Positive response has been observed among the advanced cervical and endometrial cancer patients who have been treated multiple lines of SOCs including PD-1 drugs and/ or chemotherapy in the Phase I/II study (clinicaltrials.gov, NCT05383482).

Results of the Phase Ib study in all 31 subjects and in a subgroup with PIK3CA/AKT1/PTEN alterations from U.S. and China have demonstrated promising anti-cancer efficacy with a well-tolerated safety profile. Laekna has commenced a subsequent Phase III clinical trial AFFIRM-205 in China for the combination therapy in patients with PIK3CA/AKT1/PTEN alterations in May 2024, and plans to complete subject enrollment by Q4,2025.

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.

The results of this study showed that among the 14 TNBC patients who completed at least 2 cycles of treatment and had at least 1 tumor assessment, five showed confirmed partial response (ORR 35.7%), four had stable disease (28.6%), resulting in a disease control rate (DCR) of 64.3% in the best response assessment. The median duration of response (DOR) was 9.26 months (95% CI: 2.3 to not estimable). Five TNBC patients were treated for more than 32 weeks, with one patient reaching a duration of 73 weeks. 

LAE120 is a novel, allosteric and highly potent USP1 inhibitor, displaying monotherapy potency and combination activity with PARP inhibitor in HRD (homologous recombination deficiency) cancers. It has a unique chemical structure differentiated from all the other disclosed USP1 inhibitors and is expected to induce a different conformational change in USP1. LAE120 shows robust tumor inhibitory activity in MDA-MB-436 and K562 xenograft models as a single agent and exhibits synergistic effect in combination with PARP inhibitors. LAE120 demonstrates good therapeutic window in DRF study.

Laekna has established a global-leading and proprietary aHSC depletion discovery platform, which enables Laekna to discover and develop the next generation therapeutics against liver fibrosis, such as LAE105.In vitro, a panel of antibodies and bi-functional engagers targeting various aHSC targets have demonstrated potent and dose-dependent aHSC killing activity in the presence of human NK cells. In vivo, antibodies with enhanced effector function showed significant anti-fibrotic effects in two different liver fibrosis animal models.