Gosselies, Belgium – May 21st, 2026
EPICS Therapeutics announces the publication of a peer-reviewed article in the Journal of Medicinal Chemistry describing the discovery and optimization of EP102, its clinical-stage METTL3 inhibitor for the treatment of solid tumors and acute myeloid leukemia (AML).
The study, titled “Optimization of METTL3 Inhibitors for the Treatment of Solid Tumors and AML,” details the scientific path from early discovery compounds to EP102, a best-in-class, potent, selective, and orally available inhibitor of the METTL3 enzyme, now in clinical development for advanced solid tumors.
METTL3 is a master regulator of RNA biology, responsible for installing the m⁶A modification on messenger RNA, a molecular signal that helps determine how genes are translated into proteins. In healthy cells, this process provides resilience permitting cells to grow and differentiate. In cancer, however, METTL3 is dysregulated to thereby enable tumor cells to grow, adapt, and resist treatment.
By targeting METTL3, EP102 aims to reprogram tumor biology at the RNA level, offering a fundamentally new way to intervene in cancer beyond traditional DNA or protein-focused approaches.
Highlights from the publication
- From parenteral to oral therapy: EP102 is effective by oral admnistration commensurate with its improved pharmacokinetic profile, while maintinaing potency, relative to prototype compounds that were limited to use as injectables.
- Consistent antitumor activity: EP102 demonstrated strong efficacy across multiple preclinical models, including both hematological and solid tumors.
- Direct engagement of RNA regulation: The compound reduced m⁶A RNA methylation (a chemical mark that controls how genetic messages are translated into proteins) in vitro and in vivo, confirming its mechanism of action and its ability to modulate how cancer cells produce key proteins.
- Balanced drug profile: EP102 showed high selectivity, metabolic stability, and favorable pharmacokinetics supporting its advancement into clinical development.
- A complete optimization journey: The study outlines how step-by-step structural refinements enabled the transition from the prototype compound EP652 to the clinical candidate EP102.
These findings establish METTL3 inhibition as a viable therapeutic strategy and support the continued development of EP102.
Commenting on the significance of the study, Graeme Fraser, PhD, Chief Executive Officer and Chief Scientific Officer, said: “The research team at EPICS has a proven track-record of putting quality products into clinical development that ultimately progress to market. Our experimental data demonstrate that EP102 is the best-in-class METTL3 inhibitor and we believe it to be ideally suited to define the therapeutic breadth of METTL3 inhibition as a novel approach for the treatment of solid tumors and blood cancers.”
Describing the optimization process that led to the selection of EP102 as a clinical candidate, Guillaume Dutheuil, PhD, Head of Medicinal Chemistry & CMC, said: “From our proof-of-concept compound EP652, used as an injectable treatment, metabolic soft spots were identified and chemical structural modifications were extensively explored, with the aim of maintaining potency while improving pharmacokinetic properties. Step-by-step refinements of the core structure, including the introduction of an oxetane group and optimization of the hinge region through replacement of aniline and triazole groups, were necessary to deliver EP102 as a potent, orally available compound, efficacious in in vivo cancer models, with a profile suitable for clinical development.”
About EP102
EP102 is a best-in-class, orally available METTL3 inhibitor currently being evaluated in patients with solid tumors.
In preclinical studies, EP102:
- Demonstrated potent inhibition of METTL3 enzymatic activity
- Reduced m⁶A RNA methylation, a key regulator of gene expression
- Showed strong antitumor activity across hematological and solid tumor models
- Achieved significant tumor growth inhibition in vivo
By blocking METTL3, EP102 aims to modulate RNA signaling that sustains tumor growth, representing a fundamentally new way to target cancer at the RNA level.
Read the “Optimization of METTL3 Inhibitors for the Treatment of Solid Tumors and AML” study here.
About EPICS Therapeutics
Epics Therapeutics is a clinical-stage Belgian, private, drug discovery and development company that invents and develops small molecule drugs targeting RNA epigenetics¹ and G-Protein Coupled Receptor² mechanisms involved in cancer development. By targeting these mechanisms, Epics Therapeutics aims to translate science into life-changing therapies for patients.
¹RNA epigenetics refers to the post-genomic changes in protein synthesis directed by chemical marks added to RNA molecules, such as N6-methyladenosine (m6A). These marks do not change the genetic code itself, but they influence how the instructions in RNA are read and used to make proteins. In healthy cells, this helps regulate growth and differentiation. In cancer, these marks are applied in an aberrant manner, tipping the balance toward uncontrolled cell proliferation.
²G-protein coupled receptors are a large family of receptors expressed on the cell surface that respond to signals like hormones, neurotransmitters, or metabolites. When activated, they trigger G-proteins in the cell membrane to transduce signals inside the cell that affect how the cell behaves with application to a broad range of physiological outputs, including in the field of cancer.
For more information, visit www.epicstherapeutics.com
Contact: EPICS Therapeutics Media Relations Desk at media_relations@epicstx.com