of idiopathic pulmonary fibrosis
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Dual αVβ6 /αVβ1 inhibitor PLN-74809 blocks multiple TGF-β activation pathways associated with IPF
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PLN-74809, a dual αVβ6/αVβ1 integrin inhibitor, inhibits fibrosis in precision-cut liver tissue from PSC and PBC patients and the Mdr2 knockout mouse
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PLN-74809, a dual αvβ6/αvβ1, oral, selective integrin inhibitor, is well tolerated and reduces lung TGF-β activity in healthy volunteers
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Selective Small Molecule Inhibitor of Integrin αvβ8 and αvβ1 Has Single Agent Activity and Potentiates Immune Checkpoint Blockade Therapy