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Journal Articles

NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations

Jessica J. Lin, Joshua C. Horan, Anupong Tangpeerachaikul, Aurélie Swalduz, Augusto Valdivia, Melissa L. Johnson, Benjamin Besse, D. Ross Camidge, Toshio Fujino, Satoshi Yoda, Linh Nguyen-Phuong, Hayato Mizuta, Ludovic Bigot, Catline Nobre, Jii Bum Lee, Mi Ra Yu, Scot Mente, Yuting Sun, Nancy E. Kohl, James R. Porter, Matthew D. Shair, Viola W. Zhu, Enriqueta Felip, Byoung Chul Cho, Luc Friboulet, Aaron N. Hata, Henry E. Pelish, Alexander Drilon
Journal: Cancer Discovery
Cancer Discov (2024) 14 (12): 2367–2386.
https://doi.org/10.1158/2159-8290.CD-24-0231
Published: 02 December 2024
View article titled, NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
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Includes: Supplementary data
Journal Articles

Precision Oncology: 2024 in Review

Matteo Repetto, Nicole Fernandez, Alexander Drilon, Debyani Chakravarty
Journal: Cancer Discovery
Cancer Discov (2024) 14 (12): 2332–2345.
https://doi.org/10.1158/2159-8290.CD-24-1476
Published: 02 December 2024
View article titled, Precision Oncology: 2024 in Review
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Journal Articles

Activating Point Mutations in the MET Kinase Domain Represent a Unique Molecular Subset of Lung Cancer and Other Malignancies Targetable with MET Inhibitors

Federica Pecci, Seshiru Nakazawa, Biagio Ricciuti, Guilherme Harada, Jessica K. Lee, Joao V. Alessi, Adriana Barrichello, Victor R. Vaz, Giuseppe Lamberti, Alessandro Di Federico, Malini M. Gandhi, Dimitris Gazgalis, William W. Feng, Jie Jiang, Simon Baldacci, Marie-Anaïs Locquet, Felix H. Gottlieb, Monica F. Chen, Elinton Lee, Danielle Haradon, Anna Smokovich, Emma Voligny, Tom Nguyen, Vikas K. Goel, Zachary Zimmerman, Sumandeep Atwal, Xinan Wang, Magda Bahcall, Rebecca S. Heist, Sumaiya Iqbal, Nishant Gandhi, Andrew Elliott, Ari M. Vanderwalde, Patrick C. Ma, Balazs Halmos, Stephen V. Liu, Jianwei Che, Alexa B. Schrock, Alexander Drilon, Pasi A. Jänne, Mark M. Awad
Journal: Cancer Discovery
Cancer Discov (2024) 14 (8): 1440–1456.
https://doi.org/10.1158/2159-8290.CD-23-1217
Published: 02 August 2024
View article titled, Activating Point Mutations in the <em>MET</em> Kinase Domain Represent a Unique Molecular Subset of Lung Cancer and Other Malignancies Targetable with MET Inhibitors
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Includes: Supplementary data
Journal Articles

Optimus-Era Dose Finding for Rare Cancers

Yonina R. Murciano-Goroff, Sean M. Devlin, Alexia Iasonos, Alexander Drilon
Journal: Cancer Discovery
Cancer Discov (2024) 14 (6): 909–914.
https://doi.org/10.1158/2159-8290.CD-24-0368
Published: 03 June 2024
View article titled, Optimus-Era Dose Finding for Rare Cancers
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Journal Articles

Quantifying the Expanding Landscape of Clinical Actionability for Patients with Cancer

Sarah P. Suehnholz, Moriah H. Nissan, Hongxin Zhang, Ritika Kundra, Subhiksha Nandakumar, Calvin Lu, Stephanie Carrero, Amanda Dhaneshwar, Nicole Fernandez, Benjamin W. Xu, Maria E. Arcila, Ahmet Zehir, Aijazuddin Syed, A. Rose Brannon, Julia E. Rudolph, Eder Paraiso, Paul J. Sabbatini, Ross L. Levine, Ahmet Dogan, Jianjiong Gao, Marc Ladanyi, Alexander Drilon, Michael F. Berger, David B. Solit, Nikolaus Schultz, Debyani Chakravarty
Journal: Cancer Discovery
Cancer Discov (2024) 14 (1): 49–65.
https://doi.org/10.1158/2159-8290.CD-23-0467
Published: 12 January 2024
View article titled, Quantifying the Expanding Landscape of Clinical Actionability for Patients with Cancer
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Includes: Supplementary data
Journal Articles

Precision Oncology: 2023 in Review

Yonina R. Murciano-Goroff, Sarah P. Suehnholz, Alexander Drilon, Debyani Chakravarty
Journal: Cancer Discovery
Cancer Discov (2023) 13 (12): 2525–2531.
https://doi.org/10.1158/2159-8290.CD-23-1194
Published: 12 December 2023
View article titled, Precision Oncology: 2023 in Review
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Journal Articles

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

Alexander Drilon, Manish R. Sharma, Melissa L. Johnson, Timothy A. Yap, Shirish Gadgeel, Dale Nepert, Gang Feng, Micaela B. Reddy, Allison S. Harney, Mohamed Elsayed, Adam W. Cook, Christina E. Wong, Ronald J. Hinklin, Yutong Jiang, Eric N. Brown, Nickolas A. Neitzel, Ellen R. Laird, Wen-I Wu, Anurag Singh, Ping Wei, Keith A. Ching, John J. Gaudino, Patrice A. Lee, Dylan P. Hartley, S. Michael Rothenberg
Journal: Cancer Discovery
Cancer Discov (2023) 13 (8): 1789–1801.
https://doi.org/10.1158/2159-8290.CD-23-0361
Published: 04 August 2023
View article titled, SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy
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Includes: Supplementary data
Journal Articles

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

Alexander Drilon, Joshua C. Horan, Anupong Tangpeerachaikul, Benjamin Besse, Sai-Hong Ignatius Ou, Shirish M. Gadgeel, D. Ross Camidge, Anthonie J. van der Wekken, Linh Nguyen-Phuong, Adam Acker, Clare Keddy, Katelyn S. Nicholson, Satoshi Yoda, Scot Mente, Yuting Sun, John R. Soglia, Nancy E. Kohl, James R. Porter, Matthew D. Shair, Viola Zhu, Monika A. Davare, Aaron N. Hata, Henry E. Pelish, Jessica J. Lin
Journal: Cancer Discovery
Cancer Discov (2023) 13 (3): 598–615.
https://doi.org/10.1158/2159-8290.CD-22-0968
Published: 01 March 2023
View article titled, NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
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Includes: Supplementary data
Journal Articles

Precision Oncology: 2022 in Review

Ezra Rosen, Alexander Drilon, Debyani Chakravarty
Journal: Cancer Discovery
Cancer Discov (2022) 12 (12): 2747–2753.
https://doi.org/10.1158/2159-8290.CD-22-1154
Published: 02 December 2022
View article titled, Precision Oncology: 2022 in Review
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Journal Articles

Zenocutuzumab, a HER2xHER3 Bispecific Antibody, Is Effective Therapy for Tumors Driven by NRG1 Gene Rearrangements

Alison M. Schram, Igor Odintsov, Madelyn Espinosa-Cotton, Inna Khodos, Whitney J. Sisso, Marissa S. Mattar, Allan J.W. Lui, Morana Vojnic, Sara H. Shameem, Thrusha Chauhan, Jean Torrisi, Jim Ford, Marie N. O'Connor, Cecile A.W. Geuijen, Ron C.J. Schackmann, Jeroen J. Lammerts van Bueren, Ernesto Wasserman, Elisa de Stanchina, Eileen M. O'Reilly, Marc Ladanyi, Alexander Drilon, Romel Somwar
Journal: Cancer Discovery
Cancer Discov (2022) 12 (5): 1233–1247.
https://doi.org/10.1158/2159-8290.CD-21-1119
Published: 02 May 2022
View article titled, Zenocutuzumab, a HER2xHER3 Bispecific Antibody, Is Effective Therapy for Tumors Driven by <em>NRG1</em> Gene Rearrangements
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Includes: Supplementary data
Journal Articles

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

Emiliano Cocco, Ji Eun Lee, Srinivasaraghavan Kannan, Alison M. Schram, Helen H. Won, Sophie Shifman, Amanda Kulick, Laura Baldino, Eneda Toska, Amaia Arruabarrena-Aristorena, Srushti Kittane, Fan Wu, Yanyan Cai, Sabrina Arena, Benedetta Mussolin, Ram Kannan, Neil Vasan, Alexander N. Gorelick, Michael F. Berger, Ofra Novoplansky, Sankar Jagadeeshan, Yi Liao, Uwe Rix, Sandra Misale, Barry S. Taylor, Alberto Bardelli, Jaclyn F. Hechtman, David M. Hyman, Moshe Elkabets, Elisa de Stanchina, Chandra S. Verma, Andrea Ventura, Alexander Drilon, Maurizio Scaltriti
Journal: Cancer Discovery
Cancer Discov (2021) 11 (1): 126–141.
https://doi.org/10.1158/2159-8290.CD-20-0571
Published: 06 January 2021
View article titled, TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors
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Includes: Supplementary data
Journal Articles

A Phase I/Ib Trial of the VEGFR-Sparing Multikinase RET Inhibitor RXDX-105

Alexander Drilon, Siqing Fu, Manish R. Patel, Marwan Fakih, Ding Wang, Anthony J. Olszanski, Daniel Morgensztern, Stephen V. Liu, Byoung Chul Cho, Lyudmila Bazhenova, Cristina P. Rodriguez, Robert C. Doebele, Antoinette Wozniak, Karen L. Reckamp, Tara Seery, Petros Nikolinakos, Zheyi Hu, Jennifer W. Oliver, Denise Trone, Katherine McArthur, Rupal Patel, Pratik S. Multani, Myung-Ju Ahn
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2019) 9 (3): 384–395.
https://doi.org/10.1158/2159-8290.CD-18-0839
Published: 01 March 2019
View article titled, A Phase I/Ib Trial of the VEGFR-Sparing Multikinase RET Inhibitor RXDX-105
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Includes: Supplementary data
Journal Articles

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

Alexander Drilon, Sai-Hong Ignatius Ou, Byoung Chul Cho, Dong-Wan Kim, Jeeyun Lee, Jessica J. Lin, Viola W. Zhu, Myung-Ju Ahn, D. Ross Camidge, Judy Nguyen, Dayong Zhai, Wei Deng, Zhongdong Huang, Evan Rogers, Juliet Liu, Jeff Whitten, John K. Lim, Shanna Stopatschinskaja, David M. Hyman, Robert C. Doebele, J. Jean Cui, Alice T. Shaw
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2018) 8 (10): 1227–1236.
https://doi.org/10.1158/2159-8290.CD-18-0484
Published: 02 October 2018
View article titled, Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations
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Includes: Supplementary data
Journal Articles

Response to ERBB3-Directed Targeted Therapy in NRG1-Rearranged Cancers

Alexander Drilon, Romel Somwar, Biju P. Mangatt, Henrik Edgren, Patrice Desmeules, Anja Ruusulehto, Roger S. Smith, Lukas Delasos, Morana Vojnic, Andrew J. Plodkowski, Joshua Sabari, Kenneth Ng, Joseph Montecalvo, Jason Chang, Huichun Tai, William W. Lockwood, Victor Martinez, Gregory J. Riely, Charles M. Rudin, Mark G. Kris, Maria E. Arcila, Christopher Matheny, Ryma Benayed, Natasha Rekhtman, Marc Ladanyi, Gopinath Ganji
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2018) 8 (6): 686–695.
https://doi.org/10.1158/2159-8290.CD-17-1004
Published: 31 May 2018
View article titled, Response to ERBB3-Directed Targeted Therapy in <em>NRG1</em>-Rearranged Cancers
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Includes: Supplementary data
Journal Articles

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

Alexander Drilon, Ramamoorthy Nagasubramanian, James F. Blake, Nora Ku, Brian B. Tuch, Kevin Ebata, Steve Smith, Veronique Lauriault, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Paul D. Larsen, Karyn S. Bouhana, Shannon L. Winski, Robyn Hamor, Wen-I Wu, Andrew Parker, Tony H. Morales, Francis X. Sullivan, Walter E. DeWolf, Lance A. Wollenberg, Paul R. Gordon, Dorothea N. Douglas-Lindsay, Maurizio Scaltriti, Ryma Benayed, Sandeep Raj, Bethany Hanusch, Alison M. Schram, Philip Jonsson, Michael F. Berger, Jaclyn F. Hechtman, Barry S. Taylor, Steve Andrews, S. Michael Rothenberg, David M. Hyman
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2017) 7 (9): 963–972.
https://doi.org/10.1158/2159-8290.CD-17-0507
Published: 31 August 2017
View article titled, A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion–Positive Solid Tumors
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Includes: Supplementary data
Journal Articles

Prospective Comprehensive Molecular Characterization of Lung Adenocarcinomas for Efficient Patient Matching to Approved and Emerging Therapies

Emmet J. Jordan, Hyunjae R. Kim, Maria E. Arcila, David Barron, Debyani Chakravarty, JianJiong Gao, Matthew T. Chang, Andy Ni, Ritika Kundra, Philip Jonsson, Gowtham Jayakumaran, Sizhi Paul Gao, Hannah C. Johnsen, Aphrothiti J. Hanrahan, Ahmet Zehir, Natasha Rekhtman, Michelle S. Ginsberg, Bob T. Li, Helena A. Yu, Paul K. Paik, Alexander Drilon, Matthew D. Hellmann, Dalicia N. Reales, Ryma Benayed, Valerie W. Rusch, Mark G. Kris, Jamie E. Chaft, José Baselga, Barry S. Taylor, Nikolaus Schultz, Charles M. Rudin, David M. Hyman, Michael F. Berger, David B. Solit, Marc Ladanyi, Gregory J. Riely
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2017) 7 (6): 596–609.
https://doi.org/10.1158/2159-8290.CD-16-1337
Published: 01 June 2017
View article titled, Prospective Comprehensive Molecular Characterization of Lung Adenocarcinomas for Efficient Patient Matching to Approved and Emerging Therapies
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Includes: Supplementary data
Journal Articles

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)

Alexander Drilon, Salvatore Siena, Sai-Hong Ignatius Ou, Manish Patel, Myung Ju Ahn, Jeeyun Lee, Todd M. Bauer, Anna F. Farago, Jennifer J. Wheler, Stephen V. Liu, Robert Doebele, Laura Giannetta, Giulio Cerea, Giovanna Marrapese, Michele Schirru, Alessio Amatu, Katia Bencardino, Laura Palmeri, Andrea Sartore-Bianchi, Angelo Vanzulli, Sara Cresta, Silvia Damian, Matteo Duca, Elena Ardini, Gang Li, Jason Christiansen, Karey Kowalski, Ann D. Johnson, Rupal Patel, David Luo, Edna Chow-Maneval, Zachary Hornby, Pratik S. Multani, Alice T. Shaw, Filippo G. De Braud
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2017) 7 (4): 400–409.
https://doi.org/10.1158/2159-8290.CD-16-1237
Published: 02 April 2017
View article titled, 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)
Open the PDF for 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) in another window
Includes: Supplementary data
Journal Articles

Response to MET Inhibitors in Patients with Stage IV Lung Adenocarcinomas Harboring MET Mutations Causing Exon 14 Skipping

Paul K. Paik, Alexander Drilon, Pang-Dian Fan, Helena Yu, Natasha Rekhtman, Michelle S. Ginsberg, Laetitia Borsu, Nikolaus Schultz, Michael F. Berger, Charles M. Rudin, Marc Ladanyi
Journal: Cancer Discovery
Series: Author Choice
Cancer Discov (2015) 5 (8): 842–849.
https://doi.org/10.1158/2159-8290.CD-14-1467
Published: 03 August 2015
View article titled, Response to MET Inhibitors in Patients with Stage IV Lung Adenocarcinomas Harboring <em>MET</em> Mutations Causing Exon 14 Skipping
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Includes: Supplementary data
Journal Articles

Response to Cabozantinib in Patients with RET Fusion-Positive Lung Adenocarcinomas

Alexander Drilon, Lu Wang, Adnan Hasanovic, Yoshiyuki Suehara, Doron Lipson, Phil Stephens, Jeffrey Ross, Vincent Miller, Michelle Ginsberg, Maureen F. Zakowski, Mark G. Kris, Marc Ladanyi, Naiyer Rizvi
Journal: Cancer Discovery
Cancer Discov (2013) 3 (6): 630–635.
https://doi.org/10.1158/2159-8290.CD-13-0035
Published: 06 June 2013
View article titled, Response to Cabozantinib in Patients with <em>RET</em> Fusion-Positive Lung Adenocarcinomas
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