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Insights into the cellular pharmacological properties of the BET-inhibitor OTX015/MK-8628 (birabresib), alone and in combination, in leukemia models.

Astorgues-Xerri L, Vázquez R, Odore E, Rezai K, Kahatt C, Mackenzie S, Bekradda M, Coudé MM, Dombret H, Gardin C, Lokiec F, Raymond E, Noel K, Cvitkovic E, Herait P, Bertoni F, Riveiro ME.

Leuk Lymphoma. 2019 Jun 17:1-4. doi: 10.1080/10428194.2019.1617860. [Epub ahead of print] No abstract available.


Epigenetic Control of Mitochondrial Fission Enables Self-Renewal of Stem-like Tumor Cells in Human Prostate Cancer.

Civenni G, Bosotti R, Timpanaro A, Vàzquez R, Merulla J, Pandit S, Rossi S, Albino D, Allegrini S, Mitra A, Mapelli SN, Vierling L, Giurdanella M, Marchetti M, Paganoni A, Rinaldi A, Losa M, Mira-Catò E, D'Antuono R, Morone D, Rezai K, D'Ambrosio G, Ouafik L, Mackenzie S, Riveiro ME, Cvitkovic E, Carbone GM, Catapano CV.

Cell Metab. 2019 May 20. pii: S1550-4131(19)30244-X. doi: 10.1016/j.cmet.2019.05.004. [Epub ahead of print]


BET bromodomain inhibitor birabresib in mantle cell lymphoma: in vivo activity and identification of novel combinations to overcome adaptive resistance.

Tarantelli C, Bernasconi E, Gaudio E, Cascione L, Restelli V, Arribas AJ, Spriano F, Rinaldi A, Mensah AA, Kwee I, Ponzoni M M.D, Zucca E, Carrassa L, Riveiro ME, Rezai K, Stathis A, Cvitkovic E, Bertoni F.

ESMO Open. 2018 Sep 26;3(6):e000387. doi: 10.1136/esmoopen-2018-000387. eCollection 2018.


Individual Amino Acid Supplementation Can Improve Energy Metabolism and Decrease ROS Production in Neuronal Cells Overexpressing Alpha-Synuclein.

Delic V, Griffin JWD, Zivkovic S, Zhang Y, Phan TA, Gong H, Chaput D, Reynes C, Dinh VB, Cruz J, Cvitkovic E, Placides D, Frederic E, Mirzaei H, Stevens SM Jr, Jinwal U, Lee DC, Bradshaw PC.

Neuromolecular Med. 2017 Sep;19(2-3):322-344. doi: 10.1007/s12017-017-8448-8. Epub 2017 Jun 15.


The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with everolimus.

Vázquez R, Riveiro ME, Astorgues-Xerri L, Odore E, Rezai K, Erba E, Panini N, Rinaldi A, Kwee I, Beltrame L, Bekradda M, Cvitkovic E, Bertoni F, Frapolli R, D'Incalci M.

Oncotarget. 2017 Jan 31;8(5):7598-7613. doi: 10.18632/oncotarget.13814.


OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations.

Riveiro ME, Astorgues-Xerri L, Vazquez R, Frapolli R, Kwee I, Rinaldi A, Odore E, Rezai K, Bekradda M, Inghirami G, D'Incalci M, Noel K, Cvitkovic E, Raymond E, Bertoni F.

Oncotarget. 2016 Dec 20;7(51):84675-84687. doi: 10.18632/oncotarget.13181.


Therapeutic efficacy of the bromodomain inhibitor OTX015/MK-8628 in ALK-positive anaplastic large cell lymphoma: an alternative modality to overcome resistant phenotypes.

Boi M, Todaro M, Vurchio V, Yang SN, Moon J, Kwee I, Rinaldi A, Pan H, Crescenzo R, Cheng M, Cerchietti L, Elemento O, Riveiro ME, Cvitkovic E, Bertoni F, Inghirami G; AIRC 5xMille Consortium ‘Genetics-Driven Targeted Management of Lymphoid Malignancies’.

Oncotarget. 2016 Nov 29;7(48):79637-79653. doi: 10.18632/oncotarget.12876.


Promising in vivo efficacy of the BET bromodomain inhibitor OTX015/MK-8628 in malignant pleural mesothelioma xenografts.

Vázquez R, Licandro SA, Astorgues-Xerri L, Lettera E, Panini N, Romano M, Erba E, Ubezio P, Bello E, Libener R, Orecchia S, Grosso F, Riveiro ME, Cvitkovic E, Bekradda M, D'Incalci M, Frapolli R.

Int J Cancer. 2017 Jan 1;140(1):197-207. doi: 10.1002/ijc.30412. Epub 2016 Sep 19.


Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma.

Gaudio E, Tarantelli C, Ponzoni M, Odore E, Rezai K, Bernasconi E, Cascione L, Rinaldi A, Stathis A, Riveiro E, Cvitkovic E, Zucca E, Bertoni F.

Oncotarget. 2016 Sep 6;7(36):58142-58147. doi: 10.18632/oncotarget.10983.


OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models.

Berenguer-Daizé C, Astorgues-Xerri L, Odore E, Cayol M, Cvitkovic E, Noel K, Bekradda M, MacKenzie S, Rezai K, Lokiec F, Riveiro ME, Ouafik L.

Int J Cancer. 2016 Nov 1;139(9):2047-55. doi: 10.1002/ijc.30256. Epub 2016 Jul 30.


Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition.

Henssen A, Althoff K, Odersky A, Beckers A, Koche R, Speleman F, Schäfers S, Bell E, Nortmeyer M, Westermann F, De Preter K, Florin A, Heukamp L, Spruessel A, Astrahanseff K, Lindner S, Sadowski N, Schramm A, Astorgues-Xerri L, Riveiro ME, Eggert A, Cvitkovic E, Schulte JH.

Clin Cancer Res. 2016 May 15;22(10):2470-81. doi: 10.1158/1078-0432.CCR-15-1449. Epub 2015 Dec 2.


Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies.

Odore E, Lokiec F, Cvitkovic E, Bekradda M, Herait P, Bourdel F, Kahatt C, Raffoux E, Stathis A, Thieblemont C, Quesnel B, Cunningham D, Riveiro ME, Rezaï K.

Clin Pharmacokinet. 2016 Mar;55(3):397-405. doi: 10.1007/s40262-015-0327-6.


The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs.

Boi M, Gaudio E, Bonetti P, Kwee I, Bernasconi E, Tarantelli C, Rinaldi A, Testoni M, Cascione L, Ponzoni M, Mensah AA, Stathis A, Stussi G, Riveiro ME, Herait P, Inghirami G, Cvitkovic E, Zucca E, Bertoni F.

Clin Cancer Res. 2015 Apr 1;21(7):1628-38. doi: 10.1158/1078-0432.CCR-14-1561. Epub 2015 Jan 26.


Fsn0503h antibody-mediated blockade of cathepsin S as a potential therapeutic strategy for the treatment of solid tumors.

Vázquez R, Astorgues-Xerri L, Bekradda M, Gormley J, Buick R, Kerr P, Cvitkovic E, Raymond E, D'Incalci M, Frapolli R, Riveiro ME.

Biochimie. 2015 Jan;108:101-7. doi: 10.1016/j.biochi.2014.10.025. Epub 2014 Nov 5.


OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis.

Astorgues-Xerri L, Riveiro ME, Tijeras-Raballand A, Serova M, Rabinovich GA, Bieche I, Vidaud M, de Gramont A, Martinet M, Cvitkovic E, Faivre S, Raymond E.

Eur J Cancer. 2014 Sep;50(14):2463-77. doi: 10.1016/j.ejca.2014.06.015. Epub 2014 Jul 16.


Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib.

Zucchetti M, Bonezzi K, Frapolli R, Sala F, Borsotti P, Zangarini M, Cvitkovic E, Noel K, Ubezio P, Giavazzi R, D'Incalci M, Taraboletti G.

Cancer Chemother Pharmacol. 2013 Oct;72(4):879-87. doi: 10.1007/s00280-013-2270-2. Epub 2013 Aug 24.


Spectrum of cellular responses to pyriplatin, a monofunctional cationic antineoplastic platinum(II) compound, in human cancer cells.

Lovejoy KS, Serova M, Bieche I, Emami S, D'Incalci M, Broggini M, Erba E, Gespach C, Cvitkovic E, Faivre S, Raymond E, Lippard SJ.

Mol Cancer Ther. 2011 Sep;10(9):1709-19. doi: 10.1158/1535-7163.MCT-11-0250. Epub 2011 Jul 12.


Single agent and combination studies of pralatrexate and molecular correlates of sensitivity.

Serova M, Bieche I, Sablin MP, Pronk GJ, Vidaud M, Cvitkovic E, Faivre S, Raymond E.

Br J Cancer. 2011 Jan 18;104(2):272-80. doi: 10.1038/sj.bjc.6606063. Epub 2010 Dec 21.


ProLindac (AP5346): a review of the development of an HPMA DACH platinum Polymer Therapeutic.

Nowotnik DP, Cvitkovic E.

Adv Drug Deliv Rev. 2009 Nov 12;61(13):1214-9. doi: 10.1016/j.addr.2009.06.004. Epub 2009 Aug 9. Review.


Epithelial-to-mesenchymal transition and resistance to ingenol 3-angelate, a novel protein kinase C modulator, in colon cancer cells.

Ghoul A, Serova M, Astorgues-Xerri L, Bieche I, Bousquet G, Varna M, Vidaud M, Phillips E, Weill S, Benhadji KA, Lokiec F, Cvitkovic E, Faivre S, Raymond E.

Cancer Res. 2009 May 15;69(10):4260-9. doi: 10.1158/0008-5472.CAN-08-2837. Epub 2009 May 5.


Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells.

Benhadji KA, Serova M, Ghoul A, Cvitkovic E, Le Tourneau C, Ogbourne SM, Lokiec F, Calvo F, Hammel P, Faivre S, Raymond E.

Br J Cancer. 2008 Dec 2;99(11):1808-15. doi: 10.1038/sj.bjc.6604642.


Effects of protein kinase C modulation by PEP005, a novel ingenol angelate, on mitogen-activated protein kinase and phosphatidylinositol 3-kinase signaling in cancer cells.

Serova M, Ghoul A, Benhadji KA, Faivre S, Le Tourneau C, Cvitkovic E, Lokiec F, Lord J, Ogbourne SM, Calvo F, Raymond E.

Mol Cancer Ther. 2008 Apr;7(4):915-22. doi: 10.1158/1535-7163.MCT-07-2060.


Antiproliferative effects of sapacitabine (CYC682), a novel 2'-deoxycytidine-derivative, in human cancer cells.

Serova M, Galmarini CM, Ghoul A, Benhadji K, Green SR, Chiao J, Faivre S, Cvitkovic E, Le Tourneau C, Calvo F, Raymond E.

Br J Cancer. 2007 Sep 3;97(5):628-36. Epub 2007 Jul 17.


A phase I and pharmacokinetic study of irofulven and capecitabine administered every 2 weeks in patients with advanced solid tumors.

Alexandre J, Kahatt C, Bertheault-Cvitkovic F, Faivre S, Shibata S, Hilgers W, Goldwasser F, Lokiec F, Raymond E, Weems G, Shah A, MacDonald JR, Cvitkovic E.

Invest New Drugs. 2007 Oct;25(5):453-62. Epub 2007 Jul 13.


A phase II study of an oxaliplatin/vinorelbine/5-fluorouracil combination in patients with anthracycline-pretreated and taxane-pretreated metastatic breast cancer.

Delozier T, Guastalla JP, Yovine A, Levy C, Chollet P, Mousseau M, Delva R, Coeffic D, Vannetzel JM, Zazzi ES, Brienza S, Cvitkovic E.

Anticancer Drugs. 2006 Oct;17(9):1067-73.


Repression of cell cycle-related proteins by oxaliplatin but not cisplatin in human colon cancer cells.

Voland C, Bord A, Péleraux A, Pénarier G, Carrière D, Galiègue S, Cvitkovic E, Jbilo O, Casellas P.

Mol Cancer Ther. 2006 Sep;5(9):2149-57.


Pharmacokinetics, metabolism, and routes of excretion of intravenous irofulven in patients with advanced solid tumors.

Paci A, Rezai K, Deroussent A, De Valeriola D, Re M, Weill S, Cvitkovic E, Kahatt C, Shah A, Waters S, Weems G, Vassal G, Lokiec F.

Drug Metab Dispos. 2006 Nov;34(11):1918-26. Epub 2006 Aug 8.


Preclinical and clinical development of novel agents that target the protein kinase C family.

Serova M, Ghoul A, Benhadji KA, Cvitkovic E, Faivre S, Calvo F, Lokiec F, Raymond E.

Semin Oncol. 2006 Aug;33(4):466-78. Review.


A phase I and pharmacokinetic study of irofulven and cisplatin administered in a 30-min infusion every two weeks to patients with advanced solid tumors.

Hilgers W, Faivre S, Chieze S, Alexandre J, Lokiec F, Goldwasser F, Raymond E, Kahatt C, Taamma A, Weems G, MacDonald JR, Misset JL, Cvitkovic E.

Invest New Drugs. 2006 Jul;24(4):311-9.


Oxaliplatin combined with 5-FU in second line treatment of advanced pancreatic adenocarcinoma. Results of a phase II trial.

Mitry E, Ducreux M, Ould-Kaci M, Boige V, Seitz JF, Bugat R, Breau JL, Bouché O, Etienne PL, Tigaud JM, Morvan F, Cvitkovic E, Rougier P.

Gastroenterol Clin Biol. 2006 Mar;30(3):357-63.


Phase II study of an oxaliplatin/vinorelbine combination in patients with anthracycline- and taxane-pre-treated metastatic breast cancer.

Petit T, Benider A, Yovine A, Bougnoux P, Spaeth D, Maindrault-Goebel F, Serin D, Tigaud JD, Eymard JC, Simon H, Bertaux B, Brienza S, Cvitkovic E.

Anticancer Drugs. 2006 Mar;17(3):337-43.


A phase II study of a paclitaxel and oxaliplatin combination in platinum-sensitive recurrent advanced ovarian cancer patients.

Viens P, Petit T, Yovine A, Bougnoux P, Deplanque G, Cottu PH, Delva R, Lotz JP, Belle SV, Extra JM, Cvitkovic E.

Ann Oncol. 2006 Mar;17(3):429-36.


Characterizations of irofulven cytotoxicity in combination with cisplatin and oxaliplatin in human colon, breast, and ovarian cancer cells.

Serova M, Calvo F, Lokiec F, Koeppel F, Poindessous V, Larsen AK, Laar ES, Waters SJ, Cvitkovic E, Raymond E.

Cancer Chemother Pharmacol. 2006 Apr;57(4):491-9. Epub 2005 Aug 2.


Characterization and multiparameter analysis of visual adverse events in irofulven single-agent phase I and II trials.

Raymond E, Kahatt C, Rigolet MH, Sutherland W, Lokiec F, Alexandre J, Tombal B, Elman M, Lee MS, MacDonald JR, Cullen M, Misset JL, Cvitkovic E.

Clin Cancer Res. 2004 Nov 15;10(22):7566-74. Erratum in: Clin Cancer Res. 2005 Feb 15;11(4):1684.


Phase I and pharmacokinetic study of irofulven administered weekly or biweekly in advanced solid tumor patients.

Alexandre J, Raymond E, Kaci MO, Brain EC, Lokiec F, Kahatt C, Faivre S, Yovine A, Goldwasser F, Smith SL, MacDonald JR, Misset JL, Cvitkovic E.

Clin Cancer Res. 2004 May 15;10(10):3377-85.


Randomized phase II study evaluating oxaliplatin alone, oxaliplatin combined with infusional 5-FU, and infusional 5-FU alone in advanced pancreatic carcinoma patients.

Ducreux M, Mitry E, Ould-Kaci M, Boige V, Seitz JF, Bugat R, Breau JL, Bouché O, Etienne PL, Tigaud JM, Morvan F, Cvitkovic E, Rougier P.

Ann Oncol. 2004 Mar;15(3):467-73.


Phase II study of ecteinascidin-743 in advanced pretreated soft tissue sarcoma patients.

Yovine A, Riofrio M, Blay JY, Brain E, Alexandre J, Kahatt C, Taamma A, Jimeno J, Martin C, Salhi Y, Cvitkovic E, Misset JL.

J Clin Oncol. 2004 Mar 1;22(5):890-9.


Phase I and pharmacological study of an oxaliplatin and carboplatin combination in advanced malignancies.

Mita C, Chatelut E, Bekradda M, Soulié P, Canal P, Misset JL, Cvitkovic E, Bugat R.

Ann Oncol. 2003 Dec;14(12):1776-82.


Enhanced antitumor activity of irofulven in combination with 5-fluorouracil and cisplatin in human colon and ovarian carcinoma cells.

Poindessous V, Koeppel F, Raymond E, Cvitkovic E, Waters SJ, Larsen AK.

Int J Oncol. 2003 Nov;23(5):1347-55.


Phase II study of oxaliplatin versus oxaliplatin combined with infusional 5-fluorouracil in hormone refractory metastatic prostate cancer patients.

Droz JP, Muracciole X, Mottet N, Ould Kaci M, Vannetzel JM, Albin N, Culine S, Rodier JM, Misset JL, Mackenzie S, Cvitkovic E, Benoit G.

Ann Oncol. 2003 Aug;14(8):1291-8.


Phase I population pharmacokinetics of irofulven.

Urien S, Alexandre J, Raymond E, Brain E, Smith S, Shah A, Cvitkovic E, Lokiec F.

Anticancer Drugs. 2003 Jun;14(5):353-8.


Cancer of the nasopharynx.

Licitra L, Bernier J, Cvitkovic E, Grandi C, Spinazzé S, Bruzzi P, Gatta G, Molinari R.

Crit Rev Oncol Hematol. 2003 Feb;45(2):199-213. Review.


Cellular and molecular pharmacology of oxaliplatin.

Raymond E, Faivre S, Chaney S, Woynarowski J, Cvitkovic E.

Mol Cancer Ther. 2002 Jan;1(3):227-35. Review.


Phase II study of oxaliplatin, fluorouracil, and folinic acid in locally advanced or metastatic gastric cancer patients.

Louvet C, André T, Tigaud JM, Gamelin E, Douillard JY, Brunet R, François E, Jacob JH, Levoir D, Taamma A, Rougier P, Cvitkovic E, de Gramont A.

J Clin Oncol. 2002 Dec 1;20(23):4543-8.


Irinotecan plus oxaliplatin: a promising combination for advanced colorectal cancer.

Wasserman E, Sutherland W, Cvitkovic E.

Clin Colorectal Cancer. 2001 Nov;1(3):149-53. Review.


Exacerbation of oxaliplatin neurosensory toxicity following surgery.

Gornet JM, Savier E, Lokiec F, Cvitkovic E, Misset JL, Goldwasser F.

Ann Oncol. 2002 Aug;13(8):1315-8.


Influence of oxaliplatin on 5-fluorouracil plasma clearance and clinical consequences.

Boisdron-Celle M, Craipeau C, Brienza S, Delva R, Guérin-Meyer V, Cvitkovic E, Gamelin E.

Cancer Chemother Pharmacol. 2002 Mar;49(3):235-43. Epub 2002 Jan 16.


Gemcitabine combined with oxaliplatin in advanced pancreatic adenocarcinoma: final results of a GERCOR multicenter phase II study.

Louvet C, André T, Lledo G, Hammel P, Bleiberg H, Bouleuc C, Gamelin E, Flesch M, Cvitkovic E, de Gramont A.

J Clin Oncol. 2002 Mar 15;20(6):1512-8.


Oxaliplatin plus vinorelbine in advanced non-small-cell lung cancer: final results of a multicenter phase II study.

Monnet I, de CH, Soulié P, Saltiel-Voisin S, Bekradda M, Saltiel JC, Brain E, Rixe O, Yataghene Y, Misset JL, Cvitkovic E.

Ann Oncol. 2002 Jan;13(1):103-7.


A comparison of limited sampling strategies for prediction of Ecteinascidin 743 clearance when administered as a 24-h infusion.

van Kesteren C, Mathĵt RA, López-Lázaro L, Cvitkovic E, Taamma A, Jimeno JM, Guzman C, Schellens JH, Misset JL, Brain E, Hillebrand MJ, Rosing H, Beijnen JH.

Cancer Chemother Pharmacol. 2001 Dec;48(6):459-66.


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