SALT LAKE CITY, Utah, May 19, 2020 /PRNewswire/ -- Tolero Pharmaceuticals, Inc., a clinical-stage company focused on developing novel therapeutics for hematological and oncological diseases, today announced the submission of an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA) for its investigational small-molecule pyruvate kinase M2 isoform (PKM2) activator, TP-1454. Under this IND, Tolero intends to conduct a Phase 1/1b, first-in-human, open-label, dose‑escalation, safety, pharmacokinetic and pharmacodynamic study, which will evaluate oral TP‑1454 alone, and in combination with ipilimumab and nivolumab, in patients with advanced metastatic or progressive solid tumors.

"The IND submission for TP-1454 represents an important step in advancing Tolero's pipeline of innovative oncology compounds," said David J. Bearss, Ph.D., Chief Executive Officer, Tolero Pharmaceuticals, and Chief Scientific Officer and Global Head of Research, Global Oncology. "TP-1454 will be the first PKM2 activator to be tested in cancer patients, representing a novel mechanism that aims to target the underlying metabolics driving tumor growth and anti-cancer immune suppression. We look forward to building our understanding of the potential role of PKM2 activation in the treatment of solid tumors."

The primary objectives of the study are to establish the safety of oral TP-1454 administered once daily as monotherapy in patients with advanced metastatic or progressive solid tumors and as combination therapy with ipilimumab and nivolumab in patients who are eligible for standard of care treatment. In addition, the study will establish the dose of TP-1454 alone and in combination with ipilimumab and nivolumab for future studies in select tumor types. Secondary objectives include assessing the pharmacokinetic profile and antitumor activity of TP-1454 alone and in combination with ipilimumab and nivolumab and evaluating proof of mechanism of TP-1454.

About TP-1454

TP-1454 is an investigational oral pyruvate kinase M2 isoform (PKM2) activator, that will be evaluated in a Phase 1/1b study in patients with advanced metastatic or progressive solid tumors. TP-1454 will be the first PKM2 activator tested in cancer patients. Pyruvate kinase is the enzyme responsible for catalyzing the last step of glycolysis. PKM2 plays a critical role in the metabolic changes observed in cancer and immune cells and establishes a metabolic advantage for tumor cells over the tumor immune microenvironment.¹

About Tolero Pharmaceuticals, Inc.

Tolero Pharmaceuticals is a clinical-stage biopharmaceutical company researching and developing treatments to improve and extend the lives of patients with hematological and oncological diseases. Tolero has a diverse pipeline that targets important biological drivers of blood disorders to treat leukemias, anemia, and solid tumors, as well as targets of drug resistance and transcriptional control.

Tolero Pharmaceuticals is based in the United States and is an indirect, wholly-owned subsidiary of Sumitomo Dainippon Pharma Co., Ltd., a pharmaceutical company based in Japan. Tolero works closely with its parent company, Sumitomo Dainippon Pharma, and Boston Biomedical, Inc., also a wholly-owned subsidiary, to advance a pipeline of innovative oncology treatments. The organizations apply their expertise and collaborate to achieve a common objective - expediting the discovery, development and commercialization of novel treatment options.

Additional information about the company and its product pipeline can be found at www.toleropharma.com.

Tolero Pharmaceuticals Forward-Looking Statements

This press release contains "forward-looking statements," as that term is defined in the Private Securities Litigation Reform Act of 1995 regarding the research, development and commercialization of pharmaceutical products. The forward-looking statements in this press release are based on management's assumptions and beliefs in light of information presently available, and involve both known and unknown risks and uncertainties, which could cause actual outcomes to differ materially from current expectations. Any forward-looking statements set forth in this press release speak only as of the date of this press release. We do not undertake to update any of these forward-looking statements to reflect events or circumstances that occur after the date hereof. Information concerning pharmaceuticals (including compounds under development) contained within this material is not intended as advertising or medical advice.

1. Alves-Filho JC, Pålsson-McDermott EM. Pyruvate Kinase M2: A Potential Target for Regulating Inflammation. Front Immunol. 2016;7:145.

SOURCE Tolero Pharmaceuticals, Inc.

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www.toleropharma.com