We are pleased to announce the publication of our latest patent:
WO 2026/132447, Polycyclic MTHFD2 Inhibitors and Uses Thereof.
MTHFD2 (Methylenetetrahydrofolate Dehydrogenase 2) is a compelling and underexplored therapeutic target. Overexpressed across multiple cancer types including breast, colorectal, and leukaemia - while barely detectable in most healthy adult tissues, it offers a wide therapeutic window for oncology. More recently, MTHFD2 has also emerged as a relevant target in autoimmune and inflammatory diseases, including rheumatoid arthritis, multiple sclerosis, SLE, and IBD, where its inhibition promotes regulatory T cell activity and suppresses inflammatory pathways.
This patent covers a novel class of polycyclic compounds built on a benzo[b][1,6]naphthyridine tricyclic scaffold: structurally distinct from all previously described MTHFD2 inhibitor classes, with 286+ exemplified compounds spanning broad chemical diversity across both oncology and autoimmune indications.
The core scaffold was identified using Makya, our synthesis-aware generative AI platform, which enabled exploration of novel, synthetically accessible chemical space beyond known MTHFD2 chemotypes.
The patent claims compound protection across the full genus of Formula (I) and its pharmaceutically acceptable salts, a pharmaceutical composition, medical use for the treatment of autoimmune, inflammatory, and proliferative diseases, and a novel manufacturing process, providing broad and robust IP coverage across the program.
This publication reflects the depth of expertise within the Iktos drug discovery team, and what becomes possible when AI-driven design and medicinal chemistry work hand in hand.
Access the patent following the link:
WO 2026/132447 A1 | PCT/EP2025/088398 | Published 25 June 2026
