redaporfin

Redaporfin is a synthetic bacteriochlorin-based photosensitizer developed for use in photodynamic therapy (PDT) of cancer. Upon intravenous administration and subsequent local illumination with light of an appropriate wavelength at the tumor site (typically after systemic administration), redaporfin preferentially accumulates in hyperproliferative tissues such as tumors. When activated by light exposure during PDT procedures it generates reactive oxygen species (ROS), including singlet oxygen and superoxide ions. These ROS induce cytotoxicity through free radical-mediated DNA damage and cell death. Mechanistically redaporfin shows selective tropism for the endoplasmic reticulum (ER) and Golgi apparatus (GA). Light activation causes ROS-dependent damage to these organelles leading to ER stress and inhibition of GA-dependent protein secretion. This triggers a cascade involving mitochondrial apoptosis pathways as well as immunogenic cell death mechanisms[1][5][6]. Redaporfin has demonstrated high efficacy in preclinical models and promising results in early clinical trials for advanced head and neck cancer; it has also received Orphan Drug Designation from the EMA for biliary tract cancer[3].

Other names

3,3',3'',3'''-(7,8,17,18-tetrahydroporphyrin-5,10,15,20-tetrayl)tetrakis(2,4-difluoro-n-methylbenzenesulfonamide)Benzenesulfonamide, 3,3',3'',3'''-(7,8,17,18-tetrahydro-21h,23h-porphine-5,10,15,20-tetrayl)tetrakis(2,4-difluoro-n-methyl-