Bexotegrast (PLN-74809) Bexotegrast (PLN-74809)

Bexotegrast (PLN-74809)

Our lead product candidate, bexotegrast (PLN-74809), is an oral, small molecule, dual-selective inhibitor of αvβ6 and αvβ1 being developed for the treatment of idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC).


While expressed at very low levels in normal tissues, αvβ6 and αvβ1 integrins are upregulated in the pulmonary tissues of IPF patients, and in the liver tissues of PSC patients. Both of these integrins serve as activators of TGF-ß, leading to increased collagen production and, ultimately, fibrosis in these tissues. By blocking the activation of TGF-ß by both αvβ6 and αvβ1, we believe bexotegrast (PLN-74809) may slow and potentially halt the progression of fibrosis in these patient populations.

A part of IPF and PSC scheme

Program Highlights

  • Bexotegrast (PLN-74809) has shown a favorable safety tolerability and pharmacokinetic profiles in a Phase 2a trial
  • Good oral bioavailability and long half-life are promising for potential once-daily dosing
  • Bexotegrast (PLN-74809) in a Phase 2a trial was well tolerated over 12 weeks of treatment with no drug-related severe or serious adverse events
  • Bexotegrast (PLN-74809) at 320 mg dose in a Phase 2a trial demonstrated statistically significant increase in FVC, an FDA approvable endpoint, at 4, 8 and 12 weeks of treatment
  • Targeting of tissue-specific integrins is designed to maximize antifibrotic effect while avoiding systemic effects of TGF-β inhibition
  • There are currently only two existing FDA-approved therapies for IPF; while both have shown modest slowing of disease progression, medical need remains high
  • There are currently no FDA-approved therapies for PSC

Development Status

  • Global Phase 2a PSC trials enrolling
  • Granted Orphan Drug Designation from FDA and EMA in IPF and PSC
  • Granted Fast Track Designation from FDA in IPF
  • Positive data from Phase 2a IPF trial announced