Synonyms: PM 01183 | PM-01183 | PM01183 | Zepzelca®
lurbinectedin is an approved drug (FDA (2020))
Compound class:
Synthetic organic
Comment: Lurbinectedin (PM01183) is an investigational anti-tumour agent [3] with potential activity against a wide range of tumours. Structurally it is a synthetic tetrahydroisoquinoline that is related to the marine ecteinascidins (e.g. trabectedin). Like trabectedin, lurbinectedin binds to the minor groove of DNA. Stable lurbinectedin-DNA adducts induce DNA double- and single-strand breaks which cause cell cycle arrest and ultimately, apoptotic cell death.
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References |
1. Elez ME, Tabernero J, Geary D, Macarulla T, Kang SP, Kahatt C, Pita AS, Teruel CF, Siguero M, Cullell-Young M et al.. (2014)
First-in-human phase I study of Lurbinectedin (PM01183) in patients with advanced solid tumors. Clin Cancer Res, 20 (8): 2205-14. [PMID:24563480] |
2. Farago AF, Drapkin BJ, Lopez-Vilarino de Ramos JA, Galmarini CM, Núñez R, Kahatt C, Paz-Ares L. (2019)
ATLANTIS: a Phase III study of lurbinectedin/doxorubicin versus topotecan or cyclophosphamide/doxorubicin/vincristine in patients with small-cell lung cancer who have failed one prior platinum-containing line. Future Oncol, 15 (3): 231-239. [PMID:30362375] |
3. Leal JF, Martínez-Díez M, García-Hernández V, Moneo V, Domingo A, Bueren-Calabuig JA, Negri A, Gago F, Guillén-Navarro MJ, Avilés P et al.. (2010)
PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol, 161 (5): 1099-110. [PMID:20977459] |