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Drug Evaluations

The long and winding road for the development of tasquinimod as an oral second-generation quinoline-3-carboxamide antiangiogenic drug for the treatment of prostate cancer

Pages 1235-1243 | Published online: 13 Sep 2010

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Roberto Petrioli, Edoardo Francini, Anna Ida Fiaschi, Letizia Laera & Giandomenico Roviello. (2015) Targeted Therapies for Prostate Cancer. Cancer Investigation 33:7, pages 276-285.
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Nihar K Patel, Antoine Finianos, Kristen D Whitaker & Jeanny B Aragon-Ching. (2014) Advanced prostate cancer – patient survival and potential impact of enzalutamide and other emerging therapies. Therapeutics and Clinical Risk Management 10, pages 651-664.
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Neha Gupta, Omar Al Ustwani, Li Shen & Roberto Pili. (2014) Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer. OncoTargets and Therapy 7, pages 223-234.
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Articles from other publishers (34)

Dong Ren & Guannan Zhang. 2024. Therapy Resistance in Prostate Cancer. Therapy Resistance in Prostate Cancer 137 155 .
Julie Blatt, Jennifer E. Brondon, Elizabeth L. Nieman, Kynlon Phillips & Arti Pandya. (2023) Repurposing of antiangiogenic agents for treatment of vascular anomalies. Pharmacology & Therapeutics 250, pages 108520.
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John T. Isaacs, Susan L. Dalrymple, Lizamma Antony, David Marc Rosen, Ilsa M. Coleman, Peter S. Nelson, Maya Kostova, Iain A. Murray, Gary H. Perdew, Samuel R. Denmeade, Emmanuel S. Akinboye & W. Nathaniel Brennen. (2023) Third generation quinoline‐3‐carboxamide transcriptional disrupter of HDAC4, HIF‐1α, and MEF‐2 signaling for metastatic castration‐resistant prostate cancer. The Prostate.
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Dima A. Sabbah, Hla H. Samarat, Eveen Al‐Shalabi, Sanaa K. Bardaweel, Rima Hajjo, Kamal Sweidan, Reema Abu Khalaf, Aya M. Al‐Zuheiri & Ghassan Abushaikha. (2022) Design, Synthesis, and Biological Examination of N‐ Phenyl‐6‐fluoro‐4‐hydroxy‐2‐quinolone‐3‐carboxamides as Anticancer Agents . ChemistrySelect 7:19.
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Ashraf A. Aly, Mohamed Ramadan, Gamal El-Din A. Abuo-Rahma, Yaseen A.M.M. Elshaier, Mohammed A.I. Elbastawesy, Alan B. Brown & Stefan Bräse. 2021. 147 196 .
Paola De Cicco, Giuseppe Ercolano & Angela Ianaro. (2020) The New Era of Cancer Immunotherapy: Targeting Myeloid-Derived Suppressor Cells to Overcome Immune Evasion. Frontiers in Immunology 11.
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Manni Wang, Fan Xia, Yuquan Wei & Xiawei Wei. (2020) Molecular mechanisms and clinical management of cancer bone metastasis. Bone Research 8:1.
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Ping Gong, Hongjian Liu, Xinyu Liu, Ge Zhou, Meitian Liu, Xiaodi Yang, Wenjing Xiong, Qi Wang, Juan MaZheng RenMinfu HeXiumin Zhang. (2018) Efficacy of tasquinimod in men with metastatic castration-resistant prostate cancer. Medicine 97:46, pages e13204.
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Sahar Tahvili, Marie Törngren, Dan Holmberg, Tomas Leanderson & Fredrik Ivars. (2018) Paquinimod prevents development of diabetes in the non-obese diabetic (NOD) mouse. PLOS ONE 13:5, pages e0196598.
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Andrew J. Armstrong, Michael S. Humeniuk, Patrick Healy, Russell Szmulewitz, Carolyn Winters, Julie Kephart, Michael R. Harrison, Elia Martinez, Kelly Mundy, Susan Halabi & Daniel George. (2017) Phase Ib Trial of Cabazitaxel and Tasquinimod in Men With Heavily Pretreated Metastatic Castration Resistant Prostate Cancer (mCRPC): The CATCH Trial. The Prostate 77:4, pages 385-395.
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Raffaele Ratta, Roberta Zappasodi, Daniele Raggi, Paolo Grassi, Elena Verzoni, Andrea Necchi, Massimo Di Nicola, Roberto Salvioni, Filippo de Braud & Giuseppe Procopio. (2016) Immunotherapy advances in uro-genital malignancies. Critical Reviews in Oncology/Hematology 105, pages 52-64.
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Alessandra Modena, Francesco Massari, Chiara Ciccarese, Matteo Brunelli, Matteo Santoni, Rodolfo Montironi, Guido Martignoni & Giampaolo Tortora. (2016) Targeting Met and VEGFR Axis in Metastatic Castration-Resistant Prostate Cancer: ‘Game Over’?. Targeted Oncology 11:4, pages 431-446.
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Ida Silvestri, Susanna Cattarino, Sabrina Giantulli, Cristina Nazzari, Giulia Collalti & Alessandro Sciarra. (2016) A Perspective of Immunotherapy for Prostate Cancer. Cancers 8:7, pages 64.
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Amit R. Mehta & Andrew J. Armstrong. (2015) Tasquinimod in the treatment of castrate-resistant prostate cancer – current status and future prospects. Therapeutic Advances in Urology 8:1, pages 9-18.
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Yu Zhou, Jiang Wang, Zhanni Gu, Shuni Wang, Wei Zhu, José Luis Aceña, Vadim A. Soloshonok, Kunisuke Izawa & Hong Liu. (2016) Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas. Chemical Reviews 116:2, pages 422-518.
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Francesco Pantano, Giulia Ribelli, Michele Iuliani, Marco Fioramonti, Mark Leakos, Alice Zoccoli, Daniele Santini, Giovanni Muto & Giuseppe Tonini. (2016) New Molecular Targets in Metastatic Prostate Cancer. Journal of Cancer Therapy 07:06, pages 388-401.
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Antonio Macciò, Giulia Gramignano & Clelia Madeddu. (2015) A Multitargeted Treatment Approach for Anemia and Cachexia in Metastatic Castration-Resistant Prostate Cancer. Journal of Pain and Symptom Management 50:2, pages e1-e4.
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John T. Isaacs, Susan L. Dalrymple, D. Marc Rosen, Hans Hammers, Anders Olsson & Tomas Leanderson. (2014) Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment. Oncotarget 5:18, pages 8093-8106.
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Daniel L. Suzman, Sosipatros A. Boikos & Michael A. Carducci. (2014) Bone-targeting agents in prostate cancer. Cancer and Metastasis Reviews 33:2-3, pages 619-628.
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Jocelyn L. Wozney & Emmanuel S. Antonarakis. (2014) Growth factor and signaling pathways and their relevance to prostate cancer therapeutics. Cancer and Metastasis Reviews 33:2-3, pages 581-594.
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John G. Moffat, Joachim Rudolph & David Bailey. (2014) Phenotypic screening in cancer drug discovery — past, present and future. Nature Reviews Drug Discovery 13:8, pages 588-602.
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Nico C. van de Merbel, Peter Walland, Mikael Tiensuu & Carl J. Sennbro. (2014) Quantitative determination of the anti-tumor agent tasquinimod in human urine by liquid chromatography–tandem mass spectrometry. Journal of Chromatography B 961, pages 42-48.
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Emmanuel S. Akinboye, Ray J. Butcher, Sema Ozturk Yildirim & John T. Isaacs. (2014) 4-Hydroxy-5-methoxy- N ,1-dimethyl-2-oxo- N -[4-(trifluoromethyl)phenyl]-1,2-dihydroquinoline-3-carboxamide . Acta Crystallographica Section E Structure Reports Online 70:3, pages o297-o298.
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E. Raymond, A. Dalgleish, J.-E. Damber, M. Smith & R. Pili. (2013) Mechanisms of action of tasquinimod on the tumour microenvironment. Cancer Chemotherapy and Pharmacology 73:1, pages 1-8.
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A.J. Armstrong, M. Häggman, W.M. Stadler, J.R. Gingrich, V. Assikis, J. Polikoff, J.E. Damber, L. Belkoff, Ö. Nordle, G. Forsberg, M.A. Carducci & R. Pili. (2013) Long-term Survival and Biomarker Correlates of Tasquinimod Efficacy in a Multicenter Randomized Study of Men with Minimally Symptomatic Metastatic Castration-Resistant Prostate Cancer. Clinical Cancer Research 19:24, pages 6891-6901.
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Tian Yi Zhang, Neeraj Agarwal, Guru Sonpavde, Giuseppe DiLorenzo, Joaquim Bellmunt & Nicholas J. Vogelzang. (2013) Management of Castrate Resistant Prostate Cancer—Recent Advances and Optimal Sequence of Treatments. Current Urology Reports 14:3, pages 174-183.
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John T. Isaacs, Lizamma Antony, Susan L. Dalrymple, W. Nathaniel Brennen, Stephanie Gerber, Hans Hammers, Michel Wissing, Sushant Kachhap, Jun Luo, Li Xing, Per Björk, Anders Olsson, Anders Björk & Tomas Leanderson. (2013) Tasquinimod Is an Allosteric Modulator of HDAC4 Survival Signaling within the Compromised Cancer Microenvironment. Cancer Research 73:4, pages 1386-1399.
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Jesal C. Patel, Benjamin L. Maughan, Archana M. Agarwal, Julia A. Batten, Tian Y. Zhang & Neeraj Agarwal. (2013) Emerging Molecularly Targeted Therapies in Castration Refractory Prostate Cancer. Prostate Cancer 2013, pages 1-12.
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Michael T. Schweizer & Michael A. Carducci. (2013) From Bevacizumab to Tasquinimod. The Cancer Journal 19:1, pages 99-106.
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Karin Jennbacken, Karin Welén, Anders Olsson, Bengt Axelsson, Marie Törngren, Jan‐Erik Damber & Tomas Leanderson. (2011) Inhibition of metastasis in a castration resistant prostate cancer model by the quinoline‐3‐carboxamide tasquinimod (ABR‐215050). The Prostate 72:8, pages 913-924.
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Susan L. Dalrymple, Robyn E. Becker, Haoming Zhou, Theodore L. DeWeese & John T. Isaacs. (2012) Tasquinimod prevents the angiogenic rebound induced by fractionated radiation resulting in an enhanced therapeutic response of prostate cancer xenografts. The Prostate 72:6, pages 638-648.
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G.P. Hansson, M. Olin, C. Svanström, L.D. Svensson & C.J. Sennbro. (2011) Bioanalysis in clinical development of tasquinimod using liquid chromatography/tandem mass spectrometry. Journal of Chromatography B 879:30, pages 3401-3406.
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Roberto PiliMichael HäggmanWalter M. StadlerJeffrey R. GingrichVasileios J. AssikisAnders BjörkÖrjan NordleGoran ForsbergMichael A. CarducciAndrew J. Armstrong. (2011) Phase II Randomized, Double-Blind, Placebo-Controlled Study of Tasquinimod in Men With Minimally Symptomatic Metastatic Castrate-Resistant Prostate Cancer. Journal of Clinical Oncology 29:30, pages 4022-4028.
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Yi Jiang, Ze-Hong Miao, Lei Xu, Bing Yu, Jing-Xu Gong, Lin-Jiang Tong, Yi Chen, Zhao-Li Zhou, Hong-Chun Liu, Yi Wang, Yue-Wei Guo & Jian Ding. (2011) Drug Transporter-independent Liver Cancer Cell Killing by a Marine Steroid Methyl Spongoate via Apoptosis Induction. Journal of Biological Chemistry 286:30, pages 26461-26469.
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