[Progress in the studies on antitumor natural product ecteinascidin-743].
The alkaloid ecteinascidin-743, isolated from the marine tunicate Ecteinascidia turbinata, binds to DNA and induces cytotoxic effects in several tumors. The drug is being codeveloped by Pharma Mar and Ortho Biotech. In May 2001 and October 2003, it was granted orphan drug status by the European Commission for soft tissue sarcoma and ovarian cancer, respectively. This paper reviews its research progress, including chemical synthesis, in vitro studies and mechanism of action, antitumor activity in vivo, toxicity, pharmacokinetics, and clinical studies.
Wang
Ye
Y
Department of Drug Synthesis, Institute of Materia Medica, CAMS and PUMC, Beijing 100050, China.
Liu
Zhan-zhu
ZZ
Chen
Shi-zhi
SZ
Liang
Xiao-tian
XT
D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D004149:Dioxoles / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D006801:Humans; D007546:Isoquinolines / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D044005:Tetrahydroisoquinolines; D000077606:Trabectedin
D018906:Antineoplastic Agents, Alkylating; D004149:Dioxoles; D007546:Isoquinolines; D044005:Tetrahydroisoquinolines; D000077606:Trabectedin