plinabulin + top1-adc

**Plinabulin + TOP1-ADC** is a preclinical-stage combination regimen being developed by BeyondSpring. It combines plinabulin, a first-in-class small molecule guanine nucleotide exchange factor H1 (GEF-H1) agonist and tubulin-disrupting agent, with topoisomerase I inhibitor-based antibody-drug conjugates (TOP1-ADCs), such as trastuzumab deruxtecan (T-DXd) or datopotamab deruxtecan (Dato-DXd). Plinabulin binds to beta-tubulin, disrupting microtubule polymerization and releasing GEF-H1, which triggers a signaling cascade leading to dendritic cell maturation, antigen presentation, and T-cell activation. The TOP1-ADC component delivers a cytotoxic topoisomerase I inhibitor payload directly to tumor cells expressing specific antigens (such as HER2 or TROP2). Preclinical studies have demonstrated that this combination produces synergistic antitumor activity, increases complete tumor regressions, and mitigates chemotherapy-induced neutropenia (CIN) and other toxicities associated with ADC therapy, with or without the addition of immune checkpoint inhibitors.

Other names

plinabulin + TOP1-ADCplinabulin + topoisomerase I inhibitor antibody-drug conjugateplinabulin + topoisomerase inhibitor ADC