905
Views
60
CrossRef citations to date
0
Altmetric
Drug Evaluations

Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies

, MD (Assistant Member) & , MD FACS (Director of Regional Therapies, Associate Member)
Pages 893-899 | Published online: 29 Apr 2013

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (3)

Erin McClure, Ayushi Patel, Michael J. Carr, James Sun & Jonathan S. Zager. (2021) The combination of encorafenib and binimetinib for the treatment of patients with BRAF-mutated advanced, unresectable, or metastatic melanoma: an update. Expert Review of Precision Medicine and Drug Development 6:1, pages 19-29.
Read now
Jinwoong Kim, Byeongha Choi, Daseul Im, Hoyong Jung, Hyungwoo Moon, Waqar Aman & Jung-Mi Hah. (2019) Computer-aided design and synthesis of 3-carbonyl-5-phenyl-1H-pyrazole as highly selective and potent BRAFV600E and CRAF inhibitor. Journal of Enzyme Inhibition and Medicinal Chemistry 34:1, pages 1314-1320.
Read now
Piotr Rutkowski & Christian Blank. (2014) Dabrafenib for the treatment of BRAF V600-positive melanoma: a safety evaluation. Expert Opinion on Drug Safety 13:9, pages 1249-1258.
Read now

Articles from other publishers (57)

Ankit Kumar Singh, Pankaj Sonawane, Adarsh Kumar, Harshwardhan Singh, Vladislav Naumovich, Prateek Pathak, Maria Grishina, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Amita Verma & Pradeep Kumar. (2023) Challenges and Opportunities in the Crusade of BRAF Inhibitors: From 2002 to 2022. ACS Omega 8:31, pages 27819-27844.
Crossref
Aarion Romany, Ruibin Liu, Shaoqi Zhan, Joseph Clayton & Jana Shen. (2023) Analysis of the ERK Pathway Cysteinome for Targeted Covalent Inhibition of RAF and MEK Kinases. Journal of Chemical Information and Modeling 63:8, pages 2483-2494.
Crossref
Alison Celine Dcruz, Vignesh Balaji E, Suman Manandhar, Akshara Kumar, Tanvi V. Gujaran, Paniz Hedayat & K. Sreedhara Ranganath Pai. (2023) BRAF gene as a potential target to attenuate drug resistance and treat cancer. Gene Reports 30, pages 101740.
Crossref
Ankit Kumar Singh, Adarsh Kumar, Suresh Thareja & Pradeep Kumar. (2023) Current Insights into the Role of BRAF Inhibitors in Treatment of Melanoma. Anti-Cancer Agents in Medicinal Chemistry 23:3, pages 278-297.
Crossref
Surya K. De. 2023. Medicines for Cancer. Medicines for Cancer 205 411 .
Qiang Ye, Zi Li, Yang Li, Yirong Li, Yan Zhang, Runlin Gui, Yue Cui, Qi Zhang, Lu Qian, Yuyan Xiong & Yi Yu. (2022) Exosome-Derived microRNA: Implications in Melanoma Progression, Diagnosis and Treatment. Cancers 15:1, pages 80.
Crossref
Marta Morante, Atanasio Pandiella, Piero Crespo & Ana Herrero. (2022) Immune Checkpoint Inhibitors and RAS–ERK Pathway-Targeted Drugs as Combined Therapy for the Treatment of Melanoma. Biomolecules 12:11, pages 1562.
Crossref
Ankit Kumar Singh, Jurica Novak, Adarsh Kumar, Harshwardhan Singh, Suresh Thareja, Prateek Pathak, Maria Grishina, Amita Verma, Jagat Pal Yadav, Habibullah Khalilullah, Vikas Pathania, Hemraj Nandanwar, Mariusz Jaremko, Abdul-Hamid Emwas & Pradeep Kumar. (2022) Gaussian field-based 3D-QSAR and molecular simulation studies to design potent pyrimidine–sulfonamide hybrids as selective BRAF V600E inhibitors . RSC Advances 12:46, pages 30181-30200.
Crossref
Satapanawat Sittihan, Pattarawut Sopha & Somsak Ruchirawat. (2021) Synthesis and Anticancer Activity of Pentafluorobenzenesulfonamide Derivatives as Caspase‐Dependent Apoptosis‐Inducing Agents. ChemMedChem 17:3.
Crossref
Lidija D. Vuković, Pan Chen, Sampada Mishra, Karen H. White, Jason P. Gigley & Daniel L. Levy. (2021) Nuclear Transport Factor 2 (NTF2) suppresses WM983B metastatic melanoma by modifying cell migration, metastasis, and gene expression. Scientific Reports 11:1.
Crossref
Mohammed S. Abdel-Maksoud, Rasha Mohamed Hassan, Aida Abdel-Sattar El-Azzouny, Mohamed Nabil Aboul-Enein & Chang-Hyun Oh. (2021) Anticancer profile and anti-inflammatory effect of new N-(2-((4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine sulfonamide derivatives. Bioorganic Chemistry 117, pages 105424.
Crossref
Rozita Bagheri-Yarmand, Naifa L. Busaidy, Elena McBeath, Brian P. Danysh, Kurt W. Evans, Tyler J. Moss, Argun Akcakanat, Patrick K. S. Ng, Christina M. Knippler, Jalyn A. Golden, Michelle D. Williams, Asha S. Multani, Maria E. Cabanillas, Kenna R. Shaw, Funda Meric-Bernstam, Manisha H. Shah, Matthew D. Ringel & Marie Claude Hofmann. (2021) RAC1 Alterations Induce Acquired Dabrafenib Resistance in Association with Anaplastic Transformation in a Papillary Thyroid Cancer Patient. Cancers 13:19, pages 4950.
Crossref
Mohammed S. Abdel-Maksoud, Ahmed A. B. Mohamed, Rasha M. Hassan, Mohamed A. Abdelgawad, Garri Chilingaryan, Samy Selim, Mohamed S. Abdel-Bakky & Mohammad M. Al-Sanea. (2021) Design, Synthesis and Anticancer Profile of New 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-Linked Sulfonamide Derivatives with V600EBRAF Inhibitory Effect. International Journal of Molecular Sciences 22:19, pages 10491.
Crossref
Mudasir Nabi Peerzada, Ernest Hamel, Ruoli Bai, Claudiu T. Supuran & Amir Azam. (2021) Deciphering the key heterocyclic scaffolds in targeting microtubules, kinases and carbonic anhydrases for cancer drug development. Pharmacology & Therapeutics 225, pages 107860.
Crossref
Ramona Rudalska, Jule Harbig, Marteinn T. Snaebjornsson, Sabrina Klotz, Stefan Zwirner, Liudmyla Taranets, Florian Heinzmann, Thales Kronenberger, Michael Forster, Wei Cui, Luana D’Artista, Elias Einig, Martina Hinterleitner, Werner Schmitz, Agata Dylawerska, Tae-Won Kang, Antti Poso, Mathias T. Rosenfeldt, Nisar P. Malek, Michael Bitzer, Stefan Laufer, Bernd J. Pichler, Nikita Popov, Almut Schulze, Lars Zender & Daniel Dauch. (2021) LXRα activation and Raf inhibition trigger lethal lipotoxicity in liver cancer. Nature Cancer 2:2, pages 201-217.
Crossref
Yadi Zhou, Junfei Zhao, Jiansong Fang, William Martin, Lang Li, Ruth Nussinov, Timothy A. Chan, Charis Eng & Feixiong Cheng. (2021) My personal mutanome: a computational genomic medicine platform for searching network perturbing alleles linking genotype to phenotype. Genome Biology 22:1.
Crossref
Eslam M.H. Ali, Mohammed S. Abdel-Maksoud, Usama M. Ammar, Karim I. Mersal, Kyung Ho Yoo, Park Jooryeong & Chang-Hyun Oh. (2021) Design, synthesis, and biological evaluation of novel imidazole derivatives possessing terminal sulphonamides as potential BRAFV600Einhibitors. Bioorganic Chemistry 106, pages 104508.
Crossref
Sudha Vengurlekar & Subhash Chandra Chaturvedi. 2021. Nano Drug Delivery Strategies for the Treatment of Cancers. Nano Drug Delivery Strategies for the Treatment of Cancers 107 118 .
S. X. Guo, F. He, A. L. Dai, R. F. Zhang, S. H. Chen & J. Wu. (2020) Synthesis and biological activities of novel trifluoromethylpyridine amide derivatives containing sulfur moieties. RSC Advances 10:59, pages 35658-35670.
Crossref
Usama M. Ammar, Mohammed S. Abdel-Maksoud, Eslam M.H. Ali, Karim I. Mersal, Kyung Ho Yoo & Chang-Hyun Oh. (2020) Structural optimization of imidazothiazole derivatives affords a new promising series as B-Raf V600E inhibitors; synthesis, in vitro assay and in silico screening. Bioorganic Chemistry 100, pages 103967.
Crossref
Mohammed S. Abdel-Maksoud, Eslam M.H. Ali, Usama M. Ammar, Karim I. Mersal, Kyung Ho Yoo & Chang-Hyun Oh. (2020) Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF. Bioorganic & Medicinal Chemistry 28:11, pages 115493.
Crossref
Andressa Peres de Oliveira, Luidy Kazuo Issayama, Isadora Carolina Betim Pavan, Fernando Riback Silva, Talita Diniz Melo-Hanchuk, Fernando Moreira Simabuco & Jörg Kobarg. (2020) Checking NEKs: Overcoming a Bottleneck in Human Diseases. Molecules 25:8, pages 1778.
Crossref
Abdulaziz B. Hamid & Ruben C. Petreaca. (2020) Secondary Resistant Mutations to Small Molecule Inhibitors in Cancer Cells. Cancers 12:4, pages 927.
Crossref
Zheng Zhao & Philip E. Bourne. 2020. Next Generation Kinase Inhibitors. Next Generation Kinase Inhibitors 13 28 .
Athina Moschopoulou, Stefan Zwirner, Lars Zender & Daniel Dauch. 2021. Proteinkinase Inhibitors. Proteinkinase Inhibitors 125 153 .
N. A. Seebacher, A. E. Stacy, G. M. Porter & A. M. Merlot. (2019) Clinical development of targeted and immune based anti-cancer therapies. Journal of Experimental & Clinical Cancer Research 38:1.
Crossref
Y-h. Taguchi. (2019) Drug candidate identification based on gene expression of treated cells using tensor decomposition-based unsupervised feature extraction for large-scale data. BMC Bioinformatics 19:S13.
Crossref
Ming-zhao Gao, Hong-bin Wang, Xiang-ling Chen, Wen-ting Cao, Li Fu, Yun Li, Hai-tian Quan, Cheng-ying Xie & Li-guang Lou. (2018) Aberrant modulation of ribosomal protein S6 phosphorylation confers acquired resistance to MAPK pathway inhibitors in BRAF-mutant melanoma. Acta Pharmacologica Sinica 40:2, pages 268-278.
Crossref
Hoyong Jung, Jinwoong Kim, Daseul Im, Hyungwoo Moon & Jung-Mi Hah. (2019) Design, synthesis, and in vitro evaluation of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl)-aryl amide for selective RAF inhibition. Bioorganic & Medicinal Chemistry Letters 29:4, pages 534-538.
Crossref
Abdel B. Halim. 2019. Biomarkers, Diagnostics and Precision Medicine in the Drug Industry. Biomarkers, Diagnostics and Precision Medicine in the Drug Industry 41 74 .
Sreeja Sarasamma, Yu-Heng Lai, Sung-Tzu Liang, Kechun Liu & Chung-Der Hsiao. (2018) The Power of Fish Models to Elucidate Skin Cancer Pathogenesis and Impact the Discovery of New Therapeutic Opportunities. International Journal of Molecular Sciences 19:12, pages 3929.
Crossref
B.M.E. Tullemans, J.W.M. Heemskerk & M.J.E. Kuijpers. (2018) Acquired platelet antagonism: off‐target antiplatelet effects of malignancy treatment with tyrosine kinase inhibitors. Journal of Thrombosis and Haemostasis 16:9, pages 1686-1699.
Crossref
Han-Hee Park, Se-Yeon Park, Shinmee Mah, Jung-Hee Park, Soon-Sun Hong, Sungwoo Hong & You-Sun Kim. (2018) HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Experimental & Molecular Medicine 50:9, pages 1-15.
Crossref
Junlong Li, Medha Sasane, Jie Zhang, Jing Zhao, Marie Louise Ricculli, Zhiwen Yao, Suman Redhu & James Signorovitch. (2018) Is time to progression associated with post-progression survival in previously treated metastatic non-small cell lung cancer with BRAF V600E mutation? A secondary analysis of phase II clinical trial data. BMJ Open 8:8, pages e021642.
Crossref
I-Chun Tsai, Kelly McKnight, Spencer U. McKinstry, Andrew T. Maynard, Perciliz L. Tan, Christelle Golzio, C. Thomas White, Daniel J. Price, Erica E. Davis, Heather Amrine-Madsen & Nicholas Katsanis. (2018) Small molecule inhibition of RAS/MAPK signaling ameliorates developmental pathologies of Kabuki Syndrome. Scientific Reports 8:1.
Crossref
Jimmy Caroli, Giovanni Sorrentino, Mattia Forcato, Giannino Del Sal & Silvio Bicciato. (2018) GDA, a web-based tool for Genomics and Drugs integrated analysis. Nucleic Acids Research 46:W1, pages W148-W156.
Crossref
Sebastian Brandner & Zane Jaunmuktane. (2017) Neurological update: gliomas and other primary brain tumours in adults. Journal of Neurology 265:3, pages 717-727.
Crossref
Maxim Sorokin, Roman Kholodenko, Anna Grekhova, Maria Suntsova, Margarita Pustovalova, Natalia Vorobyeva, Irina Kholodenko, Galina Malakhova, Andrew Garazha, Artem Nedoluzhko, Raif Vasilov, Elena Poddubskaya, Olga Kovalchuk, Leila Adamyan, Vladimir Prassolov, Daria Allina, Denis Kuzmin, Kirill Ignatev, Andreyan Osipov & Anton Buzdin. (2017) Acquired resistance to tyrosine kinase inhibitors may be linked with the decreased sensitivity to X-ray irradiation. Oncotarget 9:4, pages 5111-5124.
Crossref
Fatemeh Bootorabi, Hamed Manouchehri, Reza Changizi, Harlan Barker, Elisabetta Palazzo, Annalisa Saltari, Mataleena Parikka, Carlo Pincelli & Ashok Aspatwar. (2017) Zebrafish as a Model Organism for the Development of Drugs for Skin Cancer. International Journal of Molecular Sciences 18:7, pages 1550.
Crossref
Hongbin Wang, Haitian Quan & Liguang Lou. (2017) AKT is critically involved in the antagonism of BRAF inhibitor sorafenib against dabrafenib in colorectal cancer cells harboring both wild-type and mutant (V600E) BRAF genes. Biochemical and Biophysical Research Communications 489:1, pages 14-20.
Crossref
Peng-Fei Wang, Han-Yue Qiu, Ze-Feng Wang, Yong-Jiao Zhang, Zhong-Chang Wang, Dong-Dong Li & Hai-Liang Zhu. (2017) Identification of novel B-RafV600E inhibitors employing FBDD strategy. Biochemical Pharmacology 132, pages 63-76.
Crossref
E Müller, S Bauer, T Stühmer, A Mottok, C-J Scholz, T Steinbrunn, D Brünnert, A Brandl, H Schraud, S Kreßmann, A Beilhack, A Rosenwald, R C Bargou & M Chatterjee. (2016) Pan-Raf co-operates with PI3K-dependent signalling and critically contributes to myeloma cell survival independently of mutated RAS. Leukemia 31:4, pages 922-933.
Crossref
Dwight Owen & Manisha H. Shah. 2017. Management of Thyroid Nodules and Differentiated Thyroid Cancer. Management of Thyroid Nodules and Differentiated Thyroid Cancer 433 450 .
Fan Liu, Lan Wang, Fabiana Perna & Stephen D. Nimer. (2016) Beyond transcription factors: how oncogenic signalling reshapes the epigenetic landscape. Nature Reviews Cancer 16:6, pages 359-372.
Crossref
Samia Aci-Sèche, Sonia Ziada, Abdennour Braka, Rohit Arora & Pascal Bonnet. (2016) Advanced molecular dynamics simulation methods for kinase drug discovery. Future Medicinal Chemistry 8:5, pages 545-566.
Crossref
Isabella C. Glitza, Dae Won Kim, Young Kwang Chae & Kevin B. Kim. 2016. Genetics of Melanoma. Genetics of Melanoma 237 265 .
Claudio Tabolacci, Martina Cordella, Lorenzo Turcano, Stefania Rossi, Alessandro Lentini, Sabrina Mariotti, Roberto Nisini, Giovanni Sette, Adriana Eramo, Lucia Piredda, Ruggero De Maria, Francesco Facchiano & Simone Beninati. (2015) Aloe-emodin exerts a potent anticancer and immunomodulatory activity on BRAF-mutated human melanoma cells. European Journal of Pharmacology 762, pages 283-292.
Crossref
Nina F. Schwenzer & Anna Christina Pfannenberg. (2015) PET/CT, MR, and PET/MR in Lymphoma and Melanoma. Seminars in Nuclear Medicine 45:4, pages 322-331.
Crossref
Yingjun Li, Huimin Cheng, Zhang Zhang, Xiaoxi Zhuang, Jinfeng Luo, Huoyou Long, Yang Zhou, Yong Xu, Rana Taghipouran, Dan Li, Adam Patterson, Jeff Smaill, Zhengchao Tu, Donghai Wu, Xiaomei Ren & Ke Ding. (2015) N -(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors . ACS Medicinal Chemistry Letters 6:5, pages 543-547.
Crossref
Eishu Hirata, Maria?Romina Girotti, Amaya Viros, Steven Hooper, Bradley Spencer-Dene, Michiyuki Matsuda, James Larkin, Richard Marais & Erik Sahai. (2015) Intravital Imaging Reveals How BRAF Inhibition Generates Drug-Tolerant Microenvironments with High Integrin ?1/FAK Signaling. Cancer Cell 27:4, pages 574-588.
Crossref
Rohit Arora, Michela Di Michele, Elisabeth Stes, Elien Vandermarliere, Lennart Martens, Kris Gevaert, Erika Van Heerde, Joannes T. M. Linders, Dirk Brehmer, Edgar Jacoby & Pascal Bonnet. (2015) Structural Investigation of B-Raf Paradox Breaker and Inducer Inhibitors. Journal of Medicinal Chemistry 58:4, pages 1818-1831.
Crossref
Djoeke de Wit, Henk-Jan Guchelaar, Jan den Hartigh, Hans Gelderblom & Nielka P. van Erp. (2015) Individualized dosing of tyrosine kinase inhibitors: are we there yet?. Drug Discovery Today 20:1, pages 18-36.
Crossref
Botond Cseh, Eszter Doma & Manuela Baccarini. (2014) “RAF” neighborhood: Protein-protein interaction in the Raf/Mek/Erk pathway. FEBS Letters 588:15, pages 2398-2406.
Crossref
M.A. Rahman, A. Salajegheh, R.A. Smith & A.K.-Y. Lam. (2014) BRAF inhibitors: From the laboratory to clinical trials. Critical Reviews in Oncology/Hematology 90:3, pages 220-232.
Crossref
Hans Starz. (2014) Von der OP bis zur Immuntherapie. MMW - Fortschritte der Medizin 156:4, pages 41-44.
Crossref
Blanca Homet & Antoni Ribas. (2014) New drug targets in metastatic melanoma. The Journal of Pathology 232:2, pages 134-141.
Crossref
Daniele Santini, Bruno Vincenzi, Olga Venditti, Emanuela Dell’Aquila, Anna Maria FrezzaMarianna Silletta, Francesco Maria Guida, Rosario Francesco Grasso, Nicola Silvestris, Gaetano Lanzetta & Giuseppe Tonini. (2013) Sunitinib in malignant melanoma: a treatment option only for KIT -mutated patients? . Future Oncology 9:12, pages 1809-1811.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.