Sapience Therapeutics Enrolls First Patient in Phase 2 Study of ST316, a First-in-Class β-catenin Antagonist, in Colorectal Cancer

-ST316 will be evaluated in several combinations and lines of treatment-

TARRYTOWN, N.Y., Oct. 1, 2024 /PRNewswire/ -- Sapience Therapeutics, Inc., a clinical-stage biotechnology company focused on the discovery and development of peptide therapeutics to address oncogenic and immune dysregulation that drive cancer, announced today that the first patient has been enrolled in its Phase 2 dose expansion study evaluating ST316, the Company's first-in-class antagonist of β-catenin.  Enrollment of the study's Phase 1 monotherapy dose escalation portion was completed in July 2024.

ST316 is designed to selectively shut down the Wnt/β-catenin signaling pathway in tumor cells but not in normal cells, allowing for anti-cancer activity without the toxicity related to broad inhibition of this pathway. The Wnt/β-catenin signaling pathway is one of the most active pathways in several cancers and drives more than 80% of colorectal cancers (CRCs), the first indication to be evaluated in the ST316 Phase 2 expansion. There are more than 1 million people living with CRC in the United States, with another 150,000 expected to be diagnosed this year alone.

Dr. Abi Vainstein-Haras, Sapience's Chief Medical Officer, stated, "The promising results seen in our Phase 1 study demonstrate ST316's potential to be an effective therapy for Wnt pathway-driven cancers, including CRC among others.  Given ST316's favorable safety and tolerability profile, together with robust pre-clinical data, Sapience is committed to maximizing the potential of ST316 in various therapeutic combinations across lines of treatment."

"CRC patients who are refractory to current therapies desperately need new options like ST316," said Dr. Barry Kappel, Sapience's founder and Chief Executive Officer. "With CRC being the second-leading cause of cancer death in the United States, and with alarming increases in incidence among younger Americans, we are dedicated to widening the treatment options for this devastating disease."

ST316-101 (NCT05848739) is a first-in-human, open-label, Phase 1-2 dose-escalation and expansion  study designed to determine the safety, tolerability, PK, PD and early efficacy of ST316. The Phase 1 dose escalation portion of the study tested various dose levels of ST316 in patients with select advanced solid tumors that are known to harbor abnormalities of the Wnt/β-catenin signaling pathway, including CRC.  The Phase 1 portion completed enrollment in July 2024.  In the Phase 2 dose expansion portion of the study, ST316 is being tested in CRC patients in combination with relevant standards of care and in multiple lines of treatment.  Sapience is conducting the Phase 2 study across several sites in the United States.

About ST316

ST316 is a first-in-class peptide antagonist of the interaction between β-catenin and its co-activator, BCL9, a complex responsible for driving oncogene expression in multiple cancers where aberrant Wnt/β-catenin pathway signaling is observed. ST316 exposure in cancer cells prevents BCL9-driven nuclear localization of β-catenin and inhibits formation of the Wnt enhanceosome protein complex. Disruption of this interaction selectively suppresses the transcription of oncogenic Wnt target genes that regulate proliferation, migration, invasion and the metastatic potential of tumor cells, as well as genes that regulate the immunosuppression of the tumor microenvironment. ST316 creates a pro-immune tumor microenvironment and in preclinical models has shown to be synergistic with checkpoint inhibition. Due to its selectivity and downstream modulation of the Wnt/β-catenin pathway, ST316 presents an opportunity to safely and effectively target Wnt/β-catenin driven cancers without the toxicities previously seen with other Wnt pathway agents.

About Sapience Therapeutics

Sapience Therapeutics, Inc. is a privately held, clinical-stage biotechnology company focused on discovering and developing peptide therapeutics to address oncogenic and immune dysregulation that drive cancer.  With in-house discovery capabilities, Sapience has built a pipeline of therapeutic candidates called SPEARs™ (Stabilized Peptides Engineered Against Regulation) that disrupt intracellular protein-protein interactions, enabling targeting of transcription factors which have traditionally been considered undruggable, and can direct cargo to cell surface targets with their new class of molecule called SPARCs™ (Stabilized Peptides Against Receptors on Cancer), enabling delivery of payloads such as α-particles to cancer cells. Sapience is advancing two clinical programs through Phase 2 studies: ST316, a first-in-class antagonist of β-catenin, and ST101, a first-in-class antagonist of C/EBPβ. 

For more information on Sapience Therapeutics, please visit www.sapiencetherapeutics.com and engage with us on LinkedIn.

Cautionary Note on Forward-Looking Statements

This press release contains forward-looking statements. Any statements herein other than statements of historical fact could be deemed to be forward-looking statements. These forward-looking statements may include, among other things, statements regarding future events that involve significant risks and uncertainties (including with respect to Sapience's preclinical and clinical development programs). These forward-looking statements are based on management's current expectations, and actual results and future events may differ materially as a result of certain factors, including, without limitation, our ability to obtain additional funds, and meet applicable regulatory standards and receive required regulatory approvals. Forward-looking statements speak only as of the date of this press release. Sapience does not undertake any obligation to update any forward-looking statements as a result of new information, future events, changed assumptions or otherwise, except as required by law.

Media and Investor Contact:
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SOURCE Sapience Therapeutics, Inc.