Lurbinectedin (PM01183) Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
Targets
DNA minor groove ; RMG2 cell growth (Cell-based assay); RMG1 cell growth (Cell-based assay) ; 1.16 nM ;1.25 nM
In vitro
Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. Lurbinectedin plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines.
In vivo
An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of lurbinectedin-based chemotherapies.
1.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]
2.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]
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B2421611