Tolero Pharma Submits Investigational New Drug Application for Experimental PKM2 Activator TP-1454

Tolero Pharmaceuticals, Inc., a clinical-stage company focused on developing novel therapeutics for hematological and oncological diseases, 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.