[Chemical modification of anticancer agents from viewpoints of their pharmacokinetics].
Many derivatives modifying chemical structures have been synthesized from several drugs. These include following antibiotics: adriamycin; 4'-epiadriamycin, THP-adriamycin, demethoxy-daunomycin, aclacinomycin, mitomycin C; 7N-(p-hydroxyphenyl)-mitomycin C, bleomycin; peplomycin, oilbleomycin, neocarzinostatin; macromomycin, and following antimetabolites: 5-FU; tegafur, HCFU, 5'-DFUR, phthalidyl-5-FU, FUdR; TK-117, FF-705, Ara-C; behenoyl-Ara-C. Most derivatives of antibiotics were a low toxic type and showed a shorter distribution time and a rapid inactivation, except peplomycin and 4-demethoxy-daunomycin. Antimetabolite derivatives were a masked type. They were activated to 5-FU, FUdR or Ara-C and persisted for a long time in the body. The mode of activation and KADME varied each other. By considering these pharmacokinetic behaviors, a suitable method of administration should be established.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000378:metabolism; D000970:Antineoplastic Agents / Q000378:metabolism*; D003561:Cytarabine / Q000378:metabolism; D004317:Doxorubicin / Q000378:metabolism; D005354:Fibrosarcoma / Q000378:metabolism; D005472:Fluorouracil / Q000097:blood; D007700:Kinetics; D051379:Mice; D016685:Mitomycin; D008937:Mitomycins / Q000378:metabolism; D011817:Rabbits; D012513:Sarcoma, Experimental / Q000378:metabolism*; D005641:Tegafur / Q000378:metabolism
D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D008937:Mitomycins; D003561:Cytarabine; D005641:Tegafur; D016685:Mitomycin; D004317:Doxorubicin; D005472:Fluorouracil