Phase I clinical and pharmacokinetic study of PM01183 (a tetrahydroisoquinoline, Lurbinectedin) in combination with gemcitabine in patients with advanced solid tumors

Author:

Paz-Ares Luis,Forster Martin,Boni Valentina,Szyldergemajn Sergio,Corral Jesús,Turnbull Samantha,Cubillo Antonio,Teruel Carlos Fernandez,Calderero Iker López,Siguero Mariano,Bohan Patrick,Calvo Emiliano

Funder

Pharma Mar, S.A.

Publisher

Springer Science and Business Media LLC

Subject

Pharmacology (medical),Pharmacology,Oncology

Reference28 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(5):1099–1110

2. Bueren-Calabuig JA, Giraudon C, Galmarini CM, Egly JM, Gago F (2011) Temperature-induced melting of double-stranded DNA in the absence and presence of covalently bonded antitumour drugs: insight from molecular dynamics simulations. Nucleic Acids Res 39(18):8248–8257. doi: 10.1093/nar/gkr512

3. Santamaria G, Martínez-Leal JF, Cuevas C, Garcia-Fernandez LF, Galmarini CM Lurbinectedin (PM01183) specifically targets RNA Pol II for degradation via the proteasome pathway in a transcription and TC-NER dependent fashion. Eur J Cancer 50:20. doi: 10.1016/S0959-8049(14)70173-x

4. Soares DG, Machado MS, Rocca CJ, Poindessous V, Ouaret D, Sarasin A, Galmarini CM, Henriques JA, Escargueil AE, Larsen AK (2011) Trabectedin and its C subunit modified analogue PM01183 attenuate nucleotide excision repair and show activity toward platinum-resistant cells. Mol Cancer Ther 10(8):1481–1489. doi: 10.1158/1535-7163.MCT-11-0252

5. 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. doi: 10.1158/1535-7163.mct-16-0172

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