folate receptor alpha (FRα)-targeted antibody-drug conjugate

A folate receptor alpha (FRα)-targeted antibody-drug conjugate (ADC) is a class of targeted cancer therapeutics designed to selectively deliver cytotoxic payloads to cancer cells overexpressing folate receptor alpha (FRα, encoded by the FOLR1 gene). FRα is a glycosylphosphatidylinositol (GPI)-anchored membrane glycoprotein involved in folate transport that is highly expressed in epithelial ovarian, fallopian tube, primary peritoneal, endometrial, and non-small cell lung cancers, while showing limited expression in normal tissues. These ADCs typically consist of an anti-FRα monoclonal antibody conjugated via a chemical linker to a potent cytotoxic payload, such as a microtubule inhibitor (e.g., maytansinoid DM4, hemiasterlin, or eribulin) or a topoisomerase I inhibitor (e.g., exatecan or DXd). Upon binding to FRα on the cell surface, the ADC is internalized via receptor-mediated endocytosis, and the payload is released intracellularly to induce cell cycle arrest and apoptosis. Mirvetuximab soravtansine (Elahere) was the first FRα-targeted ADC to receive FDA approval, with several next-generation candidates (such as rinatabart sesutecan, luveltamab tazevibulin, and AZD5335) in clinical development.

Other names

anti-FRα ADCfolate receptor alpha-targeted ADCfolate receptor alpha-targeted antibody-drug conjugateFRα-targeted ADCFRα-targeted antibody-drug conjugate