Mark Yarchoan, John D Powderly, Bruno R Bastos, Thomas B Karasic, Oxana V Crysler, Pamela N Munster, Meredith A McKean, Leisha A Emens, Yvonne M Saenger, Yasser Ged, Robert Stagg, Steven Smith, Chan C Whiting, Anne Moon, Peppi Prasit, Yonchu Jenkins, Nathan Standifer, Thomas W Dubensky, Sam H Whiting, Susanna V Ulahannan
PURPOSE: TPST-1120 is a first-in-class oral inhibitor of peroxisome proliferator-activated receptor α (PPARα), a fatty-acid ligand-activated transcription factor that regulates genes involved in fatty acid oxidation, angiogenesis, and inflammation, and is a novel target for cancer therapy. TPST-1120 displayed anti-tumor activity in xenograft models and synergistic tumor reduction in syngeneic tumor models when combined with anti-PD-1 agents. PATIENTS AND METHODS: This phase 1, open-label, dose-escalation study (NCT03829436) evaluated TPST-1120 as monotherapy in patients with advanced solid tumors and in combination with nivolumab in patients with renal cell carcinoma (RCC), cholangiocarcinoma (CCA), or hepatocellular carcinoma...
March 29, 2024: Cancer Res Commun