PLN-101095

PLN-101095 is an orally bioavailable small molecule inhibitor that selectively targets the integrins αvβ8 and αvβ1 in the tumor microenvironment. By binding to these integrins, it blocks their interaction with the latency-associated peptide of transforming growth factor-beta (TGF-β), thereby preventing TGF-β activation. This mechanism aims to overcome resistance to immune checkpoint inhibitors by reducing TGF-β–mediated immunosuppression, promoting T-cell infiltration, and enhancing anti-tumor immune responses. Developed by Pliant Therapeutics, PLN-101095 is being evaluated primarily for use in patients with advanced or metastatic solid tumors that are resistant to immune checkpoint inhibitors such as pembrolizumab. Interim Phase 1 data have shown antitumor activity and a favorable safety profile[1][2][3][4][5][6].

Other names

alphaVbeta1/8 inhibitor PLN-101095