HARRISON, New York, September 19, 2022 /PRNewswire/ — Sapience Therapeutics, Inc., a clinical-stage biotechnology company focused on the discovery and development of peptide therapeutics to address oncogenic and immunogenic dysregulations that cause cancer, announced today that preclinical data on ST101, the first in-class peptide antagonist of C/EBPβ, have been published online in Molecular Cancer Therapeutics, a journal of the American Association for Cancer Research. The published data describe preclinical evidence supporting the advancement of ST101 as a novel therapy for the treatment of advanced solid tumors. The full manuscript, entitled “Anticancer activity of ST101, a novel CCAAT/enhancer-binding protein β antagonist‘ can be found here on the internet.
The data in the manuscript describe ST101 antagonism of CCAAT/Enhancer Binding Protein β (C/EBPβ), a fundamental transcription factor of the leucine zipper family that is upregulated or overactivated in many cancers, resulting in gene transactivation leading to oncogenesis drives. ST101 binds C/EBPβ, preventing its dimerization and enhancing ubiquitin proteasome-dependent C/EBPβ degradation. ST101 exposure significantly decreases expression of C/EBPβ target genes, including genes responsible for survival, transcription factors, and cell cycle-related proteins. The result of ST101 exposure is potent tumor-specific cytotoxic activity in vitro in cancer cell lines including glioblastoma, breast, melanoma, prostate and lung cancer, while normal human immune and epithelial cells are unaffected. In vivo xenograft models indicate that ST101 exposure results in potent inhibition or regression of tumor growth, both as a single agent and in combination studies.
“The release of ST101 in Molecular Cancer Therapeutics is an exciting achievement that highlights the tremendous unmet need for novel therapies to treat solid tumors and the role ST101 can play to fill that need,” he said Jim Rotolo, Ph.D., Vice President of Sapience, Translational Pharmacology and Principal Investigator. “We are excited to publish ST101’s mechanism of action and to demonstrate the therapeutic promise of disrupting C/EBPβ-gated oncogenic activity. We look forward to reporting and releasing additional data on ST101 and advancing the program through its ongoing Phase 1-2 trial.”
In its ongoing Phase 1-2 study, ST101 has demonstrated clinical proof-of-concept with an mRANO-confirmed partial response in a patient with recurrent GBM, a durable RECIST 1.1-confirmed partial response in a patient with cutaneous melanoma, and long-lasting stable disease in several other patients.
About ST101 and the phase 1-2 study
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 trial in patients with advanced unresectable and metastatic solid tumors (NCT04478279). ST101-101 is an open-label, phase 1-2, dose-ranging study 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: phase 1 dose escalation/regime exploration and phase 2 dose expansion. In the ongoing Phase 2 dose expansion, Sapience is actively recruiting patients with GBM, metastatic cutaneous melanoma, castration-resistant prostate cancer, and locally advanced or metastatic hormone receptor-positive breast cancer. In the ongoing dose escalation portion of the study, ST101 has demonstrated clinical proof-of-concept with a durable RECIST 1.1-confirmed partial response (PR) in one patient with cutaneous melanoma and evidence of long-term stable disease in several additional patients. In the ongoing Phase 2 dose-expansion portion of the study, ST101 has demonstrated clinical proof-of-concept with an mRANO-confirmed partial response in one patient with recurrent GBM and evidence of long-term stable disease in several additional patients.
ST101 has been granted fast track designation by the FDA for recurrent GBM and advanced cutaneous melanoma in patients with disease progression on or after anti-PD-1/anti-PD-L1 therapy, and orphan designation for advanced melanoma, glioma and AML and by the European Commission for the Treatment of Glioma.
About Sapience Therapeutics
Sapience Therapeutics, Inc. is a privately held clinical-stage biotechnology company focused on the discovery and development of peptide therapeutics to address oncogenic and immunogenic dysregulations that cause cancer. Its pipeline of Stabilized Peptides Engineered Against Regulation (SPEARs™) disrupts intracellular protein-protein interactions and enables the targeting of transcription factors traditionally thought to be drug-free. Sapience’s lead program, ST101, is a first-in-class C/EBPβ antagonist that has demonstrated clinical proof-of-concept in multiple indications. For more information about Sapience Therapeutics, visit www.sapiencetherapeutics.com and get involved with us LinkedIn.
Cautionary Note Regarding Forward-Looking Statements
This press release contains forward-looking statements. All statements contained herein, other than statements of historical fact, may 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 those relating 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 could differ materially due to certain factors, including without limitation, our ability to obtain additional funding and to meet applicable regulatory standards and obtain required regulatory approvals . Forward-looking statements speak only as of the date of this press release. Except as required by law, Sapience undertakes no obligation to update any forward-looking statement, whether as a result of new information, future events, changed assumptions or otherwise.
Sapience Therapeutics, Inc.
Barry KappelPhD, MBA
President and Chief Executive Officer
Media and investor contact:
View original content to download multimedia: https://www.prnewswire.com/news-releases/sapience-therapeutics-announces-publication-showcasing-the-mechanism-of-action-and-anti-tumor-activity -of-st101-a-novel-and-selective-peptide-antagonist-of-cebp-in-molecular-cancer-therapeutics-301627498.html
SOURCE Sapience Therapeutics