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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

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TP Therapeutics, a privately held, clinical-stage biopharmaceutical
company developing oncology therapies with a focus on addressing drug
resistance, announced today that updated interim data from its ongoing
Phase 1/2 TRIDENT-1 study of Repotrectinib (TPX-0005) will be presented
in an oral presentation at the International Association for the Study
of Lung Cancer (IASLC) 19th World Conference on Lung Cancer to be held
Sept. 23-26, 2018, in Toronto.

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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