TP Therapeutics Announces Updated Interim Phase 1 Data with Repotrectinib (TPX-0005) in ROS1 Fusion-positive NSCLC to be Presented at World Conference on Lung Cancer

The presentation will provide an updated interim analysis of the Phase 1 study in ROS1 fusion-positive non-small-cell lung cancer (NSCLC) patients across multiple doses of Repotrectinib, TP Therapeutics’ investigational next-generation tyrosine kinase inhibitor (TKI) designed to effectively target ROS1, TRKA-C and ALK fusion proteins, and overcome clinical resistance due to secondary kinase domain mutations. Preclinical and early clinical findings have shown Repotrectinib to be a potent and selective inhibitor for ALK, ROS1, and TRK family.

World Conference on Lung Cancer
Presentation Title: Safety and Preliminary Clinical Activity of Ropotrectinib¹ (TPX-0005), a Next-Generation ROS1/TRK/ALK Inhibitor, in Advanced ROS1 Fusion-Positive Non-Small Cell Lung Cancer
Topic: Targeted Therapy
Date: Monday, Sept. 24, 2018
Session: Novel Therapies in ROS1, HER2 and rare EGFR Mutations (10:30 a.m. to Noon)
Abstract: 14217
Presenter: Jessica J. Lin, M.D., Massachusetts General Hospital Cancer Center

Initial preliminary data from the ongoing Phase 1 portion of the TRIDENT-1 study were presented in June 2018 at the annual meeting of the American Society of Clinical Oncology (ASCO). In addition, the preclinical and clinical proof-of-concept data for Repotrectinib were recently published in the journal Cancer Discovery (The Cancer Discovery article may be found online at: http://cancerdiscovery.aacrjournals.org/content/early/2018/08/09/2159-8290.CD-18-0484?papetoc=).

About repotrectinib (TPX-0005)

Repotrectinib (TPX-0005) is a potent and orally bioavailable investigational small molecule kinase inhibitor for ALK, ROS1, and TRK family. The clinical benefits of targeting ALK, ROS1, or TRK fusion kinase have been demonstrated with multiple kinase inhibitors already approved for the treatment of ALK+ non-small cell lung cancer (NSCLC), in addition to crizotinib for ROS1+ NSCLC, and larotrectinib and entrectinib in clinical studies for TRK+ cancers. The successes of these therapies are overshadowed by the development of acquired resistance. The acquired solvent front mutations including ALK G1202R, ROS1 G2032R, TRKA G595R and TRKC G623R render a common clinical resistance to the current ALK, ROS1, and TRK inhibitors.

Repotrectinib has demonstrated potency against wildtype and mutated ALK, ROS1 and TRK family kinases, especially the clinically significant solvent front mutations, gatekeeper mutations, and emerging compound mutations after multiple line treatments. Repotrectinib may provide a new opportunity to inhibit the abnormal signaling of ALK, ROS1, or TRK family in solid malignancies, and overcome multiple resistance mechanisms seen in refractory 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.

¹Note: TPX-0005 had an initial generic name of “ropotrectinib,” which was later changed to repotrectinib and is now the accepted name by USAN and WHO INN.

About TP Therapeutics, Inc.

TP Therapeutics, Inc. (TP) is a clinical-stage structure-based oncology drug design company founded in October 2013 by Dr. J. Jean Cui, the lead inventor of Pfizer’s oncology drug crizotinib and lorlatinib. The TP team is focused on the design and development of novel chemical entities within oncology for established oncogene drivers with high incidence of secondary resistance mutations; newly identified disease-driven targets; and potential targets regulating the tumor microenvironment and tumor immunity. For more information, please visit us at www.tptherapeutics.com.

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