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Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

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La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, California 92121, United States
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*E-mail: [email protected]. Phone: (858) 526-4290.
Cite this: J. Med. Chem. 2014, 57, 11, 4720–4744
Publication Date (Web):May 13, 2014
https://doi.org/10.1021/jm500261q
Copyright © 2014 American Chemical Society
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    Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-positive non-small-cell lung carcinoma patients, progression during treatment eventually develops. Resistant patient samples revealed a variety of point mutations in the kinase domain of ALK, including the L1196M gatekeeper mutation. In addition, some patients progress due to cancer metastasis in the brain. Using structure-based drug design, lipophilic efficiency, and physical-property-based optimization, highly potent macrocyclic ALK inhibitors were prepared with good absorption, distribution, metabolism, and excretion (ADME), low propensity for p-glycoprotein 1-mediated efflux, and good passive permeability. These structurally unusual macrocyclic inhibitors were potent against wild-type ALK and clinically reported ALK kinase domain mutations. Significant synthetic challenges were overcome, utilizing novel transformations to enable the use of these macrocycles in drug discovery paradigms. This work led to the discovery of 8k (PF-06463922), combining broad-spectrum potency, central nervous system ADME, and a high degree of kinase selectivity.

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    X-ray data and 207-member panel kinase selectivity data for compound 8k and experimental data for compounds 6e, 6f, 6h, 9, 10, 17, 20, 21, 30, 31, 44, 45, 49–51, 55, 57, 59, 60, and 69–75 not explicitly shown in the schemes. This material is available free of charge via the Internet at http://pubs.acs.org.

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    56. Xinsheng Xiao, Ying Xie, Siyi Bai, Yuanfu Deng, Huanfeng Jiang, and Wei Zeng . Transition-Metal-Free Tandem Chlorocyclization of Amines with Carboxylic Acids: Access to Chloroimidazo[1,2-α]pyridines. Organic Letters 2015, 17 (16) , 3998-4001. https://doi.org/10.1021/acs.orglett.5b01868
    57. Zoran Rankovic . CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure. Journal of Medicinal Chemistry 2015, 58 (6) , 2584-2608. https://doi.org/10.1021/jm501535r
    58. Christopher R. Butler, Michael A. Brodney, Elizabeth M. Beck, Gabriela Barreiro, Charles E. Nolan, Feng Pan, Felix Vajdos, Kevin Parris, Alison H. Varghese, Christopher J. Helal, Ricardo Lira, Shawn D. Doran, David R. Riddell, Leanne M. Buzon, Jason K. Dutra, Luis A. Martinez-Alsina, Kevin Ogilvie, John C. Murray, Joseph M. Young, Kevin Atchison, Ashley Robshaw, Cathleen Gonzales, Jinlong Wang, Yong Zhang, and Brian T. O’Neill . Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design. Journal of Medicinal Chemistry 2015, 58 (6) , 2678-2702. https://doi.org/10.1021/jm501833t
    59. Siming Liu, Chuan Huang, Chunhui Huang, Yaqi Huang, Yonghuan Yu, Guowu Wu, Fengqiu Guo, Ying Jiang, Shanhe Wan, Zhengguang Zhu, Yuanxin Tian, Jianghua Zhu, Jiajie Zhang. Discovery of novel 2-aminopyridine derivatives as ROS1 and ALK dual inhibitors to combat drug-resistant mutants including ROS1 G2032R and ALK G1202R. Journal of Enzyme Inhibition and Medicinal Chemistry 2023, 38 (1) https://doi.org/10.1080/14756366.2023.2227779
    60. Esther R. Berko, Gabriela M. Witek, Smita Matkar, Zaritza O. Petrova, Megan A. Wu, Courtney M. Smith, Alex Daniels, Joshua Kalna, Annie Kennedy, Ivan Gostuski, Colleen Casey, Kateryna Krytska, Mark Gerelus, Dean Pavlick, Susan Ghazarian, Julie R. Park, Araz Marachelian, John M. Maris, Kelly C. Goldsmith, Ravi Radhakrishnan, Mark A. Lemmon, Yaël P. Mossé. Circulating tumor DNA reveals mechanisms of lorlatinib resistance in patients with relapsed/refractory ALK-driven neuroblastoma. Nature Communications 2023, 14 (1) https://doi.org/10.1038/s41467-023-38195-0
    61. Yanyan Diao, Dandan Liu, Huan Ge, Rongrong Zhang, Kexin Jiang, Runhui Bao, Xiaoqian Zhu, Hongjie Bi, Wenjie Liao, Ziqi Chen, Kai Zhang, Rui Wang, Lili Zhu, Zhenjiang Zhao, Qiaoyu Hu, Honglin Li. Macrocyclization of linear molecules by deep learning to facilitate macrocyclic drug candidates discovery. Nature Communications 2023, 14 (1) https://doi.org/10.1038/s41467-023-40219-8
    62. Hua Gao, Jing-Yi Zhang, Li-Jie Zhao, Yuan-Yuan Guo. Synthesis and clinical application of small-molecule inhibitors and PROTACs of anaplastic lymphoma kinase. Bioorganic Chemistry 2023, 140 , 106807. https://doi.org/10.1016/j.bioorg.2023.106807
    63. . ALK/multikinase Inhibitors. 2023, 195-213. https://doi.org/10.1002/9781394207145.ch9
    64. Geoffrey Liu, Vincent K. Lam. Podcast on Lorlatinib as a First-Line Treatment Option for Patients with ALK-Positive Metastatic NSCLC with Brain Metastasis. Advances in Therapy 2023, 40 (10) , 4117-4126. https://doi.org/10.1007/s12325-023-02606-x
    65. Yuyao Luo, Zhe Zhang, XuanZhu Guo, Xuemei Tang, Sijie Li, Guotao Gong, Shun Gao, Yan Zhang, Sheng Lin. Comparative safety of anaplastic lymphoma kinase tyrosine kinase inhibitors in advanced anaplastic lymphoma kinase-mutated non-small cell lung cancer: Systematic review and network meta-analysis. Lung Cancer 2023, 184 , 107319. https://doi.org/10.1016/j.lungcan.2023.107319
    66. V. Pratap Reddy Gajulapalli. Development of Kinase‐Centric Drugs: A Computational Perspective. ChemMedChem 2023, 198 https://doi.org/10.1002/cmdc.202200693
    67. Yingxue Li, Yanna Lv, Cheng Zhang, Binyu Fu, Yue Liu, Jinxing Hu. Recent advances in the development of dual ALK/ROS1 inhibitors for non-small cell lung cancer therapy. European Journal of Medicinal Chemistry 2023, 257 , 115477. https://doi.org/10.1016/j.ejmech.2023.115477
    68. Isao Miyazaki, Igor Odintsov, Keiji Ishida, Allan J. W. Lui, Masanori Kato, Tatsuya Suzuki, Tom Zhang, Kentaro Wakayama, Renate I. Kurth, Ryan Cheng, Hidenori Fujita, Lukas Delasos, Morana Vojnic, Inna Khodos, Yukari Yamada, Kota Ishizawa, Marissa S. Mattar, Kaoru Funabashi, Qing Chang, Shuichi Ohkubo, Wakako Yano, Ryuichiro Terada, Claudio Giuliano, Yue Christine Lu, Annalisa Bonifacio, Siddharth Kunte, Monika A. Davare, Emily H. Cheng, Elisa de Stanchina, Emanuela Lovati, Yoshikazu Iwasawa, Marc Ladanyi, Romel Somwar. Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations. Nature Cancer 2023, 4 (9) , 1345-1361. https://doi.org/10.1038/s43018-023-00630-y
    69. Xiaoling Song, Yifan Wu, Xiaojuan Qu, Biao Jiang. Applications of macrocyclic molecules in cancer therapy: Target cancer development or overcome drug resistance. MedComm – Oncology 2023, 2 (3) https://doi.org/10.1002/mog2.50
    70. Brian Anderson, Peter Rosston, Han Wee Ong, Mohammad Anwar Hossain, Zachary W. Davis-Gilbert, David H. Drewry. How many kinases are druggable? A review of our current understanding. Biochemical Journal 2023, 480 (16) , 1331-1363. https://doi.org/10.1042/BCJ20220217
    71. E. V. Reutova, K. K. Laktionov, E. Yu. Antonova, J. K. Avakyants, G. A. Tkachenko. Safety profile of lorlatinib: correction of adverse events. Meditsinskiy sovet = Medical Council 2023, (11) , 18-25. https://doi.org/10.21518/ms2023-239
    72. Anne-Florence Blandin, Ross Giglio, Maya Srikanth Graham, Guadalupe Garcia, Seth Malinowski, Jared K. Woods, Shakti Ramkissoon, Lori Ramkissoon, Frank Dubois, Kathleen Schoolcraft, Jessica Tsai, Dayle Wang, Robert Jones, Jayne Vogelzang, Kristine Pelton, Sarah Becker, Fiona Watkinson, Claire Sinai, Elizabeth F. Cohen, Matthew A. Booker, Michael Y. Tolstorukov, Veerle Haemels, Liliana Goumnerova, Karen Wright, Mark Kieran, Katie Fehnel, David Reardon, Arnault Tauziede-Espariat, Rishi Lulla, Benjamin Carcamo, Stanley Chaleff, Alain Charest, Frederik De Smet, Azra H. Ligon, Adrian Dubuc, Melanie Pages, Pascale Varlet, Patrick Y. Wen, Brian M. Alexander, Susan Chi, Sanda Alexandrescu, Ralf Kittler, Robert Bachoo, Pratiti Bandopadhayay, Rameen Beroukhim, Keith L. Ligon. ALK Amplification and Rearrangements Are Recurrent Targetable Events in Congenital and Adult Glioblastoma. Clinical Cancer Research 2023, 29 (14) , 2651-2667. https://doi.org/10.1158/1078-0432.CCR-21-3521
    73. Zainab Rehman, W.Trent Franks, Bao Nguyen, Heather Frericks Schmidt, Garry Scrivens, Steven P. Brown. Discovering the Solid-State Secrets of Lorlatinib by NMR Crystallography: To Hydrogen Bond or not to Hydrogen Bond. Journal of Pharmaceutical Sciences 2023, 112 (7) , 1915-1928. https://doi.org/10.1016/j.xphs.2023.02.022
    74. Swapnil P. Bhujbal, Jung-Mi Hah. An Intriguing Purview on the Design of Macrocyclic Inhibitors for Unexplored Protein Kinases through Their Binding Site Comparison. Pharmaceuticals 2023, 16 (7) , 1009. https://doi.org/10.3390/ph16071009
    75. Kihang Choi. The Structure–property Relationships of Clinically Approved Protein Kinase Inhibitors. Current Medicinal Chemistry 2023, 30 (22) , 2518-2541. https://doi.org/10.2174/0929867329666220822123552
    76. Lidong Gong, Ridong Li, Jingjing Gong, Xianling Ning, Jiawei Sun, Qiang Ma, Chuanda Zhu, Yuanyuan Yang, Kerui Lin, Yanglonghao Li, Qiang Zhang, Tiancheng Li, Zhiqiang Lin. Discovery of a miniaturized PROTAC with potent activity and high selectivity. Bioorganic Chemistry 2023, 136 , 106556. https://doi.org/10.1016/j.bioorg.2023.106556
    77. Furong Zeng, Lin Ye, Qian Zhou, Yi He, Yilei Zhang, Guangtong Deng, Xiang Chen, Hong Liu. Inhibiting SCD expression by IGF1R during lorlatinib therapy sensitizes melanoma to ferroptosis. Redox Biology 2023, 61 , 102653. https://doi.org/10.1016/j.redox.2023.102653
    78. Jiayou Cai, Bin Sun, Siqi Yu, Han Zhang, Weicheng Zhang. Heck Macrocyclization in Forging Non-Natural Large Rings including Macrocyclic Drugs. International Journal of Molecular Sciences 2023, 24 (9) , 8252. https://doi.org/10.3390/ijms24098252
    79. Kelly C. Goldsmith, Julie R. Park, Kimberly Kayser, Jemily Malvar, Yueh-Yun Chi, Susan G. Groshen, Judith G. Villablanca, Kateryna Krytska, Lillian M. Lai, Patricia T. Acharya, Fariba Goodarzian, Bruce Pawel, Hiroyuki Shimada, Susan Ghazarian, Lisa States, Lynley Marshall, Louis Chesler, Meaghan Granger, Ami V. Desai, Rajen Mody, Daniel A. Morgenstern, Suzanne Shusterman, Margaret E. Macy, Navin Pinto, Gudrun Schleiermacher, Kieuhoa Vo, Holger C. Thurm, Joseph Chen, Marlon Liyanage, Gerson Peltz, Katherine K. Matthay, Esther R. Berko, John M. Maris, Araz Marachelian, Yael P. Mossé. Lorlatinib with or without chemotherapy in ALK-driven refractory/relapsed neuroblastoma: phase 1 trial results. Nature Medicine 2023, 29 (5) , 1092-1102. https://doi.org/10.1038/s41591-023-02297-5
    80. Yasushi Goto, Hirotsugu Kenmotsu, Motohiro Tamiya, Shuji Murakami, Takayasu Kurata, Noriko Yanagitani, Hirokazu Taniguchi, Shoichi Kuyama, Junichi Shimizu, Toshihide Yokoyama, Naoko Shimada, Tadashi Maeda, Akihiro Tamiya, Ayumi Uchiyama, Kazuyoshi Imaizumi, Takayuki Takahama, Terufumi Kato, Hidetoshi Hayashi, Naoko Shiraiwa, Shigeyuki Toyoizumi, Hironori Kikkawa, Despina Thomaidou, Makoto Nishio. A Retrospective, Multicenter, Observational Study to Evaluate Clinical Outcomes of Lorlatinib After Alectinib in Patients With ALK-Positive NSCLC in Japan. JTO Clinical and Research Reports 2023, 4 (5) , 100508. https://doi.org/10.1016/j.jtocrr.2023.100508
    81. Md Shahid Ayaz, Ritu Bhupal, Priyanka Sharma, Adarsh Sahu, Parwati Singh, Ghanshyam Das Gupta, Vivek Asati. Recent Updates on Structural Aspects of ALK Inhibitors as an Anticancer Agent. Anti-Cancer Agents in Medicinal Chemistry 2023, 23 (8) , 900-921. https://doi.org/10.2174/1871520623666230110114620
    82. Dorine de Jong, Jeeban P. Das, Hong Ma, Jacienta Pailey Valiplackal, Conor Prendergast, Tina Roa, Brian Braumuller, Aileen Deng, Laurent Dercle, Randy Yeh, Mary M. Salvatore, Kathleen M. Capaccione. Novel Targets, Novel Treatments: The Changing Landscape of Non-Small Cell Lung Cancer. Cancers 2023, 15 (10) , 2855. https://doi.org/10.3390/cancers15102855
    83. Sai-Hong Ignatius Ou, Alexandria T.M. Lee, Misako Nagasaka. From preclinical efficacy to 2022 updated CROWN trial, lorlatinib is the preferred 1st-line treatment of advanced ALK+ NSCLC.. Critical Reviews in Oncology/Hematology 2023, 448 , 104019. https://doi.org/10.1016/j.critrevonc.2023.104019
    84. Deyi Ma, Mengrao Guo, Xin Zhai. An updated patent review of anaplastic lymphoma kinase inhibitors (2018–2022). Expert Opinion on Therapeutic Patents 2023, 33 (4) , 323-337. https://doi.org/10.1080/13543776.2023.2216381
    85. Benjamin J Solomon, Todd M Bauer, Tony S K Mok, Geoffrey Liu, Julien Mazieres, Filippo de Marinis, Yasushi Goto, Dong-Wan Kim, Yi-Long Wu, Jacek Jassem, Froylán López López, Ross A Soo, Alice T Shaw, Anna Polli, Rossella Messina, Laura Iadeluca, Francesca Toffalorio, Enriqueta Felip. Efficacy and safety of first-line lorlatinib versus crizotinib in patients with advanced, ALK-positive non-small-cell lung cancer: updated analysis of data from the phase 3, randomised, open-label CROWN study. The Lancet Respiratory Medicine 2023, 11 (4) , 354-366. https://doi.org/10.1016/S2213-2600(22)00437-4
    86. Jan E. Strøbech, Pietro Giuriatti, Rikke Stagaard, Paulo De Sepulveda, Sebastian R. Nielsen, Janine T. Erler. FES null mice demonstrate a reduction in neutrophil dependent pancreatic cancer metastatic burden. Frontiers in Oncology 2023, 13 https://doi.org/10.3389/fonc.2023.1096499
    87. 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. NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations. Cancer Discovery 2023, 13 (3) , 598-615. https://doi.org/10.1158/2159-8290.CD-22-0968
    88. So Yeong Cheon, Sunghark Kwon. Molecular Anatomy of the EML4-ALK Fusion Protein for the Development of Novel Anticancer Drugs. International Journal of Molecular Sciences 2023, 24 (6) , 5821. https://doi.org/10.3390/ijms24065821
    89. Mariona Riudavets, David Planchard. An update on lorlatinib: a novel first line treatment for ALK -positive advanced lung cancer. Expert Opinion on Pharmacotherapy 2023, 24 (3) , 291-299. https://doi.org/10.1080/14656566.2022.2161880
    90. Koichi Ando, Ryo Manabe, Yasunari Kishino, Sojiro Kusumoto, Toshimitsu Yamaoka, Akihiko Tanaka, Tohru Ohmori, Hironori Sagara. Comparative Efficacy of ALK Inhibitors for Treatment-Naïve ALK-Positive Advanced Non-Small Cell Lung Cancer with Central Nervous System Metastasis: A Network Meta-Analysis. International Journal of Molecular Sciences 2023, 24 (3) , 2242. https://doi.org/10.3390/ijms24032242
    91. Misako Nagasaka, Sai-Hong Ignatius Ou. CROWN 2022 Second Interim Updates: When Will Be the Coronation of Lorlatinib?. Journal of Thoracic Oncology 2023, 18 (2) , 139-142. https://doi.org/10.1016/j.jtho.2022.10.019
    92. Marina Ferreira Candido, Mariana Medeiros, Luciana Chain Veronez, David Bastos, Karla Laissa Oliveira, Julia Alejandra Pezuk, Elvis Terci Valera, María Sol Brassesco. Drugging Hijacked Kinase Pathways in Pediatric Oncology: Opportunities and Current Scenario. Pharmaceutics 2023, 15 (2) , 664. https://doi.org/10.3390/pharmaceutics15020664
    93. Masatoshi Yamazoe, Hiroaki Ozasa, Takahiro Tsuji, Tomoko Funazo, Hiroshi Yoshida, Kentaro Hashimoto, Kazutaka Hosoya, Tatsuya Ogimoto, Hitomi Ajimizu, Hironori Yoshida, Ryo Itotani, Yuichi Sakamori, Kiyomitsu Kuninaga, Wataru Aoki, Toyohiro Hirai. Yes‐associated protein 1 mediates initial cell survival during lorlatinib treatment through AKT signaling in ROS1 ‐rearranged lung cancer. Cancer Science 2023, 114 (2) , 546-560. https://doi.org/10.1111/cas.15622
    94. Kei Oguchi, Hikari Araki, Shingo Tsuji, Masayuki Nakamura, Akihiro Miura, Kaoru Funabashi, Akiko Osada, Sakiho Tanaka, Takamasa Suzuki, Susumu S. Kobayashi, Shinji Mizuarai. TAS2940 , a novel brain‐penetrable pan‐ERBB inhibitor, for tumors with HER2 and EGFR aberrations. Cancer Science 2023, 114 (2) , 654-664. https://doi.org/10.1111/cas.15617
    95. Rongrong Wu, Shinan Liu, Guoli Lv, Chaowen Deng, Ruolan Wang, Shenglin Zhang, Dongyi Zhu, Le Wang, Youming Lei, Zhuang Luo. First-line crizotinib therapy is effective for a novel SEC31A-anaplastic lymphoma kinase fusion in a patient with stage IV lung adenocarcinoma: a case report and literature reviews. Anti-Cancer Drugs 2023, 34 (2) , 294-301. https://doi.org/10.1097/CAD.0000000000001408
    96. Masanobu Ishii, Takashi Kawai, Kenichi Tsujita, Ataru Igarashi, Manabu Suzuki, Hisato Deguchi, Jovelle Fernandez. Cost-Effectiveness of Vonoprazan Compared With Proton Pump Inhibitors in Patients Taking Low-Dose Aspirin for Secondary Prevention of Cardiovascular Events in Japan. Circulation Journal 2023, 87 (2) , 348-359. https://doi.org/10.1253/circj.CJ-22-0127
    97. Surya K. De. Targeted therapy. 2023, 205-411. https://doi.org/10.1016/B978-0-443-13312-1.00002-7
    98. Carmen Avendaño, J. Carlos Menéndez. Anticancer drugs acting on signaling pathways, part 1: Tyrosine kinase inhibitors. 2023, 493-563. https://doi.org/10.1016/B978-0-12-818549-0.00018-2
    99. Yang Yu, Zhe Wang, Lingling Wang, Qinghua Wang, Rongfan Tang, Sutong Xiang, Qirui Deng, Tingjun Hou, Huiyong Sun. Deciphering the Shared and Specific Drug Resistance Mechanisms of Anaplastic Lymphoma Kinase via Binding Free Energy Computation. Research 2023, 6 https://doi.org/10.34133/research.0170
    100. Hirokazu Taniguchi, Kazumasa Akagi, Yosuke Dotsu, Tadaaki Yamada, Sawana Ono, Erika Imamura, Hiroshi Gyotoku, Shinnosuke Takemoto, Hiroyuki Yamaguchi, Triparna Sen, Seiji Yano, Hiroshi Mukae. Pan‐HER inhibitors overcome lorlatinib resistance caused by NRG1 / HER3 activation in ALK ‐rearranged lung cancer. Cancer Science 2023, 114 (1) , 164-173. https://doi.org/10.1111/cas.15579
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