Unlocking Cell Epigenomics to Transform Disease Treatment
Despite decades of remarkable advances in biology and technology, small-molecule drug development—the backbone of therapeutic innovation—remains inefficient, constrained by outdated design paradigms. Traditional cancer therapies often follow a “one-drug, one-target” model, focusing on cell surface receptors or kinase signaling pathways. While occasionally effective, these approaches are frequently limited by toxicity, resistance, short-lived responses, and narrow applicability.
As Einstein wisely noted, “We cannot solve our problems with the same level of thinking that created them.” Parkside Scientific Inc., based in New York City, embraces this principle by reimagining drug discovery. Rather than targeting isolated defects, Parkside addresses disease at its root—through cell epigenomics and transcriptomics—moving beyond signal-centric strategies.
Rethinking the Root of Disease
Gene expression patterns, shaped by internal and external cues, govern cell behavior. While genetic mutations or aberrant signaling may initiate disease, it is often the widespread dysregulation of epigenomic and transcriptomic control—across diverse cell types—that drives disease progression. This insight suggests a new therapeutic approach: reprogramming gene expression to restore healthy cell function.
A promising strategy targets bromodomains (BrDs)—histone reader proteins that regulate transcription by recognizing acetylated lysines. When dysregulated, these proteins can drive abnormal gene activity, fueling cancer and chronic inflammation.
Parkside’s Breakthrough: STAMP™ Technology
The BET family of BrD proteins has emerged as a key drug target. However, first-generation BET inhibitors—such as Novartis’ Pelabresib[1], developed under the one-target model—have shown limited success in clinical trials due to dose-limiting toxicity and modest, short-lived efficacy as monotherapies.
Parkside’s proprietary STAMP™ platform[2] overcomes these limitations with a network-aware approach. Instead of inhibiting a single BrD protein, STAMP™ molecules modulate multiple transcriptional pathways simultaneously—enabling lower doses, reduced toxicity, and enhanced efficacy.
Lead candidate PS1132—a STAMP™-based BrD modulator—has demonstrated strong safety, pharmacokinetics, and efficacy in Phase I trials for T-cell and B-cell lymphomas. Notably, patients who had failed multiple prior treatments—including chemotherapy, immunotherapies, and targeted agents (JAK1, PI3Kδ, BTK inhibitors)—responded well, with no significant adverse effects. PS1132 offers renewed hope—and a compelling opportunity for strategic partnerships.
A Platform with Broad Potential
Beyond blood cancers, Parkside is advancing STAMP™-based therapies for treatment-resistant prostate and breast cancer, as well as chronic inflammatory conditions such as IBD, MS, and Alzheimer’s disease.
Join the BrD Drug Discovery Revolution
Parkside Scientific is redefining therapeutic innovation through the lens of epigenomics. For partnership opportunities, contact us at info@pksci.com.
2025-04-06
[1] Pelabresib, acquired by Novartis ($2.9B), is seeking FDA approval for the treatment of myelofibrosis in combination with ruxolitinib.
[2] STAMP = Strategic Transcriptional Activity Modulator Paradigm.