[Pharmacokinetics and antitumor activity of MX2, a new morpholino anthracycline in brain tumor intracerebral transplanted in rats].
Pharmacokinetics and antitumor activity of MX2.HCl (MX2), a new morpholino anthracycline, were investigated in rats transplanted 9L gliosarcoma cells in the brain. (1) Pharmacokinetics: AUC of MX2 in the brain tumors which received intracarotid and intravenous injection of 2mg/kg of MX2 were 117.50 and 55.94 micrograms.hr/g, respectively. AUC of the brain tissue was 1.38-3.90 micrograms.hr/g. (2) Antitumor activity: The inhibition of cell growth at the concentration of 0.1 micrograms/ml was 73.1% with MTT assay. The mean survival time in tumor-bearing rats after intracarotid and intravenous injection of 2mg/kg of MX2 prolonged significantly. Therefore, it seems that MX2 will become an efficacious drug for the treatment of malignant glioma.
Kiya
K
K
Dept. of Neurosurgery, Hiroshima University School of Medicine.
Ogasawara
H
H
Fujita
H
H
Sugiyama
K
K
Kurisu
K
K
Kawamoto
K
K
Uozumi
T
T
Shinkai
H
H
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D001921:Brain / Q000378:metabolism; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D002360:Carubicin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002455:Cell Division / Q000187:drug effects; D005260:Female; D005910:Glioma / Q000188:drug therapy* / Q000378:metabolism; D009368:Neoplasm Transplantation; D051381:Rats; D011916:Rats, Inbred F344; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000903:Antibiotics, Antineoplastic; C053537:morpholinoanthracycline MX2; D002360:Carubicin