Press Release

Turning Point Therapeutics Initiates Phase 1/2 Clinical Study of TPX-0046, a Novel RET/SRC Inhibitor

SAN DIEGO, Nov. 11, 2019 (GLOBE NEWSWIRE) -- Turning Point Therapeutics, Inc. (NASDAQ: TPTX), a precision oncology company developing novel drugs to address treatment resistance, today announced initiation of a Phase 1/2 clinical study of its drug candidate TPX-0046 in patients with advanced solid tumors harboring RET genetic alterations.

TPX-0046 is a compact tyrosine kinase inhibitor (TKI) designed to target tumors with RET alterations and potentially overcome resistance that may develop in patients previously treated with other RET inhibitors.

“TPX-0046 was designed to tackle treatment resistance and specifically solvent front mutations that may emerge from current approved and investigational RET inhibitors,” said Alexander Drilon, M.D., medical oncologist and research director of the Early Drug Development Service, Memorial Sloan Kettering Cancer Center, and a principal investigator for the TPX-0046 clinical study.

The Phase 1/2 open-label, single-arm, multi-center clinical study is designed to enroll TKI-treatment naïve and -pretreated patients with RET-altered non-small-cell lung, thyroid, and other advanced cancers in a Phase 1 dose escalation portion of approximately 50 patients, and Phase 2 expansion portion of approximately 300 patients with multiple cohorts, to assess safety, tolerability, pharmacokinetics (PK) and clinical activity. The study design allows intra-patient dose escalation based on tolerability.

“TPX-0046 has the potential to address an unmet treatment need and we are excited to begin this Phase 1/2 clinical study,” said Athena Countouriotis, M.D., president and CEO of Turning Point Therapeutics. “The study also represents an important milestone for the company as TPX-0046 is our third internally designed drug candidate to advance in the clinic since June, and I am incredibly proud of our team that initiated this trial just weeks after IND clearance.”

In preclinical studies against proxy molecules for other investigational selective RET inhibitors presented recently at the 2019 congress of the European Society for Medical Oncology, TPX-0046 showed comparable potency against wildtype KIF5B-RET and stronger potency against the solvent front mutation RET G810R.

TPX-0046 is a multi-targeted RET and SRC kinase inhibitor with a novel three-dimensional macrocyclic structure that is smaller and structurally distinguished from other investigational RET inhibitors. Activation of RET-- a receptor tyrosine kinase --through gain-of-function mutations or fusions has been found in multiple tumor types, including non-small-cell lung and thyroid cancers. Dual inhibition 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.

About Turning Point Therapeutics Inc.
Turning Point Therapeutics is a clinical-stage precision oncology company with a pipeline of internally discovered investigational drugs designed to address key limitations of existing cancer therapies. The company’s lead program, repotrectinib, is a next-generation kinase inhibitor targeting genetic drivers of non-small cell lung cancer and advanced solid tumors. Repotrectinib, which is currently being studied in a registrational Phase 2 study, has shown antitumor activity and durable responses among kinase inhibitor treatment-naïve and pre-treated patients. The company’s pipeline of drug candidates also includes TPX-0022, targeting MET, CSF1R and SRC, which is currently being studied in a Phase 1 trial of patients with advanced or metastatic solid tumors harboring genetic alterations in MET; and TPX-0046, targeting RET and SRC, which is currently being studied in a Phase 1/2 trial of patients with advanced or metastatic solid tumors harboring genetic alterations in RET. Turning Point’s kinase inhibitors are designed to bind to their targets with greater precision and affinity than existing therapies, with a novel, compact structure that has demonstrated an ability to potentially overcome treatment resistance common with other kinase inhibitors. The company is driven to develop therapies that mark a turning point for patients in their cancer treatment. For more information, visit

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 SEC. All forward-looking statements contained in this press release speak only as of the date on which they were made. Turning Point Therapeutics undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made.

Jim Mazzola


Source: Turning Point Therapeutics, Inc.

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