OUR SCIENCE
Epigenetics, a proven therapeutic concept and new entry point to combat cancer
EPICS Therapeutics is among the first to translate the emerging field of RNA-epigenetics into the clinic.
OUR SCIENCE
A new entry point for cancer treatment
While most oncology efforts revisit familiar targets, RNA epigenetics represents a genuinely new entry point, a way to modulate how cells interpret genetic instruction rather than the genes themselves.
By targeting METTL3, EPICS Therapeutics brings fresh biology and a new mechanism of action to patients whose cancers no longer respond to existing therapies.
Epigenetic regulation determines how genes are switched on or off without altering the DNA sequence itself. Moreover, epigenetic therapies have validated the concept that modulating gene expression (rather than altering DNA itself) can reset abnormal cell behavior.
Yet, these approaches have reached their limits in solid tumors, showing modest efficacy, therapeutic resistance that can develop over time, and challenging safety profiles.
RNA-based regulation offers more precise control of cancer-driving pathways, is highly dynamic and adaptable, and promises to be a safer alternative since it does not permanently change gene expression.
Plus, RNA-targeting therapies can work alone or alongside DNA epigenetic drugs, opening new and complementary treatment options.
OUR SCIENCE
RNA Epigenetics, a new dimension of control
Beyond DNA and proteins, RNA molecules serve as dynamic regulators that fine-tune gene expression.
Chemical marks on RNA, collectively known as the epitranscriptome, determine how stable, translatable, or degradable a message becomes.
Among these, N⁶-methyladenosine (m⁶A) is the most abundant internal modification on messenger RNA. It is written by the METTL3 methyltransferase, which plays a pivotal role in controlling RNA fate and protein synthesis. This system can be hijacked by cancer cells whereupon RNA fate is dysregulated to promote tumor growth.
Studies have shown that METTL3 is overexpressed in many tumor types, including lung, pancreatic, ovarian, colorectal, and also in blood cancers such as acute myeloid leukemia (AML). Overexpression of METTL3 promotes tumor growth, invasion, and resistance to therapy.
“By selectively inhibiting METTL3, our data shows that it is possible to re-balance these RNA-based control mechanisms and limit tumor progression.”
Why RNA Epigenetics matters in cancer
RNA epigenetics represents a new therapeutic axis, a way to influence the flow of genetic information after transcription.
Targeting RNA-modifying enzymes brings:
- Novel, druggable nodes in signaling pathways that are distinct from, and potentially complemenary to DNA- or protein-directed therapies.
- The potential to restore balanced RNA processing and disrupt tumor-promoting networks.
- A strategy that could complement existing targeted and immune therapies.
EPICS Therapeutics is among the first to translate this emerging field into the clinic.
Our lead program, EP102, a potent and selective METTL3 inhibitor, is now being evaluated in first-in-patient studies for advanced solid tumors, bringing RNA epigenetics from concept to clinical reality.
