Phase I study of lurbinectedin, a synthetic tetrahydroisoquinoline that inhibits activated transcription, induces DNA single- and double-strand breaks, on a weekly × 2 every-3-week schedule

Author:

Jimeno Antonio,Sharma Manish R.,Szyldergemajn Sergio,Gore Lia,Geary David,Diamond Jennifer R.,Fernandez Teruel Carlos,Soto Matos-Pita Arturo,Iglesias Jorge Luis,Cullell-Young Martin,Ratain Mark J.

Funder

Pharma Mar SA

Publisher

Springer Science and Business Media LLC

Subject

Pharmacology (medical),Pharmacology,Oncology

Reference8 articles.

1. Leal JF, Martinez-Diez M, Garcia-Hernandez V, Moneo V, Domingo A, Bueren-Calabuig JA, Negri A, Gago F, Guillen-Navarro MJ, Aviles P, Cuevas C, Garcia-Fernandez LF, Galmarini CM (2010) PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol 161:1099–1110

2. Santamaria Nunez G, Robles CM, Giraudon C, Martinez-Leal JF, Compe E, Coin F, Aviles P, Galmarini CM, Egly JM (2016) Lurbinectedin specifically triggers the degradation of phosphorylated RNA polymerase II and the formation of DNA breaks in cancer cells. Mol Cancer Ther 15:1–14. doi: 10.1158/1535-7163.MCT-16-0172

3. Santamaria G, Avila S, Moneo V, Cuevas C, García-Fernández FC, Galmarini CM (2015) Synergistic combination of lurbinectedin and PARP inhibitors in breast cancer tumor cell lines 106th Annual Meeting of the American Association for Cancer Research:Abstract 2520

4. Allavena P, Belgiovine C, Liguori M, Bello E, Frapolli R, Galmarini CM, D'Incalci M (2016) Lurbinectedin reduces tumor-associated macrophages and the production of inflammatory cytokines, chemokines, and angiogenic factors in preclinical models. 107th Annual Meeting of the American Association for Cancer Research:Abstract 1284

5. Elez ME, Tabernero J, Geary D, Macarulla T, Kang SP, Kahatt C, Pita AS, Teruel CF, Siguero M, Cullell-Young M, Szyldergemajn S, Ratain MJ (2014) First-in-human phase I study of lurbinectedin (PM01183) in patients with advanced solid tumors. Clin Cancer Res 20:2205–2214. doi: 10.1158/1078-0432.CCR-13-1880

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