Basel, November 28, 2023 – TOLREMO therapeutics AG (TOLREMO) today announced that the first patient has been dosed in its first-in-human clinical trial evaluating the safety and tolerability, pharmacokinetics, and pharmacodynamics of its lead candidate, TT125-802, in patients across a range of solid tumor indications. TT125-802 is an orally available small molecule CBP/p300 bromodomain inhibitor designed to prevent non-genetic cancer drug resistance and thereby improve the response rates and durability of targeted cancer treatments. In preclinical testing, the compound has demonstrated the ability to block critical transcriptional resistance pathways responsible for cancer’s earliest escape mechanisms to targeted therapies.
"Initiating our Phase 1 clinical trial is an important corporate milestone for TOLREMO. With TT125-802, we are leveraging our scientific insights to develop an effective CBP/p300 inhibitor with the potential to prevent resistance mechanisms across a broad spectrum of current and future targeted cancer treatments,” said Stefanie Flückiger-Mangual, PhD, Co-founder and Chief Executive Officer of TOLREMO. “We are deeply committed to overcoming transcriptionally mediated cancer drug resistance for patient benefit, and this trial marks the start of an exciting new phase for the company.”
The Phase I dose-escalation study will enroll patients across a range of solid tumor indications. The primary objective will be a safety assessment of TT125-802 as a monotherapy. Secondary objectives include the analysis of the drug’s biological activity, pharmacokinetics, pharmacodynamics, and target engagement, as well as the identification of the recommended dosing regimen and potential biomarkers for future patient stratification. The trial will be conducted initially at clinical centers in Europe, with the potential to include sites in the U.S. through an open Investigational New Drug (IND) application with the Food and Drug Administration (FDA). Stepwise, TOLREMO will advance TT125-802 into clinical testing in combination with targeted therapies, such as KRAS, EGFR or AR inhibitors, in specific advanced solid tumor indications.
“TOLREMO’s in-depth preclinical analyses have showcased potency, selectivity, and safety data that demonstrate that TT125-802 has a highly differentiated profile, providing the foundation for translating these findings into the clinical setting. By specifically inhibiting transcriptional resistance pathways to targeted treatments, TT125-802 has the potential to profoundly improve the response rate and durability of other therapeutic interventions,” said Alessandra Cesano, MD, PhD, consulting Chief Medical Officer at TOLREMO therapeutics.