Totus Medicines Announces Poster Presentation for TOS-358, the First Highly Selective Covalent Molecule Targeting PI3Kα, at the 34th EORTC-NCI-AACR Symposium in Barcelona

On October 27, 2022 Totus Medicines, a drug discovery company with the mission to make any protein druggable through its breakthrough chemical biology platform, reported that the poster presentation for TOS-358 at the 34th EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium (ENA 2022) held in Barcelona Oct 26-28, 2022 (Press release, Totus Medicines, OCT 27, 2022, View Source [SID1234622527]). The poster exhibits data from the clinical development candidate TOS-358, the first highly selective covalent molecule targeting PI3Kα, which is the most mutated oncogene in cancer. Totus Medicines is set to start clinical trials of TOS-358 in early 2023.

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Presentation Title: Preclinical characterization of TOS-358, a potent and selective covalent inhibitor of wild-type and mutant PI3Kα with superior anticancer activity
Session title: New Drugs
Session type: Poster Session
Catalog number: 107
Presentation number: PB097

TOS-358 is a highly selective covalent inhibitor of PI3Kα. TOS-358 demonstrates clear superiority compared to non-covalent molecules by achieving deep and durable inhibition of PI3K-AKT signaling. In various preclinical disease models, including over 30 patient derived xenograft (PDX) models, TOS-358 led to dramatically superior efficacy compared with non-covalent compounds targeting PI3Kα such as alpelisib and GDC-0077. This stems from TOS-358’s unique ability to robustly and durably inhibit the PI3K/AKT pathway in cells prone to pathway feedback and re-activation. Based on well-established mechanistic understandings of PI3Kα and in vivo TOS-358 data across multiple preclinical species, TOS-358 has an excellent therapeutic window with minimal glucose effects in the clinic. Totus plans to present this data at a future scientific conference.

TOS-358 highlights the company’s ability to identify highly specific and potent molecules against previously poorly drugged or undrugged targets.