On October 27, 2022 Sporos BioDiscovery, Inc. (a wholly owned affiliate of Sporos Bioventures, "Sporos" or the "Company"), a precision oncology company developing a diversified pipeline of small molecule therapeutic programs targeting cancer vulnerabilities in the tumor and tumor microenvironment, reported its poster presentation highlighting preclinical data on the Company’s lead program, SPR1, a differentiated, novel TEAD inhibitor at 34th EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium on Molecular Targets and Cancer Therapeutics, taking place October 26-28, 2022, in Barcelona, Spain (Press release, Sporos Bioventures, OCT 27, 2022, View Source [SID1234622541]).
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"We were excited to present preclinical data from SPR1, a next-generation, finely tuned TEAD inhibitor program, with a unique TEAD isoform selectivity that we believe sets it apart from other TEAD inhibitors and offers a potential best-in-class profile. These preclinical data sets demonstrate compound safety and superior in vivo single-agent activity in large-volume tumor models and in combination with KRAS, MEK, and RTK inhibitors," said Dr. Stephen Rubino, Chief Executive Officer of Sporos. "Our data supports our initiative to move SPR1 into clinical development with a goal of filing an IND before the end of 2023."
The Hippo pathway (effected by the YAP/TAZ-TEAD transcriptional complex) is a major oncogenic pathway and hyperactivation of YAP/TAZ-TEAD transcription has been demonstrated as a key mechanism of resistance to MAPK pathway inhibition, as well as inhibition of its upstream inputs, such as EGFR and other receptor tyrosine kinases. The poster presents the first disclosure of SPR1, Sporos TEAD inhibitor program. Highlights of the poster, titled "A Family of Novel TEAD Palmitoylation Site Inhibitors with Exceptional Pre-clinical Anti-neoplastic Activity as a Monotherapy and in Combination with MAPK Inhibitors," include:
The synthesis of a series of small molecule inhibitors of TEAD transcription factors with nM activity in a broad range of cancer cell lines, coupled with favorable pharmacokinetic and safety profiles.
Fine-tuning of TEAD isoform specificity yielded exceptional TEAD inhibitors with low toxicity (MTD >300 mg/kg, >20X efficacious dose) coupled with high anti-tumor efficacy.
Sporos’ TEAD inhibitors yield rapid regression even in very large pre-clinical tumors, a first in the TEAD-inhibitor space.
Sporos’ TEAD inhibitors show strong synergy with precision oncology drugs targeting the MAPK pathway and its upstream inputs, including Sotorasib, Trametinib, and Osimertinib.
Differentiated activity profile of SPR1 TEAD inhibitors may derive from favorable TEAD isoform inhibitory specificity.