Entrectinib – Targeting NTRK and ROS1 Fusions
Currently undergoing STARTRK-2, a global, potentially registration enabling Phase 2 clinical trial, entrectinib is a potent, CNS-active, orally available, selective tyrosine kinase inhibitor of the TRKA, TRKB, TRKC and ROS1 proteins. This product candidate was designed to target cancers harboring activating molecular alterations to the corresponding subset of oncogenes. Learn more about gene fusions in cancer, data from the entrectinib ongoing Phase I and Phase II trials, and clinical responses. Click here to Learn more about Entrectinib (RXDX-101), and NTRK and ROS1 Fusions as well as data from the entrectinib ongoing Phase I and Phase II trials, and clinical responses.
RXDX-105 – Targeting RET and Other Kinase Targets
An orally available, VEGF-sparing, potent RET inhibitor. A Phase Ib basket study of RXDX-105 has completed enrollment.
Learn more about RET fusions.
Taladegib – Targeting Hh/SMO
A small molecule hedgehog/smoothened inhibitor. In normal cells, the hedgehog molecule acts as a ligand that can bind the smoothened transmembrane receptor and set off a signaling cascade that can influence early development and replication of adult stem cell populations. Stem cells that acquire molecular changes activating the hedgehog/smoothened pathway can transform into tumor precursors; this process has been implicated in some forms of brain cancer, skin cancer, and pancreatic cancer. Targeting these stem cells in combination with other therapeutics could potentially help eradicate residual disease.
RXDX-106 – Targeting TYRO3, AXL, MER
RXDX-106 is a novel small molecule immunomodulatory agent with potent anti-tumor activity, alone and in combination with checkpoint inhibitors, that appears to restore and enhance overall immune function by reversing immunosuppression of innate immune cells in the tumor microenvironment (TME) through TYRO3, AXL, and MER (TAM) receptor tyrosine kinase (RTK) inhibition that is in late preclinical development.
Learn more about Pan-TAM Inhibitors.