Lacutoclax (LP-108) is an orally active and selective Bcl-2 inhibitor with antitumor activity both in vivo and ex vivo for studies related to lymphoma and leukemia.

H1963 cells: 0.45 μM, H146 cells: 0.23 μM

In small cell lung cancer (SCLC) cell lines such as H146 and H1963, treatment with the active metabolite Lacutoclax (0.1–10 μM for 24–72 hours)inhibited cell proliferation, with IC₅₀ values of 0.23 μM and 0.45 μM, respectively. The treatment induced apoptosis as evidenced by caspase activation, PARP cleavage, and increased Annexin V-positive cells, indicating a mitochondrial pathway–dependent mechanism[1].

In NOD/SCID mice bearing H146 or H1963 xenografts, intravenous administration of Lacutoclax (25–100 mg/kg, once daily for 10 consecutive days) led to dose-dependent tumor growth inhibition. At 100 mg/kg, some tumors completely regressed. Treated mice maintained stable body weight with no significant toxicity, demonstrating strong antitumor efficacy and good tolerability[1].