Affiliation:
1. University Campus Bio-Medico, Medical Oncology, Via Alvaro del Portillo 200, 00128 Rome, Italy
Abstract
Ecteinascidin-743 (trabectedin, Yondelis®; PharmaMar, Madrid, Spain), a 25-year-old antineoplastic alkylating agent, has recently shown unexpected and interesting mechanisms of action. Trabectedin causes perturbation in the transcription of inducible genes (e.g., the multidrug resistance gene MDR1) and interaction with DNA repair mechanisms (e.g., the nucleotide excision repair pathway) owing to drug-related DNA double strand breaks and adduct formation. Trabectedin was the first antineoplastic agent from a marine source (namely, the Caribbean tunicate Ecteinascidia turbinata) to receive marketing authorization. This article summarizes the mechanisms of action, the complex metabolism, the main toxicities, the preclinical and clinical evidences of its antineoplastic effects in different types of cancer and, finally, the future perspectives of this promising drug.
Subject
Pharmacology,Genetics,Molecular Medicine
Reference144 articles.
1. Food-Drugs From The Sea (Proceedings of the Food-Drugs from the Sea Symposium). Kingston, RI, USA, 24–27 August, 1969). Youngken HW Jr (Ed.). Marine Technology Society, Washington, DC, USA (1970).
2. Antitumor compounds from tunicates
3. Enantioselective Total Synthesis of Ecteinascidin 743
4. Development of Yondelis® (trabectedin, ET-743). A semisynthetic process solves the supply problem
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