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PL-2100 (also referred to as PLN-2100) is a potent and selective small molecule inhibitor of the αvβ1 integrin, developed by Pliant Therapeutics for the treatment of fibrotic diseases. The αvβ1 integrin is primarily expressed on fibroblasts and plays a critical role in the mechanical activation of latent transforming growth factor-beta (TGF-β), a master cytokine that drives the fibrotic response. By specifically targeting the αvβ1 subtype, PL-2100 prevents the release of active TGF-β into the extracellular matrix, thereby inhibiting collagen deposition and tissue scarring in organs such as the lungs, liver, and kidneys. Preclinical studies have demonstrated that PL-2100 can significantly attenuate fibrosis in models of idiopathic pulmonary fibrosis (IPF) and liver fibrosis (NASH), offering a targeted therapeutic approach that aims to avoid the potential toxicities associated with broader, non-selective integrin inhibition.
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