TP-101

TP-101 is an investigational FAP-activated prodrug of the multi-kinase inhibitor ponatinib, developed by TRACT BIO for the treatment of solid tumors. Utilizing the company's stemECHO platform, TP-101 is designed to target pathogenic cancer stem cells (CSCs) within the tumor microenvironment that are often resistant to standard therapies. The drug is engineered to remain inactive in systemic circulation and is selectively activated by Fibroblast Activation Protein alpha (FAP), an enzyme highly expressed by cancer-associated fibroblasts in the stroma of many solid tumors. Upon cleavage by FAP, the active payload ponatinib is released, which inhibits a broad spectrum of tyrosine kinases including BCR-ABL, VEGFR, FGFR, and PDGFR. This targeted activation mechanism is intended to enhance the therapeutic index of ponatinib by concentrating its activity at the tumor site while minimizing systemic toxicities. TP-101 is currently in the IND-enabling stage of development.

Other names

FAP-activated ponatinibFAP-ponatinib