Verteporfin

Verteporfin(CL 318952; Visudyne), a benzoporphyrin derivative monoacid ring A, is a photosensitising drug for photodynamic therapy (PDT) activated by low-intensity, nonheat-generating light of 689nm wavelength.(In Vitro):Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 μM, 2.11 μM, and 5.61 μM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells. Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T.(In Vivo):Verteporfin (10 mg/kg, c.s.c.) and BMS-354825 significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen.