Advancing Integrin-Based Drug Discovery and Development
Our team has unmatched expertise in integrin biology and integrin drug development. We are focused on discovering and developing novel targeted therapies to address life-threatening diseases. Our research is regularly published in a variety of forums and presented at medical and scientific conferences.
Papers
IPF
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Dual αvβ6 and αvβ1 Inhibition Over 12 Weeks Reduces Active Type 1 Collagen Deposition in Individuals with Idiopathic Pulmonary Fibrosis: A Phase 2, Double-Blind, Placebo-controlled Clinical Trial
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Bexotegrast shows dose-dependent integrin αvβ6 receptor occupancy in lungs of participants with idiopathic pulmonary fibrosis: A Phase 2, open-label clinical trial
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(Supplement) Bexotegrast in patients with idiopathic pulmonary fibrosis: The INTEGRIS-IPF study
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Bexotegrast in patients with idiopathic pulmonary fibrosis: The INTEGRIS-IPF study
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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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Selective αv integrin depletion identifies a core, targetable molecular pathway that regulates fibrosis across solid 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 αvβ6 cystine knot PET tracers to detect cancer and idiopathic pulmonary fibrosis
PSC
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TGF-β as a driver of fibrosis: physiological roles and therapeutic opportunities
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The αvβ1 integrin plays a critical in vivo role in tissue fibrosis
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Selective αv integrin depletion identifies a core, targetable molecular pathway that regulates fibrosis across solid 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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Integrin αvβ6 is a marker of the progression of biliary and portal liver fibrosis and a novel target for antifibrotic therapies
Posters & Presentations
IPF
ERS September 2025
ATS May 2025
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Characterizing the antifibrotic activity of bexotegrast on distinct fibroblast populations in PCLS from multiple ILD subtypes
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(Oral Presentation) Characterizing the antifibrotic activity of bexotegrast on distinct fibroblast populations in PCLS from multiple ILD subtypes
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Plasma proteome analysis reveals shared and unique biomarkers of ILD subtypes
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Single-cell profiling demonstrates the antifibrotic effects of bexotegrast on pathologic lung cell populations in the Presence and Absence of Background Therapy
ICALF October 2024
ERS September 2024
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Post-hoc biomarker analysis in participants with IPF receiving bexotegrast over 12-weeks in INTEGRIS-IPF
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(Oral Presentation) Safety and tolerability of bexotegrast in Phase 2 trials of idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC)
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Safety and tolerability of bexotegrast in Phase 2 trials of idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC)
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(Oral Presentation) Bexotegrast reduces type 1 collagen deposition in participants with idiopathic pulmonary fibrosis (IPF) after 12 weeks of therapy
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Bexotegrast reduces type 1 collagen deposition in participants with idiopathic pulmonary fibrosis (IPF) after 12 weeks of therapy
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Bexotegrast is antifibrotic in precision-cut lung slices prepared from fibrotic interstitial lung disease explants
ATS May 2024
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(Oral Presentation) Update on the safety and tolerability of bexotegrast, a dual-selective inhibitor of integrins αvβ6 and αvβ1, in development for idiopathic pulmonary fibrosis and primary sclerosing cholangitis
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(E-Poster) Update on the safety and tolerability of bexotegrast, a dual-selective inhibitor of integrins αvβ6 and αvβ1, in development for idiopathic pulmonary fibrosis and primary sclerosing cholangitis
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Evaluation of quantitative imaging in a Phase 2a study for the treatment of idiopathic pulmonary fibrosis with bexotegrast (INTEGRIS-IPF)
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Bexotegrast targets TGF-β inhibition to specific cell types in the fibrotic human lung
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Post-hoc analysis of biomarkers of interstitial lung disease progression in participants with idiopathic pulmonary fibrosis receiving bexotegrast over 12-weeks in INTEGRIS-IPF
ERS September 2023
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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
Gordon Research Conference August 2023
ATS June 2023
ATS May 2022
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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
ATS May 2020
ERS September–October 2019
PSC
British Society of Gastroenterology (BSG) Live 2025
AASLD November 2024
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Bexotegrast, an oral inhibitor of αvβ6 and αvβ1 integrins, was shown to improve markers and symptoms of cholestasis and stabilized markers of liver fibrosis in participants with primary sclerosing cholangitis: Week 24 results from the Phase 2 INTEGRIS-PSC trial
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Identification of novel inflammatory serum and urinary protein biomarkers for PSC
ERS September 2024
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(Oral Presentation) Safety and tolerability of bexotegrast in Phase 2 trials of idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC)
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Safety and tolerability of bexotegrast in Phase 2 trials of idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC)
EASL June 2024
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Dual alpha-v/beta-6 and alpha-v/beta-1 integrin inhibitor bexotegrast targets TGF-beta inhibition to specific cell types in human liver explant tissue with biliary fibrosis
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Oral alpha-v/beta-6 and alpha-v/beta-1 integrin inhibitor bexotegrast in primary sclerosing cholangitis: Updated 12-week interim safety and efficacy analysis of the INTEGRIS-PSC Phase 2a trial
ATS May 2024
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(Oral Presentation) Update on the safety and tolerability of bexotegrast, a dual-selective inhibitor of integrins αvβ6 and αvβ1, in development for idiopathic pulmonary fibrosis and primary sclerosing cholangitis
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(E-Poster) Update on the safety and tolerability of bexotegrast, a dual-selective inhibitor of integrins αvβ6 and αvβ1, in development for idiopathic pulmonary fibrosis and primary sclerosing cholangitis
AASLD November 2023
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Oral αvβ6/αvβ1 integrin inhibition in primary sclerosing cholangitis: 12-week interim safety and efficacy analysis of INTEGRIS-PSC, a Phase 2a trial of bexotegrast
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Inhibition of integrin αVβ1 attenuates profibrogenic gene expression by myofibroblasts in fibrotic human liver explants
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Dual αVβ6/αVβ1 integrin inhibitor bexotegrast attenuates profibrogenic gene expression across multiple pathologic cell types in human liver explant tissue with biliary fibrosis
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Oral αVβ6/αVβ1 integrin inhibition in primary sclerosing cholangitis: 12-week interim safety and efficacy analysis of INTEGRIS-PSC, a phase 2a trial of bexotegrast
Gordon Research Conference August 2023
EASL June 2023
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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
AASLD November 2019
Oncology
SITC November 2023
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Phase 1a trial of PLN-101095, an integrin αvβ8 and αvβ1 inhibitor, as monotherapy and in combination with pembrolizumab, in treatment-resistant patients with advanced or metastatic solid tumors
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Integrin αvβ1 is expressed in multiple solid tumors and drives the adhesion of cancer-associated fibroblasts to latent TGF-β
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Selective targeting of integrins αVß8 and αVß1 within the dynamic ecosystem of pancreatic cancer to improve overall anti-tumor response