Esophageal cancer chemotherapy drug mitoxantrone aminoguanidine hydrazone Study
C squint tracking the Freedlander and French in 1958 were synthesized and used in animal experiments, found that mice with L1210 leukemia on the anti-tumor effect.
Experimental Study of mitoxantrone guanidine hydrazone, 1961 Regelson and Holland began clinical trials; the same year, Freireich, etc. I started on the NCT, E clinical trials. Me-GAG of the mechanism is not fully understood, may be related to embedded DNA, inhibition of DNA synthesis and inhibit the synthesis of DNA-RNA transcription on the template.
Mitoxantrone guanidine hydrazone experimental study, the drug in mice P388, L1210 leukemia, sarcoma 180, W256, and Ca-755 has anti-tumor effect. Me-GAG oral absorption is poor, commonly used intravenously to disappear rapidly from the blood half-life of about 30min, mainly from extra-renal excretion, metabolism in the body is unknown.
It can enter the brain tissue, but slowly, the brain concentrations were lower. This drug is toxic, mainly for bone marrow suppression and gastrointestinal reactions, therapeutic index is low.