LAE119 / Laekna Therap - LARVOL DELTA

Preclinical characterization of LAE119, a novel PARP1 selective inhibitor and trapper (AACR 2024) - "In comparison to most PARP inhibitors including AZD5305, LAE119 exhibits extremely long residence time on PARP1 in both biochemical and cellular assays. In rat hematologic toxicity study, LAE119 at 10 mpk QD dose was well tolerated and had minimal effects on hematologic parameters. Both in vitro and in vivo data strongly support the further clinical investigation of LAE119."

Preclinical • Oncology • BRCA • BRCA2 • HRD • PARP2

Laekna Announces Two Poster Presentations on Internally Discovered Drug Candidates at AACR 2024 (PRNewswire) - "LAE119 is a potent and selective PARP1 inhibitor and PARP1-DNA trapper. It demonstrates more than 1000-fold selectivity for PARP1 DNA trapping activity over PARP2. In comparison to most PARP inhibitors including AZD5305, LAE119 exhibits extremely long residence time on PARP1 in both biochemical and cellular assays and shows good activity even in tumor cells with low PARP1 protein level. It demonstrates robust anti-tumor effect in BRCA2-/- DLD-1 and MDA-MB-436 Xenograft models and has minimal effects on hematologic parameters."

Preclinical • Breast Cancer • Oncology • Solid Tumor