On November 29, 2016 Ignyta, Inc. (Nasdaq: RXDX), a biotechnology company focused on precision medicine in oncology, reported its first disclosed preclinical data on RXDX-106—its potent, selective, type II pseudo-irreversible inhibitor of TYRO3, AXL and MER (or TAM) and c-MET—will be presented at the 2016 EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) (ENA) Molecular Targets and Cancer Therapeutics Symposium in Munich, Germany, highlighting both the immuno-oncology and targeted therapeutic activity of this novel agent (Press release, Ignyta, NOV 29, 2016, View Source [SID1234516832]). Additionally, the company will present data on multiple compounds in clinical development from its robust pipeline of molecularly targeted oncology therapies, including entrectinib—an orally available, CNS-penetrant tyrosine kinase inhibitor targeting tumors that harbor TRK, ROS1 or ALK fusions—and RXDX-105—a VEGFR-sparing, potent RET inhibitor.
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"We are pleased to introduce preclinical data on RXDX-106 at ENA alongside our promising clinical data for entrectinib and RXDX-105," said Jonathan Lim, M.D., Chairman and CEO of Ignyta. "RXDX-106 is an intriguing, novel agent that may offer a dual mechanism by potentiating the immune system, while also providing selective activity against key molecular targets involved in both primary oncogenesis and resistance."
In the presented preclinical data on RXDX-106, researchers demonstrated that the agent is a potent and selective inhibitor of TAM and c-MET, and inhibited TAM-mediated and c-MET-mediated tumor growth in vivo. Additionally, researchers demonstrated, via in vitro and in vivo studies, that RXDX-106, as a single agent, appears to release the molecular brakes on immune activation in macrophages, NK cells, and T cells, resulting in the repolarization of the immune response to elicit an anti-tumor effect. Furthermore, emerging in vivo combination data suggest that RXDX-106 potentiates the activity of anti-PD-1 and anti-CTLA-4 agents. These data further support the continued evaluation of RXDX-106 in both a preclinical and clinical setting (Abstract number 73, Poster number P044; Abstract number 65, Poster number P036).
Also presented as part of this poster session were preclinical data on RXDX-105 demonstrating significant anti-tumor activity in models harboring RET fusions (Abstract number 85, Poster number P056), as well as preclinical data on entrectinib showing potent anti-tumor activity in multiple different tumor model systems driven by NTRK1/2/3, ROS1 and ALK fusions, regardless of the fusion partners or the tumor tissue of origin (Abstract number 78, Poster number P049). Additional clinical data on RXDX-105 and entrectinib will be presented later in the week at ENA.