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TPX-0046 is a multi-targeted orally bioavailable TKI with a novel three dimensional macrocyclic structure that is being developed as a RET and SRC kinase inhibitor. TPX-0046 has the ability to demonstrate clinical activity in both treatment-naïve patients and in patients that develop solvent-front mutations.

TPX-0046 has completed IND-enabling studies and cleared its IND. During the 2H of 2019, we initiated a Phase 1/2 clinical trial of TPX-0046 for the treatment of advanced solid tumors with abnormal RET genes.

A Novel Approach to Target RET Signaling
A dual inhibitor of RET and SRC represents a novel therapeutic strategy to target abnormal RET signaling in cancers.

RET is a receptor tyrosine kinase, and constitutive activation of RET through mutations, amplifications and fusions have been found in multiple tumor types, including lung cancer, thyroid cancer and colon cancer. Importantly, the inhibition of the SRC kinase has the potential to reduce the recruitment of multiple receptor tyrosine kinases involved in bypass resistance and therefore increase the therapeutic effect seen with RET inhibitors. In addition, TPX-0046 does not inhibit VEGFR kinases, which are often associated with cardiovascular toxicities such as hypertension.