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Expert Opinion on Drug Discovery Volume 8, 2013 - Issue 9
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Drug Discovery Case History

The preclinical profile of crizotinib for the treatment of non-small-cell lung cancer and other neoplastic disorders

Robert Roskoski JrBlue Ridge Institute for Medical Research, 3754 Brevard Road, Suite 116, Box 19, Horse Shoe, NC 28742, USA+1 828 891 5637; +1 828 890 8130; [email protected]
(Scientific Director)
Pages 1165-1179 | Published online: 28 Jun 2013

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Siddhartha Devarakonda, Bharath Ganesh, Janelle Mann & Ramaswamy Govindan. (2015) Crizotinib: an orphan drug for treating non-small-cell lung cancer. Expert Opinion on Orphan Drugs 3:10, pages 1209-1218.
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Articles from other publishers (28)

Robert RoskoskiJr.Jr.. (2023) Deucravacitinib is an allosteric TYK2 protein kinase inhibitor FDA-approved for the treatment of psoriasis. Pharmacological Research 189, pages 106642.
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Robert RoskoskiJrJr. (2023) Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update. Pharmacological Research 187, pages 106552.
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Robert RoskoskiJr.Jr.. (2022) Janus kinase (JAK) inhibitors in the treatment of neoplastic and inflammatory disorders. Pharmacological Research 183, pages 106362.
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Robert RoskoskiJr.Jr.. (2022) Targeting BCR-Abl in the treatment of Philadelphia-chromosome positive chronic myelogenous leukemia. Pharmacological Research 178, pages 106156.
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Robert Roskoski Jr.. (2022) Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update. Pharmacological Research 175, pages 106037.
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Mohd. Imran, Syed Mohammed Basheeruddin Asdaq, Shah Alam Khan, Dhanalekshmi Unnikrishnan Meenakshi, Abdulhakeem S. Alamri, Walaa F. Alsanie, Majid Alhomrani, Yahya Mohzari, Ahmed Alrashed, Mohammed AlMotairi, Eman H. Alkhaldi, Abeer K. Alorabi, Ahmed Subeh Alshrari, Mohammad Tauseef, Abida, Saleh I. Alaqel, Ozair Alam & Md. Afroz Bakht. (2021) Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades. Pharmaceuticals 14:8, pages 710.
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Robert RoskoskiJrJr. (2021) Hydrophobic and polar interactions of FDA-approved small molecule protein kinase inhibitors with their target enzymes. Pharmacological Research 169, pages 105660.
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Robert RoskoskiJr.Jr.. (2021) Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies. Pharmacological Research 168, pages 105579.
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Christina Kannigadu, Janine Aucamp & David D. N'Da. (2020) Synthesis and in vitro antileishmanial efficacy of benzyl analogues of nifuroxazide. Drug Development Research 82:2, pages 287-295.
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Robert RoskoskiJr.Jr.. (2021) Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update. Pharmacological Research 165, pages 105463.
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Robert RoskoskiJr.Jr.. (2021) Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs). Pharmacological Research 165, pages 105422.
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Meng Cao, Yuxiang Chen, Tianming Zhao, Shangfei Wei, Ming Guo & Xin Zhai. (2020) Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations. Bioorganic & Medicinal Chemistry 28:20, pages 115715.
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Yuki Uchihara, Takayuki Kidokoro, Kenji Tago, Tadahiko Mashino, Hiroomi Tamura & Megumi Funakoshi-Tago. (2018) A major component of vitamin E, α-tocopherol inhibits the anti-tumor activity of crizotinib against cells transformed by EML4-ALK. European Journal of Pharmacology 825, pages 1-9.
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Jean-Nicolas Gallant & Christine M Lovly. (2018) Established, emerging and elusive molecular targets in the treatment of lung cancer. The Journal of Pathology 244:5, pages 565-577.
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Yuki Uchihara, Fumihito Ueda, Kenji Tago, Yosuke Nakazawa, Tomoyuki Ohe, Tadahiko Mashino, Shigenobu Yokota, Tadashi Kasahara, Hiroomi Tamura & Megumi Funakoshi-Tago. (2017) Alpha-tocopherol attenuates the anti-tumor activity of crizotinib against cells transformed by NPM-ALK. PLOS ONE 12:8, pages e0183003.
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Robert RoskoskiJr.Jr.. (2017) ROS1 protein-tyrosine kinase inhibitors in the treatment of ROS1 fusion protein-driven non-small cell lung cancers. Pharmacological Research 121, pages 202-212.
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Robert RoskoskiJr.Jr.. (2017) Vascular endothelial growth factor (VEGF) and VEGF receptor inhibitors in the treatment of renal cell carcinomas. Pharmacological Research 120, pages 116-132.
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Yikai Wang, Zhengxia Chen, Meibi Dai, Peipei Sun, Chunqiu Wang, Yang Gao, Haixia Zhao, Wenqin Zeng, Liang Shen, Weifeng Mao, Tian Wang, Guoping Hu, Jian Li, Shuhui Chen, Chaofeng Long, Xiaoxin Chen, Junhua Liu & Yang Zhang. (2017) Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping. Bioorganic & Medicinal Chemistry Letters 27:11, pages 2420-2423.
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Robert RoskoskiJr.Jr.. (2017) Anaplastic lymphoma kinase (ALK) inhibitors in the treatment of ALK-driven lung cancers. Pharmacological Research 117, pages 343-356.
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Yazan Haddad, Zbyněk Heger & Vojtech Adam. (2017) Targeting Neuroblastoma Cell Surface Proteins: Recommendations for Homology Modeling of hNET, ALK, and TrkB. Frontiers in Molecular Neuroscience 10.
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Marcello Maugeri-Saccà, Maddalena Barba, Patrizia Vici, Laura Pizzuti, Domenico Sergi, Teresa Catenaro, Luigi Di Lauro, Marcella Mottolese, Daniele Santini, Michele Milella & Ruggero De Maria. (2016) Presurgical window of opportunity trial design as a platform for testing anticancer drugs: Pros, cons and a focus on breast cancer. Critical Reviews in Oncology/Hematology 106, pages 132-142.
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Jill Stein & Janelle Mann. (2016) Specialty pharmacy services for patients receiving oral medications for solid tumors. American Journal of Health-System Pharmacy 73:11, pages 775-796.
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Robert RoskoskiJr.Jr.. (2016) Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes. Pharmacological Research 103, pages 26-48.
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Isabella A. Guedes, Rosana H. C. N. Freitas, Natália M. Cordeiro, Thaís S. do Nascimento, Tayna S. Valerio, Patrícia D. Fernandes, Laurent E. Dardenne & Carlos A. M. Fraga. (2016) LASSBio-1829 Hydrochloride: Development of a New Orally Active N -Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties . ChemMedChem 11:2, pages 234-244.
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Robert RoskoskiJr.Jr.. (2015) A historical overview of protein kinases and their targeted small molecule inhibitors. Pharmacological Research 100, pages 1-23.
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Robert RoskoskiJr.Jr.. (2014) ErbB/HER protein-tyrosine kinases: Structures and small molecule inhibitors. Pharmacological Research 87, pages 42-59.
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Anke Rauch, Dorle Hennig, Claudia Schäfer, Matthias Wirth, Christian Marx, Thorsten Heinzel, Günter Schneider & Oliver H. Krämer. (2014) Survivin and YM155: How faithful is the liaison?. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 1845:2, pages 202-220.
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Robert RoskoskiJr.Jr.. (2014) The ErbB/HER family of protein-tyrosine kinases and cancer. Pharmacological Research 79, pages 34-74.
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