4'-O-TETRAHYDROPYRANYLADRIAMYCIN AS A POTENTIAL NEW ANTI-TUMOR AGENT

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  • 1 January 1982
    • journal article
    • research article
    • Vol. 42  (4) , 1462-1467
Abstract
Chemotherapy with 4''-O-tetrahydropyranyladriamycin (THP-ADM), a new derivative of adriamycin (ADM), was equally or more effective against several experimental mouse tumors than it was with ADM. When mice with [mouse] P388 leukemia were given i.p. injections of THP-ADM or ADM daily for 9 consecutive days, the maximum increases in life-span (ILS) of the mice were 190% and 175%, respectively. Eight of 24 mice treated with THP-ADM were free of tumor; 1 of 24 mice treated with ADM was free of tumor. A single i.p. injection of either drug was also effective; maximum ILS was 170% for mice treated with THP-ADM and 240% for those treated with ADM. Nine of 12 mice were free of tumor. THP-ADM was equally or slightly more effective against P388 leukemia than was ADM when either drug was given i.v. The maximum ILS was 106% with THP-ADM and 77% with ADM injections when the drug was given for 9 consecutive days. Single i.v. injections of THP-ADM or ADM were almost equally (ILS, 100%) effective. Chemotherapy with THP-ADM ws also very effective against [mouse] L1210 leukemia. THP-ADM administered i.p. 5 times, every other day starting from day 1, was more effective than ADM was against [mouse] Lewis lung carcinoma, [mouse] B16 melanoma and [mouse] colon adenocarcinoma 38 inoculated s.c. In the study with Lewis lung carcinoma, metastasis to the lungs was well suppressed by THP-ADM. ADM was more effective than was THP-ADM against [mouse] colon adenocarcinoma 26. Because THP-ADM was more cytotoxic than, or almost equally as cytotoxic as, ADM against the established cell lines from the above mouse tumors, THP-ADM probably is more efficiently transported into cultured cells.