131I-YZHER2:V2

131I-YZHER2:V2 is a targeted radiopharmaceutical composed of a HER2-specific affibody (YZHER2:V2) labeled with the beta- and gamma-emitting radionuclide iodine-131. The affibody binds with high affinity and specificity to human epidermal growth factor receptor 2 (HER2), which is overexpressed in certain cancer types such as ovarian and breast cancer. Through intravenous administration, the drug achieves selective uptake and prolonged retention in HER2-overexpressing tumors, allowing for focused delivery of cytotoxic ionizing radiation to tumor cells (targeted radionuclide therapy). The radiolabeled affibody is cleared primarily via renal and gastrointestinal excretion. 131I-YZHER2:V2 has demonstrated significant tumor growth inhibition and survival benefit in preclinical models of HER2-positive ovarian cancer, and has been proposed as a novel agent for HER2-targeted radionuclide therapy. Mechanistically, the agent delivers isotope-mediated radiation to HER2-expressing cells via selective binding of the affibody, with downstream effects of DNA damage and cancer cell death. The product is synthesized using genetic recombination, labeled with iodine-131 by chloramine T, and formulated for intravenous use. Preclinical studies suggest favorable pharmacokinetics and biodistribution, rapid blood clearance, high tumor:background ratio, and evidence of therapeutic efficacy in HER2-positive tumor xenografts[1][3].

Other names

YZHER2:V2 labeled with iodine-131