DZ-2384

**DZ-2384** is a novel synthetic derivative of diazonamide A, originally isolated from the marine organism *Diazona angulata*, designed as a microtubule-targeting agent (MTA) with enhanced potency and reduced toxicity compared to taxanes like paclitaxel and docetaxel. It binds uniquely to the vinca alkaloid site on tubulin, modifying protofilament curvature to straighten them, strongly inhibiting mitotic spindle formation in dividing cells while preserving microtubule networks in non-dividing cells such as neurons, resulting in a wide therapeutic window (14-32-fold vs. <2.8 for taxanes) and minimal peripheral neuropathy. DZ-2384 demonstrates superior antitumor efficacy in preclinical models of triple-negative breast cancer (TNBC), pancreatic cancer, colon cancer, leukemia, and brain metastases, including patient-derived xenografts (PDX) and syngeneic models, with complete regressions observed at low doses (e.g., 1.25 mg/kg); it shows synergistic effects with anti-CTLA-4 immunotherapy and gemcitabine, and selective tumor uptake (18-fold over plasma).[1][2][3][4]

Other names

AB-5 synthetic derivativeAB5 synthetic derivativeAB 5 synthetic derivative