Turning Point Therapeutics Announces FDA Clearance of Investigational New Drug Application for TPX-0046, a Novel RET/SRC Inhibitor
Under the IND, the company plans to initiate a Phase 1/2 first-in-human, open-label clinical study later this year. The phase 1 portion will have a dose-finding design, including intra-patient dose escalation to assess the safety, tolerability, and preliminary clinical activity of TPX-0046 in patients with advanced or metastatic solid tumors harboring oncogenic RET fusions or mutations. The phase 2 portion will evaluate the preliminary efficacy of TPX-0046 in multiple cohorts of patients with advanced or metastatic sold tumors harboring oncogenic RET fusions or mutations.
“TPX-0046 was rationally designed to address treatment resistance that we believe may develop following the use of current investigational RET inhibitors as well as other multi-targeted approved RET inhibitors,” said Athena Countouriotis, M.D., president and chief executive officer. “Similar to our lead asset, repotrectinib, our preclinical work supports a potential role for TPX-0046 in both TKI-naïve and TKI-pretreated patients, and we look forward to initiating our Phase 1/2 study later this year. Clearing our second IND this year and advancing our third clinical drug candidate are major milestones for our company, as we seek to bring new therapies to market to address high unmet medical needs in difficult to treat cancers.”
Preclinical studies of TPX-0046 demonstrate potent inhibition of wildtype and mutated RET kinases as compared to proxy chemical compounds for investigational RET inhibitors, LOXO-292 and BLU-667. In cellular assays, TPX-0046 showed comparable potency against wildtype KIF5B-RET and stronger potency against the G810R solvent front mutation. These studies were presented on
TPX-0046 is a multi-targeted RET and SRC kinase inhibitor with a novel three-dimensional macrocyclic structure. Activation of RET-- a receptor tyrosine kinase --through gain-of-function mutations and fusions has been found in multiple tumor types, including lung and thyroid cancers. Dual inhibitor of RET and SRC represents a novel therapeutic strategy to target abnormal RET signaling in cancers. Inhibition of SRC family kinases has the potential to reduce recruitment of multiple receptor tyrosine kinases involved in bypass resistance and therefore has the potential to increase the therapeutic effect of TPX-0046.
Forward Looking Statements
Statements contained in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995. Such forward-looking statements include statements regarding, among other things, the efficacy, safety and therapeutic potential of TPX-0046, the results, conduct and timing of Turning Point Therapeutics’ clinical trials, and plans regarding future clinical trials. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward-looking statements. Words such as “plans”, “will”, “believes,” “anticipates,” “expects,” “intends,” “goal,” “potential” and similar expressions are intended to identify forward-looking statements. These forward-looking statements are based upon Turning Point Therapeutics’ current expectations and involve assumptions that may never materialize or may prove to be incorrect. Actual results could differ materially from those anticipated in such forward-looking statements as a result of various risks and uncertainties, which include, without limitation, risks and uncertainties associated with Turning Point Therapeutics’ business in general, and the other risks described in Turning Point Therapeutics’ filings with the
Source: Turning Point Therapeutics, Inc.