Sapience Therapeutics Receives IND Clearance from FDA to Proceed with Phase 1-2 Study of ST316 in Patients with Solid Tumors

ST316 is the first β-catenin peptide antagonist to enter the clinic-

-Patient dosing in Phase 1 portion of study expected to begin in 1H 2023-

HARRISON, N.Y., March 14, 2023 — 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 U.S. Food and Drug Administration (FDA) cleared the Company to proceed with its Phase 1-2 clinical trial of ST316 for the treatment of solid tumors.  Sapience expects to begin patient dosing in the Phase 1 dose escalation portion of the study in the first half of 2023 to evaluate the safety, clinical activity, pharmacokinetics and pharmacodynamics of ST316.

ST316 is Sapience’s first-in-class β-catenin antagonist. β-catenin is the effector protein of the Wnt signaling pathway, one of the most important oncogenic pathways. Wnt pathway hyperactivity is known to play a role in greater than 50% of solid tumors, in which it is a driver of oncogenesis and immune suppression.  Despite this significant role in tumor formation, Wnt-driven tumors have proven difficult to treat due to the critical function of Wnt-signaling in normal physiology and the associated side effects of complete Wnt-blockade. ST316 separates β-catenin’s physiologic and oncogenic activities, enabling treatment of Wnt-driven tumors while keeping normal β-catenin function intact. ST316 suppresses transcription of Wnt target genes regulating oncogenic proliferation, migration, invasion and metastatic potential, as well as genes regulating the immunosuppression of the tumor microenvironment.

“FDA clearance of the ST316 IND is an exciting achievement for Sapience, representing the second therapeutic candidate we discovered to advance into clinical development,” said Dr. Barry Kappel, CEO and President of Sapience.  “This milestone is the result of our team’s years of commitment to finding solutions to address oncogenic drivers of disease that have proven historically challenging to drug.”

Dr. Abi Vainstein-Haras, Sapience’s Chief Medical Officer, added, “As the first peptide antagonist of β-catenin to enter the clinic, we are thrilled to progress ST316 to a Phase 1-2 study in the first half of 2023. In addition to its known involvement in the pathogenesis of several cancers, the Wnt pathway’s role in regulating immune cell infiltration of the tumor microenvironment makes it a compelling therapeutic target. With preclinical studies demonstrating a favorable safety profile and significant anti-tumor activity, we look forward to bringing ST316’s first-in-class approach to targeting Wnt-driven tumors to the cancer community.”

The Phase 1 dose-escalation portion of the study is designed as a basket study to enroll patients with tumors likely to harbor abnormalities of the Wnt/β-catenin signaling pathway.  The Phase 2 dose-expansion portion of the study will enroll patients in four specific tumor types known to harbor abnormalities of the Wnt/β-catenin signaling pathway, including cholangiocarcinoma, colorectal, triple negative breast and ovarian cancers.

About ST316

ST316 is a first-in-class peptide antagonist of the interaction between β-catenin and its co-activator BCL9, a complex that drives oncogene expression in multiple cancers where aberrant Wnt/β-catenin pathway signaling is observed. The interaction between β-catenin and BCL9 has previously been considered an ‘undruggable’ target due to the inability of small molecules to inhibit complex formation and antibodies to gain access to the cytoplasm or nucleus to disrupt the interaction. ST316 contains a cell penetration moiety to allow intracellular access and a domain designed to bind the first armadillo repeat domain of β-catenin, a site utilized by BCL9 but no other β-catenin binding partners. ST316 suppresses transcription of oncogenic Wnt target genes regulating proliferation, migration, invasion and the metastatic potential of tumor cells, as well as genes regulating the immunosuppression of the tumor microenvironment.

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 dysregulations that drive cancer. Its pipeline of SPEARs™ (Stabilized Peptides Engineered Against Regulation) disrupt intracellular protein-protein interactions, enabling targeting of transcription factors which have traditionally been considered undruggable. Sapience’s lead program, ST101, is a first-in-class antagonist of C/EBPβ that has demonstrated clinical proof-of-concept in multiple indications. 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.

Contacts

Sapience Therapeutics, Inc.:
Barry Kappel, Ph.D., M.B.A.
President and Chief Executive Officer
info@sapiencetherapeutics.com

Media and Investor Contact:
Amy Conrad
Juniper Point
(858) 366-3243
amy@juniper-point.com