LAE118 / Laekna Therap, Vasque Bio - LARVOL DELTA

Laekna…is pleased to announce that the Group has commenced subject recruitment in the Phase I clinical study (the 'Phase I Clinical Study') of LAE118 in China for the treatment of advanced solid tumors, and the first subject has been enrolled (Laekna Press Release)

Enrollment open • Solid Tumor

Expected Upcoming Milestones in Second Half of 2026 (Laekna Press Release) - "About LAE118 - Initiate a Phase I clinical study in PIK3CA mutant advanced solid tumors."

New P1 trial • Solid Tumor

A Study of LAE118 as Monotherapy and in Combination With Antitumor Agents in Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=150 | Not yet recruiting | Sponsor: Laekna Limited

Monotherapy • New P1 trial • Breast Cancer • Endometrial Cancer • Head and Neck Cancer • HER2 Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • ER • HER-2 • PGR • PIK3CA

Voluntary Announcement | Exclusive License Agreement with Vasque Bio for LAE118 (a novel PI3Kα pan-mutant selective inhibitor) in Ex-China Region (Laekna Press Release) - "Subject to terms and conditions of the License Agreement, Vasque Bio is granted, among other rights, an exclusive, worldwide license (excluding Chinese Mainland, Hong Kong Special Administrative Region, Macau Special Administrative Region and Taiwan) (the 'Licensed Territory') to develop, manufacture, commercialize and otherwise exploit LAE118 (an internally discovered Novel PI3KαPan-Mutant Selective Inhibitor). In return, the Group is entitled to receive a non-refundable and non-creditable upfront cash payment of USD10 million and the right to acquire, for no additional consideration, up to high teen percentage of Vasque Bio’s outstanding common stock or cash payments in lieu of such common stock. "

Licensing / partnership • Solid Tumor

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

Laekna…announced that the U.S. Food and Drug Administration (FDA) has accepted its Investigational New Drug application for LAE118, a novel PI3Kα pan-mutant selective inhibitor for the treatment of patients with PIK3CA-mutant solid tumors (Laekna Press Release) - "LAE118 is a novel allosteric inhibitor which demonstrated excellent potency and selectivity against various PI3Kα pan-mutant, with best-in-class potential."

IND • Oncology • Solid Tumor

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