Turning Point Therapeutics to Present Data from Four Studies at AACR Annual Meeting

Studies Demonstrate Potent Activity of the Company’s Kinase Inhibitors Against Targeted Oncogene Drivers and their Mutations

SAN DIEGO — Turning Point Therapeutics, Inc., a clinical-stage precision oncology company developing novel drugs that address treatment resistance, will present preclinical data next month highlighting the potent activity of its kinase inhibitors against targeted oncogene drivers and their mutations.

Four studies were accepted for presentation during poster sessions at the American Association for Cancer Research (AACR) Annual Meeting taking place March 29 to April 3 in Atlanta, including two presentations that further characterize lead clinical asset, repotrectinib, in tumor cells with clinically reported ROS1 and NTRK fusions and their corresponding mutations.

“The pervasive challenge of kinase mutations that lead to treatment resistance has limited the effectiveness of approved and investigational kinase inhibitors,” said Athena Countouriotis, M.D., chief executive officer. “Our team has developed a pipeline of novel, small compact kinase inhibitors that have demonstrated early preclinical and clinical effectiveness against targeted gene fusions and their mutations. We are pleased to share several of our preclinical studies at AACR as we continue to generate clinical evidence for our lead asset repotrectinib in our ongoing Phase 1/2 TRIDENT-1 study.”

The preclinical antitumor activities of Turning Point’s TPX-0022, a MET/CSF1R/SRC inhibitor, will be presented for the first time in two poster presentations. TPX-0022 was designed to target not only MET-driven tumor cells by potent inhibition of MET/SRC signaling, but also modulate the tumor microenvironment by inhibition of CSF1R. This dual modulation has demonstrated significant tumor growth inhibition in preclinical models.

The four studies to be presented are:

Title: Repotrectinib, a next generation TRK inhibitor, overcomes TRK resistance mutations including solvent front, gatekeeper and compound mutations
Sunday Mar 31, 2019, 1:00 PM – 5:00 PM
Abstract Number: 4000

Title: Repotrectinib, a new generation ROS1 inhibitor, is highly potent against fusion ROS1s and emerging resistance mutations
Session: Monday April 1, 2019, 8:00 AM – 12:00 PM
Abstract Number: 4832

Title: TPX-0022, a polypharmacology inhibitor of MET/CSF1R/SRC for treatment of cancers with abnormal HGF/MET signaling
Session: Monday April 1, 2019, 8:00 AM – 12:00 PM
Abstract Number: 3719

Title: TPX-0022, a polypharmacology inhibitor of MET/CSF1R/SRC inhibits tumor growth by promoting anti-tumor immune responses
Session: Monday April 1, 2019, 8:00 AM – 12:00 PM
Abstract Number: 3749

Turning Point Therapeutics lead drug candidate, repotrectinib, is being evaluated for the treatment of patients with ROS1+ advanced non-small-cell lung cancer (NSCLC) and patients with ROS1+, NTRK+ or ALK+ advanced solid tumors. A multi-cohort Phase 2 registrational study is planned for the second half of 2019. The company is also developing two multi-targeted kinase inhibitors — TPX-0046, a novel RET/SRC inhibitor, and TPX-0022, a novel MET/CSF1R/SRC inhibitor — and next-generation ALK inhibitors.

About Repotrectinib
Repotrectinib (TPX-0005) is a potent and orally bioavailable investigational small molecule kinase inhibitor of ROS1, TRKs and ALK. The clinical benefits of targeting ROS1, TRK, or ALK fusion kinases have been demonstrated with multiple kinase inhibitors already approved or in clinical studies. The successes of these therapies are often overshadowed by the development of acquired resistance. The acquired solvent front mutations including ROS1 G2032R, TRKA G595R and TRKC G623R, and ALK G1202R render common clinical resistance to the current ROS1, TRK, and ALK inhibitors.

Repotrectinib has demonstrated potency against wildtype and mutated ROS1, TRK and ALK kinases, especially the clinically significant solvent front mutations, gatekeeper mutations, and emerging compound mutations after multiple lines of treatment. Repotrectinib may provide a new opportunity to inhibit the abnormal signaling of ROS1, TRK or ALK in solid malignancies, and overcome multiple resistance mechanisms seen in resistant patients. Repotrectinib is currently being evaluated in a Phase 1/2, open-label, multi-center, first-in-human study of the safety, tolerability, pharmacokinetics and anti-tumor activity in patients with advanced solid tumors harboring ALK, ROS1, or NTRK1-3 rearrangements TRIDENT-1 study (www.clinicaltrial.gov number NCT03093116). Interested patients and physicians can also contact the TP Therapeutics Oncology Clinical Trial Hotline at 1-858-276-0005 or email clinical@tptherapeutics.com.

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 has shown antitumor activity and durable responses among kinase inhibitor treatment-naïve and pre-treated patients, and is planned to enter a registrational Phase 2 study in the second half of 2019. 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 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 www.tptherapeutics.com.


Turning Point Therapeutics, Inc.
Jim Mazzola