LAE-118 / Laekna Therap - LARVOL DELTA

LAE118, a pan mutant-selective PI3Ka inhibitor with superb activity against both the kinase domain and helical domain mutants (AACR 2025) - "In response to this, pan-mutant selective PI3Ka inhibitors including RLY-2608 and STX-478 are being developed in clinical trials for cancer patients with PIK3CA mutations. Human PK projection indicates LAE118 has the potential to achieve continuous inhibition of pAKT in clinic without causing hyperglycemia. LAE118 is currently in IND enabling stage, positioning it as a promising candidate for the treatment of cancers with PIK3CA mutations."

Late-breaking abstract • Oncology • PIK3CA

Advancing Diversified Pipelines (Businesswire) - "Laekna is actively advancing preclinical drug candidates. In the fourth quarter of 2024, another internally discovered anti-tumor drug candidate, LAE118, a potentially best-in-class, mutant-selective PI3Kαinhibitor, has advanced to IND-enabling study....IND is expected to be filed in the fourth quarter of 2025."

IND • Oncology

Laekna Announces Poster Presentation on Internally Discovered Selective PI3Kα Inhibitor at SABCS 2024 (PRNewswire) - "Laekna...announced that the company will present an internally discovered preclinical candidate at the 2024 San Antonio Breast Cancer Symposium (SABCS) on December 13, 2024. The presentation will feature preclinical characterization of LAE118, a novel allosteric pan-mutant selective PI3Kα inhibitor....LAE118 shows strong anti-tumor growth effect in Xenograft models at a dose that is much lower than other allosteric inhibitors and has less effect on glucose homeostasis compared to orthosteric PI3Kα inhibitors. In pre-clinical toxicology studies, LAE118 also demonstrated good tolerability."

Preclinical • Solid Tumor