[Etoposide VP 16--213)--a podophyllotoxinderivative with high antitumor activity (author's transl)].
Etoposide is a semisynthetic podophyllotoxin derivative with a broad spectrum of antitumor activity and a relatively high therapeutic index. The synergism in animal with cis-platinum, cyclophosphamide, BCNU, and cytosinarabinoside is interesting for combination regimen. Mechanisms of action are inhibition of nucleoside transfer and of DNA and RNA synthesis, single stranded breaks, inhibition of protein synthesis and of microtubular assembly. While in lower concentrations etoposide is acting cell-cycle-dependent with accumulation of cells in the G2-phase it has, in high concentrations, also a cellcycle-phase-unspecific lethal effect. Most suitable is the oral and i.v. application of etoposide in fractionated doses of 80--120 mg/m2 on 3--5 consecutive days and repetition after 21 [14--28] days. Side effects are dose-limiting bone marrow toxicity, nausea, vomiting, fever, hypotension, phlebitis, mucositis, neuropathy, cardiotoxicity, alopecia. Etoposide is one of the most active single agents in small-cell bronchus carcinoma with a remission rate of 37% (10% CR), and is very active in NHL (36%), testicular carcinoma (37%), AMML (35%), choriocarcinoma (35%), and neuroblastoma (29%). The role of etoposide in combination with other active drugs in these tumors is currently investigated in bronchus and testicular carcinoma and NHL, where etoposide will belong to the drugs of the first choice in the future.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002986:Clinical Trials as Topic; D004273:DNA, Neoplasm / Q000096:biosynthesis; D004359:Drug Therapy, Combination; D005047:Etoposide / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D009374:Neoplasms, Experimental / Q000188:drug therapy; D011034:Podophyllotoxin / Q000031:analogs & derivatives*; D012334:RNA, Neoplasm / Q000096:biosynthesis
D004273:DNA, Neoplasm; D012334:RNA, Neoplasm; D005047:Etoposide; D011034:Podophyllotoxin
Etoposid (VP 16--213). Eine antineoplastische Substanz aus der Reihe der Podophyllotoxine.