TEQ103, a novel therapeutic for the treatment of estrogen receptor alpha positive (ERα+) breast cancer

Autors:

Marie-Christine Bissery, Eef Hoeben, Elisabeth Bertrand, Sylvie Maubant, Maëva Albanese, Olivier Duchamp, Isabelle St-Jean, Mads K.Dalsgaard

Oncoteq, eScienceQPS, Université de Montréal, Oncodesign Services

Abstract :

Background:
Breast cancer is the most prevalent female cancer. Approximately 75% of them are ERα+ and are treated with ERα targeting agents. However, a good portion will ultimately relapse. TEQ103 (Sera2, ErSO-TFPy) is a first-in-class small molecule acting through the anticipatory unfolded protein response (aUPR) following dysregulation of calcium homeostasis in ERα+ tumor cells. The goal of this work is to further evaluate the efficacy, the influence of schedules of administration and the pharmacokinetics (PK) of TEQ103.

Conclusion:
These results demonstrate the significant durable antitumor effect of TEQ103 driven by the total dose administered regardless of schedule of administration, the wide therapeutic index and the concentration in the tumor tissue at levels markedly above the nM IC50 reached in vitro. These studies form the basis for PKPD Tumor Growth Inhibition modeling that will be used for projection of an efficacious starting dose in a subsequent breast cancer patients’ phase 1 clinical trial.

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