Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer

Kwak, E. L., Bang, Y., Camidge, D. R., Shaw, A. T., Solomon, B., Maki, R. G., Ou, S. I., Dezube, B. J., Janne, P. A., Costa, D. B., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1006448 · Cited by 4,442 · see citing works

Efficacy of Larotrectinib in <i>TRK</i> Fusion–Positive Cancers in Adults and Children

Drilon, A., Laetsch, T. W., Kummar, S., DuBois, S. G., Lassen, U. N., Demetri, G. D., Nathenson, M., Doebele, R. C., Farago, A. F., Pappo, A. S., et al. (2018) · New England Journal of Medicine · doi:10.1056/nejmoa1714448 · Cited by 2,824 · see citing works

Alectinib versus Crizotinib in Untreated <i>ALK</i> -Positive Non–Small-Cell Lung Cancer

Peters, S., Camidge, D. R., Shaw, A. T., Gadgeel, S., Ahn, J. S., Kim, D.-W., Ou, S.-H. I., Pérol, M., Dziadziuszko, R., Rosell, R., et al. (2017) · New England Journal of Medicine · doi:10.1056/nejmoa1704795 · Cited by 2,527 · see citing works

Crizotinib in <i>ROS1</i>-Rearranged Non–Small-Cell Lung Cancer

Shaw, A. T., Ou, S.-H. I., Bang, Y.-J., Camidge, D. R., Solomon, B. J., Salgia, R., Riely, G. J., Varella-Garcia, M., Shapiro, G. I., Costa, D. B., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1406766 · Cited by 1,964 · see citing works

Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK -Rearranged Lung Cancer

Gainor, J. F., Dardaei, L., Yoda, S., Friboulet, L., Leshchiner, I., Katayama, R., Dagogo‐Jack, I., Gadgeel, S. M., Schultz, K. R., Singh, M., et al. (2016) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-0596 · Cited by 1,158 · see citing works

The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non–Small Cell Lung Cancer

Friboulet, L., Li, N., Katayama, R., Lee, C. C., Gainor, J. F., Crystal, A., Michellys, P., Awad, M. M., Yanagitani, N., Kim, S., et al. (2014) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0846 · Cited by 847 · see citing works

Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1)

Drilon, A. E. D. C., Siena, S., Ou, S. I., Patel, M. R., Ahn, M., Lee, J., Bauer, T. M., Farago, A. F., Wheler, J. J., Liu, S. V., et al. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-1237 · Cited by 827 · see citing works

Lorlatinib in non-small-cell lung cancer with ALK or ROS1 rearrangement: an international, multicentre, open-label, single-arm first-in-man phase 1 trial

Shaw, A. T., Felip, E., Bauer, T. M., Besse, B., Navarro, A., Postel-Vinay, S. C., Gainor, J. F., Johnson, M. L., Dietrich, J., James, L. P., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30680-0 · Cited by 660 · see citing works

Targeting ALK: Precision Medicine Takes on Drug Resistance

Lin, J. J., Riely, G. J., & Shaw, A. T. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-1123 · Cited by 528 · see citing works

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion–Positive Solid Tumors

Drilon, A. E. D. C., Nagasubramanian, R., Blake, J. F., Ku, N. C., Tuch, B. B., Ebata, K. T., Smith, S., Lauriault, V., Kolakowski, G. R., Brandhuber, B. J., et al. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-17-0507 · Cited by 452 · see citing works

Acquired Resistance to Crizotinib from a Mutation in CD74 – ROS1

Awad, M. M., Katayama, R., McTigue, M. A., Liu, W., Deng, Y.-L., Brooun, A., Friboulet, L., Huang, D., Falk, M. D., Timofeevski, S. L., et al. (2013) · New England Journal of Medicine · doi:10.1056/nejmoa1215530 · Cited by 421 · see citing works

Fusions in solid tumours: diagnostic strategies, targeted therapy, and acquired resistance

Schram, A. M., Chang, M. T., Jonsson, P., & Drilon, A. E. D. C. (2017) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2017.127 · Cited by 328 · see citing works

Acquired Resistance to the TRK Inhibitor Entrectinib in Colorectal Cancer

Russo, M., Misale, S., Ge, W., Siravegna, G., Crisafulli, G., Lazzari, L., Corti, G., Rospo, G., Novara, L., Mussolin, B., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0940 · Cited by 316 · see citing works

What hides behind the MASC: clinical response and acquired resistance to entrectinib after ETV6-NTRK3 identification in a mammary analogue secretory carcinoma (MASC)

Drilon, A. E. D. C., Li, G., Doğan, S., Gounder, M. M., Shen, R., Arcila, M. E., Wang, L., Hyman, D. M., Hechtman, J. F., Ge, W., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw042 · Cited by 313 · see citing works

Open-Label, Multicenter, Phase II Study of Ceritinib in Patients With Non–Small-Cell Lung Cancer Harboring ROS1 Rearrangement

Lim, S. M., Kim, H. R., Lee, J.-S., Lee, K. H., Lee, Y., Min, Y. J., Cho, E. K., Lee, S. S., Kim, B.-S., Choi, M. Y., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2016.71.3701 · Cited by 305 · see citing works

Tyrosine kinase gene rearrangements in epithelial malignancies

Shaw, A. T., Hsu, P. P., Awad, M. M., & Engelman, J. A. (2013) · Nature reviews. Cancer · doi:10.1038/nrc3612 · Cited by 291 · see citing works

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

Zou, H. Y., Li, Q., Engstrom, L. D., West, M., Appleman, V. A., Wong, K. A., McTigue, M. A., Deng, Y.-L., Liu, W., Brooun, A., et al. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1420785112 · Cited by 272 · see citing works

Patterns of Metastatic Spread and Mechanisms of Resistance to Crizotinib in ROS1-Positive Non–Small-Cell Lung Cancer

Gainor, J. F., Tseng, D., Yoda, S., Dagogo‐Jack, I., Friboulet, L., Lin, J. J., Hubbeling, H., Dardaei, L., Farago, A. F., Schultz, K. R., et al. (2017) · JCO Precision Oncology · doi:10.1200/po.17.00063 · Cited by 269 · see citing works

Recent Advances in Targeting ROS1 in Lung Cancer

Lin, J. J., & Shaw, A. T. (2017) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2017.08.002 · Cited by 262 · see citing works

Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion–Positive Cancer

Katayama, R., Kobayashi, Y., Friboulet, L., Lockerman, E. L., Koike, S., Shaw, A. T., Engelman, J. A., & Fujita, N. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1385 · Cited by 204 · see citing works

Next-Generation Sequencing Reveals a Novel NSCLC ALK F1174V Mutation and Confirms ALK G1202R Mutation Confers High-Level Resistance to Alectinib (CH5424802/RO5424802) in ALK-Rearranged NSCLC Patients Who Progressed on Crizotinib

Ou, S. I., Azada, M. C., Hsiang, D. J. B., Herman, J., Kain, T. S., Siwak, C. T., Casey, C., He, J., Ali, S. M., Klempner, S. J., et al. (2014) · Journal of Thoracic Oncology · doi:10.1097/jto.0000000000000094 · Cited by 174 · see citing works

A Novel Crizotinib-Resistant Solvent-Front Mutation Responsive to Cabozantinib Therapy in a Patient with ROS1 -Rearranged Lung Cancer

Drilon, A. E. D. C., Somwar, R., Wagner, J. P., Vellore, N. A., Eide, C. A., Zabriskie, M. S., Arcila, M. E., Hechtman, J. F., Wang, L., Smith, R. S., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2013 · Cited by 169 · see citing works

Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1 -Rearranged Non–Small Cell Lung Cancer

Song, A., Kim, T. M., Kim, D., Kim, S., Keam, B., Lee, S., & Heo, D. S. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1350 · Cited by 128 · see citing works

Entrectinib in Patients with Advanced or Metastatic NTRK Fusion-Positive Solid Tumours: Integrated Analysis of Three Phase 1-2 Trials

Doebele, R. C., Drilon, A., Paz-Ares, L., Siena, S., Shaw, A. T., Farago, A. F., Blakely, C. M., Seto, T., Cho, B. C., Tosi, D., et al. (2020) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30691-6 · Cited by 1,790 · see citing works

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

Zhong, L., Li, Y., Xiong, L., Wang, W., Wu, M., Yuan, T., Yang, W. M., Tian, C., Miao, Z., Wang, T., et al. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-021-00572-w · Cited by 1,735 · see citing works

An Update on the Nitrogen Heterocycle Compositions and Properties of U.S. FDA-Approved Pharmaceuticals (2013–2023)

Marshall, C. M., Federice, J. G., Bell, C. N., Cox, P. B., & Njardarson, J. T. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01122 · Cited by 1,112 · see citing works

Kinase drug discovery 20 years after imatinib: progress and future directions

Cohen, P., Cross, D. A. E., & Janne, P. A. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00195-4 · Cited by 1,066 · see citing works

Systemic Therapy for Locally Advanced and Metastatic Non–Small Cell Lung Cancer

Arbour, K. C., & Riely, G. J. (2019) · JAMA · doi:10.1001/jama.2019.11058 · Cited by 1,061 · see citing works

Larotrectinib in Patients with TRK Fusion-Positive Solid Tumours: A Pooled Analysis of Three Phase 1/2 Clinical Trials

Hong, D. S., DuBois, S. G., Kummar, S., Farago, A. F., Albert, C. M., Rohrberg, K. S., van Tilburg, C. M., Nagasubramanian, R., Berlin, J. D., Federman, N., et al. (2020) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30856-3 · Cited by 1,028 · see citing works

Non–Small Cell Lung Cancer, Version 4.2024

Riely, G. J., Wood, D. E., Ettinger, D. S., Aisner, D. L., Akerley, W., Bauman, J. R., Bharat, A., Bruno, D. S., Chang, J. Y., Chirieac, L. R., et al. (2024) · Journal of the National Comprehensive Cancer Network · doi:10.6004/jnccn.2204.0023 · Cited by 897 · see citing works

Small molecules, big impact: 20 years of targeted therapy in oncology

Bedard, P. L., Hyman, D. M., Davids, M. S., & Siu, L. L. (2020) · The Lancet · doi:10.1016/s0140-6736(20)30164-1 · Cited by 616 · see citing works

Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three phase 1–2 trials

Drilon, A. E. D. C., Siena, S., Dziadziuszko, R., Barlési, F., Krebs, M., Shaw, A. T., de Braud, F., Rolfo, C. D., Ahn, M., Wolf, J., et al. (2019) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30690-4 · Cited by 533 · see citing works

Challenges and Opportunities in Cancer Drug Resistance

Ward, R. A., Fawell, S. E., Floc’h, N., Flemington, V., McKerrecher, D., & Smith, P. D. (2020) · Chemical Reviews · doi:10.1021/acs.chemrev.0c00383 · Cited by 454 · see citing works

Targeted Therapy and Checkpoint Immunotherapy in Lung Cancer

Ruiz‐Cordero, R., & Devine, W. P. (2020) · Surgical pathology clinics · doi:10.1016/j.path.2019.11.002 · Cited by 452 · see citing works

Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update

Roskoski, R. J. (2024) · Pharmacological Research · doi:10.1016/j.phrs.2024.107059 · Cited by 404 · see citing works

ESMO recommendations on the standard methods to detect NTRK fusions in daily practice and clinical research

Marchiò, C., Scaltriti, M., Ladanyi, M., Iafrate, A. J., Bibeau, F., Dietel, M., Hechtman, J. F., Troiani, T., López‐Ríos, F., Douillard, J.-Y., et al. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz204 · Cited by 371 · see citing works

Understanding and targeting resistance mechanisms in cancer

Lei, Z., Qin, T., Teng, Q., Wurpel, J. N. D., Zeng, L., Pan, Y., & Chen, Z. (2023) · MedComm · doi:10.1002/mco2.265 · Cited by 378 · see citing works

Recent advances in non-small cell lung cancer targeted therapy; an update review

Araghi, M., Mannani, R., Maleki, A. H., Hamidi, A., Rostami, S. M., Safa, S. H., Faramarzi, F., Khorasani, S., Alimohammadi, M., Tahmasebi, S., et al. (2023) · Cancer Cell International · doi:10.1186/s12935-023-02990-y · Cited by 352 · see citing works

Overcoming resistance to tumor-targeted and immune-targeted therapies

Aldea, M., Andre, F., Marabelle, A., Dogan, S., Barlesi, F., & Soria, J.-C. (2021) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-1638 · Cited by 311 · see citing works

Protein tyrosine kinase inhibitor resistance in malignant tumors: molecular mechanisms and future perspective

Yang, Y., Li, S., Wang, Y., Zhao, Y., & Li, Q. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-01168-8 · Cited by 315 · see citing works

ROS1-dependent cancers — biology, diagnostics and therapeutics

Drilon, A. E. D. C., Jenkins, C., Iyer, S. R., Schoenfeld, A. J., Keddy, C., & Davare, M. A. (2020) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-020-0408-9 · Cited by 297 · see citing works

TRK inhibitors in TRK fusion-positive cancers

Drilon, A. E. D. C. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz282 · Cited by 297 · see citing works

Somatic Genomic Testing in Patients With Metastatic or Advanced Cancer: ASCO Provisional Clinical Opinion

Chakravarty, D., Johnson, A., Sklar, J., Lindeman, N. I., Moore, K. N., Ganesan, S., Lovly, C. M., Perlmutter, J., Gray, S. W., Hwang, J., et al. (2022) · Journal of Clinical Oncology · doi:10.1200/jco.21.02767 · Cited by 289 · see citing works

Precision oncology in metastatic colorectal cancer — from biology to medicine

Nicolantonio, F. D., Vitiello, P. P., Marsoni, S., Siena, S., Tabernero, J. M., Trusolino, L., Bernards, R., & Bardelli, A. (2021) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-021-00495-z · Cited by 238 · see citing works

Repotrectinib in <i>ROS1</i> Fusion–Positive Non–Small-Cell Lung Cancer

Drilon, A., Camidge, D. R., Lin, J. J., Kim, S.-W., Solomon, B. J., Dziadziuszko, R., Besse, B., Goto, K., de Langen, A. J., Wolf, J., et al. (2024) · New England Journal of Medicine · doi:10.1056/nejmoa2302299 · Cited by 240 · see citing works

Current Landscape of Non-Small Cell Lung Cancer: Epidemiology, Histological Classification, Targeted Therapies, and Immunotherapy

Rodak, O., Peris‐Díaz, M. D., Olbromski, M., Podhorska‐Okołów, M., & Dzięgiel, P. (2021) · Cancers · doi:10.3390/cancers13184705 · Cited by 237 · see citing works

Molecular Markers and Targets in Melanoma

Teixidó, C., Castillo, P., Martínez-Vila, C., Arance, A. M., & Alós, L. (2021) · Cells · doi:10.3390/cells10092320 · Cited by 246 · see citing works

Resistance to TRK inhibition mediated by convergent MAPK pathway activation

Cocco, E., Schram, A. M., Kulick, A. R., Misale, S., Won, H. H., Yaeger, R. D., Razavi, P., Ptashkin, R. N., Hechtman, J. F., Toska, E., et al. (2019) · Nature Medicine · doi:10.1038/s41591-019-0542-z · Cited by 220 · see citing works

Drug resistance to targeted therapeutic strategies in non-small cell lung cancer

Liu, W., Du, Y., Wen, R. M., Yang, M., & Xu, J. (2019) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2019.107438 · Cited by 218 · see citing works

Salivary gland cancer: ESMO–European Reference Network on Rare Adult Solid Cancers (EURACAN) Clinical Practice Guideline for diagnosis, treatment and follow-up

van Herpen, C., Poorten, V. V., Skálová, A., Terhaard, C. H. J., Maroldi, R., van Engen, A., BAUJAT, B., Locati, L. D., Jensen, A., Smeele, L. E., et al. (2022) · ESMO Open · doi:10.1016/j.esmoop.2022.100602 · Cited by 217 · see citing works

Testing algorithm for identification of patients with TRK fusion cancer

Penault-Llorca, F. M., Rudzinski, E. R., & Sepulveda, A. R. (2019) · Journal of Clinical Pathology · doi:10.1136/jclinpath-2018-205679 · Cited by 177 · see citing works

Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies

Li, G., Cheng, Y., Han, C., Song, C., Huang, N., & Du, Y. (2022) · RSC Medicinal Chemistry · doi:10.1039/d2md00206j · Cited by 170 · see citing works

Recurrent Glioblastoma: A Review of the Treatment Options

Salgado, M. Á. V., Villamayor, M. L., Albarrán, V., Alía, V., Sotoca, P., Chamorro, J., Rosero, D. I., Barrill, A. M., Martín, M., Fernández, E., et al. (2023) · Cancers · doi:10.3390/cancers15174279 · Cited by 157 · see citing works

Emerging therapies for non-small cell lung cancer

Zhang, C., Leighl, N. B., Wu, Y.-L. L. C., & Zhong, W. (2019) · Journal of Hematology & Oncology · doi:10.1186/s13045-019-0731-8 · Cited by 153 · see citing works

Diagnosis and management of tropomyosin receptor kinase (TRK) fusion sarcomas: expert recommendations from the World Sarcoma Network

Demetri, G. D., Antonescu, C. R., Bjerkehagen, B., Bovée, J. V. M. G., Boye, K., Chacon, M. R., Tos, A. P. D., Desai, J., Fletcher, J. A., Gelderblom, H. A. J., et al. (2020) · Annals of Oncology · doi:10.1016/j.annonc.2020.08.2232 · Cited by 148 · see citing works

Spectrum of Mechanisms of Resistance to Crizotinib and Lorlatinib in <i>ROS1</i> Fusion–Positive Lung Cancer

Lin, J. J., Choudhury, N. J., Yoda, S., Zhu, V. W., Johnson, T. W., Sakhtemani, R., Dagogo-Jack, I., Digumarthy, S. R., Lee, C., Do, A., et al. (2021) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-0032 · Cited by 145 · see citing works

Oncogenic alterations in advanced NSCLC: a molecular super-highway

Friedlaender, A., Pérol, M., Banna, G. L., Parikh, K., & Addeo, A. (2024) · Biomarker Research · doi:10.1186/s40364-024-00566-0 · Cited by 144 · see citing works

Mechanisms of resistance to targeted therapy and immunotherapy in non-small cell lung cancer: promising strategies to overcoming challenges

Xiang, Y., Liu, X., Wang, Y., Zheng, D., Meng, Q., Jiang, L., Yang, S., Zhang, S., Zhang, X., Liu, Y., et al. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1366260 · Cited by 146 · see citing works

Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK)

Kong, X., Pan, P., Sun, H., Xia, H., Wang, X., Li, Y., & Hou, T. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00446 · Cited by 134 · see citing works

Targeted Therapy for Cancers: From Ongoing Clinical Trials to FDA-Approved Drugs

Choi, H. Y., & Chang, J. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241713618 · Cited by 139 · see citing works

Safety and Efficacy of Crizotinib in Patients With Advanced or Metastatic ROS1-Rearranged Lung Cancer (EUCROSS): A European Phase II Clinical Trial

Michels, S. Y. F., Massutí, B., Schildhaus, H., Franklin, J. G., Sebastian, M., Felip, E., Grohé, C., Rodríguez‐Abreu, D., Abdulla, D. S. Y., Bischoff, H. G., et al. (2019) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2019.03.020 · Cited by 132 · see citing works

Kinase Inhibitors and Kinase-Targeted Cancer Therapies: Recent Advances and Future Perspectives

Li, J.-H., Gong, C., Zhou, H.-T., Liu, J., Xia, X., Ha, W., Jiang, Y.-Z., Liu, Q.-X., & Xiong, H. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25105489 · Cited by 108 · see citing works

NTRK insights: best practices for pathologists

Hechtman, J. F. (2021) · Modern Pathology · doi:10.1038/s41379-021-00913-8 · Cited by 126 · see citing works

Therapeutic advances in non‐small cell lung cancer: Focus on clinical development of targeted therapy and immunotherapy

Cheng, Y., Zhang, T., & Xu, Q. (2021) · MedComm · doi:10.1002/mco2.105 · Cited by 125 · see citing works

The evolution of RET inhibitor resistance in RET-driven lung and thyroid cancers

Rosen, E. Y., Won, H. H., Zheng, Y., Cocco, E., Selçuklu, S. D., Gong, Y., Friedman, N. D., de Bruijn, I., Sümer, S. O., Bielski, C. M., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-28848-x · Cited by 123 · see citing works

Repotrectinib Exhibits Potent Antitumor Activity in Treatment-Naïve and Solvent-Front–Mutant ROS1-Rearranged Non–Small Cell Lung Cancer

Yun, M. R., Kim, D. H., Kim, S., Joo, H.-S., Lee, Y. W., Choi, H. M., Park, C. W., Heo, S. G., Kang, H. N., Lee, S. S., et al. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-19-2777 · Cited by 122 · see citing works

Biomarker-Targeted Therapies in Non–Small Cell Lung Cancer: Current Status and Perspectives

Guo, H., Zhang, J., Qin, C., Yan, H., Liu, T., Hu, H., Tang, S., Tang, S., & Zhou, H. (2022) · Cells · doi:10.3390/cells11203200 · Cited by 118 · see citing works

NTRK Fusions in Central Nervous System Tumors: A Rare, but Worthy Target

Gambella, A., Senetta, R., Collemi, G., Vallero, S. G., Monticelli, M., Cofano, F., Zeppa, P., Garbossa, D., Pellerino, A., Rudà, R., et al. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21030753 · Cited by 118 · see citing works

U.S. Phase I First-in-human Study of Taletrectinib (DS-6051b/AB-106), a ROS1/TRK Inhibitor, in Patients with Advanced Solid Tumors

Papadopoulos, K. P., Borazanci, E., Shaw, A. T., Katayama, R., Shimizu, Y., Zhu, V. W., Sun, T. Y., Wakelee, H. A., Madison, R., Schrock, A. B., et al. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-20-1630 · Cited by 113 · see citing works

Focus on ROS1-Positive Non-Small Cell Lung Cancer (NSCLC): Crizotinib, Resistance Mechanisms and the Newer Generation of Targeted Therapies

D’Angelo, A., Sobhani, N., Chapman, R., Bagby, S., Bortoletti, C., Traversini, M., Ferrari, K., Voltolini, L., Darlow, J., & Roviello, G. (2020) · Cancers · doi:10.3390/cancers12113293 · Cited by 107 · see citing works

Broadening the spectrum of NTRK rearranged mesenchymal tumors and usefulness of pan-TRK immunohistochemistry for identification of NTRK fusions

Brčić, I., Godschachner, T. M., Bergovec, M., Igrec, J., Till, H., Lackner, H., Scheipl, S., Kashofer, K., Brodowicz, T., Leithner, A., et al. (2020) · Modern Pathology · doi:10.1038/s41379-020-00657-x · Cited by 104 · see citing works

FDA approved fluorine-containing drugs in 2023

Wang, Q., Bian, Y., Dhawan, G., Zhang, W., Sorochinsky, A. E., Makarem, A., Soloshonok, V. A., & Han, J. (2024) · Chinese Chemical Letters · doi:10.1016/j.cclet.2024.109780 · Cited by 102 · see citing works

Characterization of on-target adverse events caused by TRK inhibitor therapy

Liu, D., Flory, J., Lin, A. L., Offin, M. D., Falcon, C. J., Murciano‐Goroff, Y. R., Rosen, E. Y., Guo, R., Basu, E. M., Li, B. T., et al. (2020) · Annals of Oncology · doi:10.1016/j.annonc.2020.05.006 · Cited by 101 · see citing works

Tyrosine Kinase Receptors in Oncology

Esteban-Villarrubia, J., Castillo, J. J. S., Pozas, J., Román, M. S., Orejana, I., Torres-Jiménez, J., Carrato, A., Alonso‐Gordoa, T., & Molina‐Cerrillo, J. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21228529 · Cited by 100 · see citing works

Receptor Tyrosine Kinase Signaling and Targeting in Glioblastoma Multiforme

Tilak, M., Holborn, J., New, L. A., Lalonde, J., & Jones, N. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22041831 · Cited by 99 · see citing works

Resistance to Avapritinib in PDGFRA-Driven GIST Is Caused by Secondary Mutations in the PDGFRA Kinase Domain

Grünewald, S., Klug, L. R., Mühlenberg, T., Lategahn, J., Falkenhorst, J., Town, A., Ehrt, C., Wardelmann, E., Hartmann, W., Schildhaus, H., et al. (2020) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-0487 · Cited by 94 · see citing works

NTRK Fusion in Non-Small Cell Lung Cancer: Diagnosis, Therapy, and TRK Inhibitor Resistance

Liu, F., Wei, Y., Zhang, H., Jiang, J., Zhang, P., & Chu, Q. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.864666 · Cited by 95 · see citing works

NTRK Fusions Identified in Pediatric Tumors: The Frequency, Fusion Partners, and Clinical Outcome

Zhao, X., Kotch, C., Fox, E., Surrey, L. F., Wertheim, G. B. W., Baloch, Z. W., Lin, F., Pillai, V., Luo, M., Kreiger, P. A., et al. (2021) · JCO Precision Oncology · doi:10.1200/po.20.00250 · Cited by 88 · see citing works

An overview of kinase downregulators and recent advances in discovery approaches

Wang, B., Wu, H., Hu, C., Wang, H., Liu, J., Wang, W., & Liu, Q. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-021-00826-7 · Cited by 91 · see citing works

Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations

Murray, B. W., Rogers, E., Zhai, D., Deng, W., Chen, X., Sprengeler, P. A., Zhang, X., Graber, A., Reich, S. H., Stopatschinskaja, S., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0632 · Cited by 89 · see citing works

EML4‑ALK fusion gene in non‑small cell lung cancer (Review)

Lei, Y., Yan, L., Shi, X., & Wang, J. (2022) · Oncology Letters · doi:10.3892/ol.2022.13397 · Cited by 86 · see citing works

Clinicopathologic Features and Response to Therapy of NRG1 Fusion–Driven Lung Cancers: The eNRGy1 Global Multicenter Registry

Drilon, A. E. D. C., Duruisseaux, M., Han, J., Ito, M., Falcon, C. J., Yang, S., Murciano‐Goroff, Y. R., Chen, H., Okada, M., Molina‐Vila, M. Á., et al. (2021) · Journal of Clinical Oncology · doi:10.1200/jco.20.03307 · Cited by 86 · see citing works

Evidence of NTRK1 Fusion as Resistance Mechanism to EGFR TKI in EGFR+ NSCLC: Results From a Large-Scale Survey of NTRK1 Fusions in Chinese Patients With Lung Cancer

Xia, H., Xue, X., Ding, H., Ou, Q., Wu, X., Nagasaka, M., Shao, Y. W., Hu, X., & Ou, S. I. (2019) · Clinical Lung Cancer · doi:10.1016/j.cllc.2019.09.004 · Cited by 82 · see citing works

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors

Cocco, E., Lee, J. E., Kannan, S., Schram, A. M., Won, H. H., Shifman, S. G., Kulick, A. R., Baldino, L., Toska, E., Arruabarrena-Aristorena, A., et al. (2019) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-0571 · Cited by 81 · see citing works

Larotrectinib, a highly selective tropomyosin receptor kinase (TRK) inhibitor for the treatment of TRK fusion cancer

Federman, N. C., & McDermott, R. (2019) · Expert Review of Clinical Pharmacology · doi:10.1080/17512433.2019.1661775 · Cited by 80 · see citing works

Entrectinib, a new multi-target inhibitor for cancer therapy

Jiang, Q., Li, M., Li, H., & Chen, L. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.112974 · Cited by 80 · see citing works

Current treatment and future challenges in ROS1- and ALK-rearranged advanced non-small cell lung cancer

Remón, J., Pignataro, D., Novello, S., & Passiglia, F. (2021) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2021.102178 · Cited by 76 · see citing works

Challenges in the Use of Targeted Therapies in Non–Small Cell Lung Cancer

Rivera‐Concepción, J., Uprety, D., & Adjei, A. A. (2022) · Cancer Research and Treatment · doi:10.4143/crt.2022.078 · Cited by 80 · see citing works

SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy

Drilon, A. E. D. C., Sharma, M. R., Johnson, M. L., Yap, T. A., Gadgeel, S. M., Nepert, D. L., Feng, G., Reddy, M. B., Harney, A. S., Elsayed, M., et al. (2023) · Cancer Discovery · doi:10.1158/2159-8290.cd-23-0361 · Cited by 75 · see citing works

Tropomyosin Receptor Kinase Inhibitors for the Treatment of TRK Fusion Cancer

Laetsch, T. W., & Hong, D. S. (2021) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-0465 · Cited by 72 · see citing works

Molecular diagnosis and targeted treatment of advanced follicular cell-derived thyroid cancer in the precision medicine era

Capdevila, J., Awada, A. H., Führer‐Sakel, D., Leboulleux, S., & Pauwels, P. (2022) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2022.102380 · Cited by 70 · see citing works

FYN: emerging biological roles and potential therapeutic targets in cancer

Peng, S., & Fu, Y. (2023) · Journal of Translational Medicine · doi:10.1186/s12967-023-03930-0 · Cited by 70 · see citing works

Advances and challenges in precision medicine in salivary gland cancer

Lassche, G., van Boxtel, W., Ligtenberg, M. J. L., Grunsven, A. C. H. V. E., & van Herpen, C. M. L. (2019) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2019.101906 · Cited by 68 · see citing works

Targeting ALK Rearrangements in NSCLC: Current State of the Art

Peng, L., Zhu, L., Sun, Y., Stebbing, J., Selvaggi, G., Zhang, Y., & Yu, Z. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.863461 · Cited by 71 · see citing works

Targeting Gatekeeper Mutations for Kinase Drug Discovery

Zhou, Y., Xiang, S., Yang, F., & Lu, X. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01361 · Cited by 68 · see citing works

<scp><i>NTRK</i></scp> fusion positive colorectal cancer is a unique subset of <scp>CRC</scp> with high <scp>TMB</scp> and microsatellite instability

Wang, H., Li, Z., Ou, Q., Wu, X., Nagasaka, M., Shao, Y., Ou, S. I., & Yang, Y. (2022) · Cancer Medicine · doi:10.1002/cam4.4561 · Cited by 64 · see citing works

Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations

Lu, X., Smaill, J. B., & Ding, K. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00507 · Cited by 67 · see citing works

NTRK kinase domain mutations in cancer variably impact sensitivity to type I and type II inhibitors

Somwar, R., Hofmann, N. E., Smith, B. D., Odintsov, I., Vojnic, M., Linkov, I., Tam, A., Khodos, I., Mattar, M. S., de Stanchina, E., et al. (2020) · Communications Biology · doi:10.1038/s42003-020-01508-w · Cited by 65 · see citing works

NTRK Fusion-positive Non–small-cell Lung Cancer: The Diagnosis and Targeted Therapy

Haratake, N., & Seto, T. (2020) · Clinical Lung Cancer · doi:10.1016/j.cllc.2020.10.013 · Cited by 64 · see citing works

Taletrectinib in <i>ROS1</i> + Non–Small Cell Lung Cancer: TRUST

Pérol, M., Li, W., Pennell, N. A., Liu, G., Ohe, Y., De Braud, F., Nagasaka, M., Felip, E., Xiong, A., Zhang, Y., et al. (2025) · Journal of Clinical Oncology · doi:10.1200/jco-25-00275 · Cited by 63 · see citing works

Targeting YAP to overcome acquired resistance to ALK inhibitors in ALK‐rearranged lung cancer

Yun, M. R., Choi, H. M., Lee, Y. W., Joo, H. S., Park, C. W., Choi, J. W., Kim, D. H., Kang, H. N., Pyo, K., Shin, E. J., et al. (2019) · EMBO Molecular Medicine · doi:10.15252/emmm.201910581 · Cited by 63 · see citing works

NTRK fusions in lung cancer: From biology to therapy

Harada, G., Santini, F. C., Wilhelm, C., & Drilon, A. E. D. C. (2021) · Lung Cancer · doi:10.1016/j.lungcan.2021.09.005 · Cited by 62 · see citing works

PGR Gene Fusions Identify a Molecular Subset of Uterine Epithelioid Leiomyosarcoma With Rhabdoid Features

Chiang, S., Samore, W. R., Zhang, L., Sung, Y., Turashvili, G., Murali, R., Soslow, R. A., Hensley, M. L., Swanson, D. M., Dickson, B. C., et al. (2019) · The American Journal of Surgical Pathology · doi:10.1097/pas.0000000000001239 · Cited by 59 · see citing works

Resistance mechanisms and potent-targeted therapies of ROS1-positive lung cancer

Roys, A., Chang, X., Liu, Y., Xu, X., Wu, Y., & Zuo, D. (2019) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-019-03902-6 · Cited by 57 · see citing works

Translocation-Related Sarcomas

Nakano, K., & Takahashi, S. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19123784 · Cited by 57 · see citing works

Molecular pathways, resistance mechanisms and targeted interventions in non-small-cell lung cancer

Wang, Z., Xing, Y., Li, B., Li, X., Liu, B., & Wang, Y. (2022) · Molecular Biomedicine · doi:10.1186/s43556-022-00107-x · Cited by 59 · see citing works

CNS metastasis in ROS1+ NSCLC: An urgent call to action, to understand, and to overcome

Ou, S. I., & Zhu, V. W. (2019) · Lung Cancer · doi:10.1016/j.lungcan.2019.02.025 · Cited by 55 · see citing works

Targeting non-small cell lung cancer: driver mutation beyond epidermal growth factor mutation and anaplastic lymphoma kinase fusion

Chu, Q. S.-C. (2020) · Therapeutic Advances in Medical Oncology · doi:10.1177/1758835919895756 · Cited by 55 · see citing works

NTRK Fusions in Sarcomas: Diagnostic Challenges and Clinical Aspects

Siozopoulou, V., Smits, E., Winne, K. D., Marcq, E., & Pauwels, P. (2021) · Diagnostics · doi:10.3390/diagnostics11030478 · Cited by 54 · see citing works

Targeting ROS1 Rearrangements in Non-small Cell Lung Cancer: Crizotinib and Newer Generation Tyrosine Kinase Inhibitors

Morris, T. A., Khoo, C., & Solomon, B. (2019) · Drugs · doi:10.1007/s40265-019-01164-3 · Cited by 53 · see citing works

Targeting the NTRK Fusion Gene in Pancreatic Acinar Cell Carcinoma: A Case Report and Review of the Literature

Gupta, M., Sherrow, C., Krone, M. E., Blais, E. M., Pishvaian, M. J., Petricoin, E. F., Matrisian, L. M., DeArbeloa, P., Gregory, G., Brown, A., et al. (2021) · Journal of the National Comprehensive Cancer Network · doi:10.6004/jnccn.2020.7641 · Cited by 53 · see citing works

Preclinical Study of a Biparatopic METxMET Antibody–Drug Conjugate, REGN5093-M114, Overcomes MET-driven Acquired Resistance to EGFR TKIs in EGFR-mutant NSCLC

Oh, S. Y., Lee, Y. W., Lee, E. J., Kim, J. H., Park, Y., Heo, S. G., Yu, M. R., Hong, M. H., DaSilva, J. O., Daly, C., et al. (2022) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-22-2180 · Cited by 51 · see citing works

Entrectinib for the treatment of metastatic NSCLC: safety and efficacy

Bianchi, A. S., Pizzutilo, E. G., Marrapese, G., Tosi, F., Cerea, G., & Siena, S. (2020) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2020.1747439 · Cited by 52 · see citing works

Clinical Relevance of an Amplicon-Based Liquid Biopsy for DetectingALKandROS1Fusion and Resistance Mutations in Patients With Non–Small-Cell Lung Cancer

Mezquita, L., Swalduz, A., Jovelet, C., Ortiz‐Cuaran, S., Howarth, K., Planchard, D., Avrillon, V., Recondo, G., Marteau, S., Benítez, J. C., et al. (2020) · JCO Precision Oncology · doi:10.1200/po.19.00281 · Cited by 51 · see citing works

The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib

Shen, T., Hu, X., Liu, X., Subbiah, V., Mooers, B. H. M., & Wu, J. (2021) · npj Precision Oncology · doi:10.1038/s41698-021-00188-x · Cited by 52 · see citing works

NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations

Drilon, A., Horan, J. C., Tangpeerachaikul, A., Besse, B., Ou, S.-H. I., Gadgeel, S. M., Camidge, D. R., van der Wekken, A. J., Nguyen-Phuong, L., Acker, A., et al. (2023) · Cancer Discovery · doi:10.1158/2159-8290.cd-22-0968 · Cited by 52 · see citing works

Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer

Liu, Z., Yu, P., Dong, L., Wang, W., Duan, S., Wang, B., Gong, X., Liang, Y. S., Wang, H., & Tian, J. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00712 · Cited by 50 · see citing works

Utility of the Ba/F3 cell system for exploring on‐target mechanisms of resistance to targeted therapies for lung cancer

Koga, T., Suda, K., & Mitsudomi, T. (2022) · Cancer Science · doi:10.1111/cas.15263 · Cited by 50 · see citing works

Chasing the Target: New Phenomena of Resistance to Novel Selective RET Inhibitors in Lung Cancer. Updated Evidence and Future Perspectives

Fancelli, S., Caliman, E., Mazzoni, F., Brugia, M., Castiglione, F., Voltolini, L., Pillozzi, S., & Antonuzzo, L. (2021) · Cancers · doi:10.3390/cancers13051091 · Cited by 50 · see citing works

ROS1 Targeted Therapies: Current Status

Azelby, C. M., Sakamoto, M., & Bowles, D. W. (2021) · Current Oncology Reports · doi:10.1007/s11912-021-01078-y · Cited by 50 · see citing works

TRK inhibitor activity and resistance in TRK fusion-positive cancers in adults

Harada, G., & Drilon, A. E. D. C. (2022) · Cancer Genetics · doi:10.1016/j.cancergen.2022.03.002 · Cited by 49 · see citing works

Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance

Wang, Z., Wang, J., Wang, Y., Xiang, S., Song, X., Tu, Z., Zhou, Y., Zhang, Z., Zhang, Z., Ding, K., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00308 · Cited by 49 · see citing works

Macrocycles and macrocyclization in anticancer drug discovery: Important pieces of the puzzle

Zhang, C., Liu, F., Zhang, Y., & Song, C. X. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116234 · Cited by 49 · see citing works

In This Issue

(2018) · Cancer Discovery · doi:10.1158/2159-8290.cd-iti8-10

Abstract 4796: Ropotrectinib is a novel polypharmacology kinase inhibitor against WT and mutant ROS1, TRK and ALK

Deng, W., Zhai, D., Huang, J., Rogers, E., Whitten, J., Lim, J. K. C., Li, Y., & Cui, J. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-4796

MA 07.09 ALK/ROS1/TRK Inhibitor TPX-0005 Effectively Overcomes Clinical Resistance Solvent Front Mutations

Cui, J. J., Zhai, D., Deng, W., Rogers, E., Ung, J., Zhang, X., Zhang, H., Huang, Z. R., Whitten, J., Lim, J. T., et al. (2017) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2017.09.510

Abstract 3168: Overcoming acquired drug resistance by TPX-0005, an ALK, ROS1 and pan-TRK inhibitor

Deng, W., Huang, J., Zhai, D., Rogers, E., & Cui, J. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-3168 · Cited by 1 · see citing works

OA09 Preliminary Clinical Activity of Repotrectinib (TPX-0005) in Advanced ROS1 Fusion-Positive Non-Small Cell Lung Cancer

Ou, S. ‐. I., Cho, B. C., Kim, D. S., Drilon, A. E. D. C., Lee, J., Lin, J. J., Zhu, V. W., Ahn, M., Camidge, D. R., Stopatschinskaja, S., et al. (2018) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2018.10.019 · Cited by 6 · see citing works