Our primary targets are MTHFD1/2 isoenzyme proteins that regulate one-carbon metabolism, often upregulated in multiple cancers. MTHFD2 is an oncofoetal protein expressed during embryogenesis, silenced in normal adult cells, and then re-expressed in cancer. Both proteins have been validated as anti-cancer targets by numerous independent laboratories. We are proud to have made a first-in-class, low nanomolar potent inhibitor of MTHFD1/2 for clinical development using state-of-the-art structural and medicinal chemistry approaches.