Sapience Therapeutics Presents Late-Breaking Data at AACR 2022 Demonstrating the Potential of Targeting Intracellular Interactions to Drug Well-Validated Cancer Pathways

-ST101 is a peptide antagonist of C/EBPβ that has demonstrated clinical proof-of-concept in Phase 1 with a confirmed Partial Response-

-ST316 is a peptide antagonist of β-catenin in IND-enabling studies-

HARRISON, N.Y., April 11, 2022 /PRNewswire/ — Sapience Therapeutics, Inc., a clinical-stage biotechnology company focused on the discovery and development of peptide therapeutics to address difficult-to-treat cancers, announced today the presentation of late-breaking research from its lead programs, ST101 and ST316, at the American Association for Cancer Research (AACR) Annual Meeting 2022. These data illustrate the potential of targeting intracellular interactions to address cancer pathways that are well-validated but have previously been considered undruggable.

“With these late-breaking data at AACR 2022, we have a growing body of preclinical and clinical evidence across our pipeline demonstrating that targeting protein-protein interactions can address cancer targets previously considered undruggable, including C/EBPβ and β-catenin, which we believe offer a wealth of therapeutic promises,” said Dr. Barry Kappel, CEO and President of Sapience. “We look forward to advancing ST101 through Phase 2 and progressing ST316 through IND-enabling studies and into the clinic.”

ST101 is a first-in-class peptide antagonist of C/EBPβ currently being evaluated in the Phase 2 portion of an ongoing Phase 1-2 clinical study in patients with advanced unresectable and metastatic solid tumors (NCT04478279). 

  • Sapience scientists presented preclinical data from a triple negative breast cancer (TNBC) model used to: (i) characterize and predict the exposure-response relationship of ST101; (ii) provide rationale to select a dose for the Phase 2 clinical study cohorts; and (iii) support the continued development of ST101 as a potent therapeutic for patients with solid tumors.
  • Following administration of ST101 in TNBC mice, significant tumor growth inhibition was observed, and the exposures required to achieve IC50 and IC90 predicts that 1 mg/kg in humans will exceed the exposure associated with the IC90 in mice.

ST316 is a first-in-class peptide antagonist of β-catenin currently being evaluated in IND-enabling studies. 

  • Sapience designed ST316 to disrupt the interaction of β-catenin with its co-activator BCL9, an interaction essential for oncogenic Wnt/β-catenin signaling but not homeostatic functions.
  • Sapience scientists presented preclinical data on ST316 demonstrating target engagement with β-catenin, in vitro activity demonstrating disruption of β-catenin nuclear localization, changes in target gene expression in HCT116 cells and significant anti-tumor activity in vivo.
  • Following once weekly administration of ST316 in HCT116 colorectal cancer subcutaneous xenograft tumors, a 99% tumor growth inhibition was observed.

Details of the late-breaking posters are as follows:

Abstract Number: 8125
Title: Characterizing the PK/PD relationship of C/EBPβ antagonist peptide ST101 in a mouse orthotopic breast cancer model
Session Title: Late-Breaking Research: Experimental and Molecular Therapeutics 2
Session Date and Time: 4/13/2022 9:00 AM
Location: New Orleans Convention Center, Poster Section 16

Abstract Number: 8148
Title: β-catenin antagonist peptide, ST316, attenuates Wnt-dependent oncogenic activity
Session Title: Late-Breaking Research: Molecular/Cellular Biology and Genetics 1
Session Date and Time: 4/11/2022 9:00 AM
Location: New Orleans Convention Center, Poster Section 16

Abstracts and full session details can be accessed through the AACR meeting planner: AACR Annual Meeting 2022 | April 8-13, 2022 | New Orleans

About ST101

ST101, a first-in-class antagonist of C/EBPβ, is currently being evaluated in the Phase 2 portion of an ongoing Phase 1-2 clinical study in patients with advanced unresectable and metastatic solid tumors (NCT04478279). This is an open-label, two-part, Phase 1-2 dose-finding study designed to determine the safety, tolerability, PK, PD, and proof-of-concept efficacy of ST101 in patients with advanced solid tumors. The study consists of two phases: a Phase 1 dose escalation/regimen exploration phase and a Phase 2 expansion phase. In the ongoing dose escalation study, ST101 has demonstrated clinical proof-of-concept with a RECIST 1.1-confirmed partial response (PR) in a patient with cutaneous melanoma and evidence of long-lasting stable disease in several additional patients. In the ongoing Phase 2 dose expansion part of the study, Sapience has initiated enrollment in patients with GBM, metastatic cutaneous melanoma, refractory, locally advanced or metastatic hormone-receptor-positive breast cancer and castrate-resistant prostate cancer. ST101 has been granted Fast Track designation for recurrent GBM and advanced cutaneous melanoma in patients who have disease progression on or after anti-PD-1/anti-PD-L1 therapy, as well as Orphan designation from the U.S. Food and Drug Administration and the European Commission for the treatment of glioma.

About ST316

ST316, a first-in-class β-catenin antagonist, is currently being evaluated in IND-enabling studies. β-catenin is a critical member of the canonical Wnt signaling pathway, a well-known development stage pathway that has been considered an “undruggable” cancer target, as small molecules have proven ineffective or toxic. Wnt/β-catenin signaling drives cancer initiation and contributes to tumor growth, angiogenesis and metastasis. ST316 exerts its activity through disruption of the BCL9/β-Catenin interaction to suppress transcription of Wnt target genes regulating proliferation, migration, invasion, and the metastatic potential of tumor cells. 

About Sapience Therapeutics

Sapience Therapeutics, Inc. is a privately held, clinical stage biotechnology company focused on discovering and developing peptide therapeutics for major unmet medical needs, particularly high mortality cancers. Sapience’s approach holds potential to target intracellular interactions that are traditionally considered “undruggable targets”. Its lead program, ST101, is a peptide antagonist of C/EBPβ that has demonstrated clinical proof-of-concept in Phase 1 with a confirmed partial response (PR). ST101 is currently being evaluated in the Phase 2 portion of an ongoing Phase 1-2 clinical study with potential applications in various solid tumors and hematologic malignancies. For more information on Sapience Therapeutics, please visit 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.


Sapience Therapeutics, Inc.
Barry Kappel, Ph.D., M.B.A.
President and Chief Executive Officer

Media and Investor Contact:
Amy Conrad
Juniper Point
(858) 366-3243

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SOURCE Sapience Therapeutics

Released April 11, 2022