OUR PIPELINE
EP102: METTL3 Inhibitor, a first-in-class approach to reprogram tumor biology
EPICS Therapeutics is advancing EP102 in patients with solid tumors — a best-in-class, potent, selective, and orally available inhibitor of the METTL3 enzyme.
EP102
EP102
What is METTL3 and why it matters
METTL3 (methyltransferase-like 3) is the catalytic core of the cellular complex that deposits N⁶-methyladenosine (m⁶A) modifications on RNA.
This m⁶A mark acts as a regulatory switch, determining how efficiently specific RNAs are translated into proteins.
In healthy cells, this process helps maintain normal growth, differentiation, and repair.
In cancer, however, METTL3 activity becomes dysregulated. Overexpression of METTL3 boosts the production of harmful proteins linked to uncontrolled proliferation, and enhanced metastatic potential across multiple tumor types, including ovarian, pancreatic, colorectal and non–small cell lung cancer (NSCLC).
“METTL3 inhibition has emerged as one of the most promising strategies in RNA-targeted oncology.”
Why EP102 is different
EP102 was designed to achieve high potency and selectivity for METTL3 with favorable oral bioavailability.
In preclinical models, EP102 demonstrated:
- Potent inhibition of METTL3 enzymatic activity
- Robust reduction of m⁶A levels in tumor RNA
- Modulating major cancer–driving signals such as HER2, MYC, and additional oncoproteins that control how tumor cells change form and acquire stem-like properties and metastasize, key traits underlying the spread of cancer and its resistance to treatment
- Near–complete tumor growth suppression in xenograft studies
