4clj › Citations

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.

Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP
J Med Chem 57 4720-44 (2014)
Related entries: 4cli, 4cmo, 4cmt, 4cmu, 4cnh, 4ctb, 4ctc, 5kz0

Cited: 237 times
EuropePMC logo PMID: 24819116

Abstract

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.

Reviews - 4clj mentioned but not cited (1)

  1. Molecular Anatomy of the EML4-ALK Fusion Protein for the Development of Novel Anticancer Drugs. Cheon SY, Kwon S. Int J Mol Sci 24 5821 (2023)

Articles - 4clj mentioned but not cited (3)



Reviews citing this publication (104)

  1. Understanding and targeting resistance mechanisms in NSCLC. Rotow J, Bivona TG. Nat Rev Cancer 17 637-658 (2017)
  2. Targeting ALK: Precision Medicine Takes on Drug Resistance. Lin JJ, Riely GJ, Shaw AT. Cancer Discov 7 137-155 (2017)
  3. Kinase drug discovery 20 years after imatinib: progress and future directions. Cohen P, Cross D, Jänne PA. Nat Rev Drug Discov 20 551-569 (2021)
  4. Therapeutic targeting of anaplastic lymphoma kinase in lung cancer: a paradigm for precision cancer medicine. Katayama R, Lovly CM, Shaw AT. Clin Cancer Res 21 2227-2235 (2015)
  5. The role of the ALK receptor in cancer biology. Hallberg B, Palmer RH. Ann Oncol 27 Suppl 3 iii4-iii15 (2016)
  6. Trends in kinase drug discovery: targets, indications and inhibitor design. Attwood MM, Fabbro D, Sokolov AV, Knapp S, Schiöth HB. Nat Rev Drug Discov 20 839-861 (2021)
  7. Making the first move in EGFR-driven or ALK-driven NSCLC: first-generation or next-generation TKI? Recondo G, Facchinetti F, Olaussen KA, Besse B, Friboulet L. Nat Rev Clin Oncol 15 694-708 (2018)
  8. Modern advances in heterocyclic chemistry in drug discovery. Taylor AP, Robinson RP, Fobian YM, Blakemore DC, Jones LH, Fadeyi O. Org Biomol Chem 14 6611-6637 (2016)
  9. Leptomeningeal carcinomatosis in non-small cell lung cancer patients: A continuing challenge in the personalized treatment era. Remon J, Le Rhun E, Besse B. Cancer Treat Rev 53 128-137 (2017)
  10. Crizotinib resistance: implications for therapeutic strategies. Dagogo-Jack I, Shaw AT. Ann Oncol 27 Suppl 3 iii42-iii50 (2016)
  11. ALK: a tyrosine kinase target for cancer therapy. Holla VR, Elamin YY, Bailey AM, Johnson AM, Litzenburger BC, Khotskaya YB, Sanchez NS, Zeng J, Shufean MA, Shaw KR, Mendelsohn J, Mills GB, Meric-Bernstam F, Simon GR. Cold Spring Harb Mol Case Stud 3 a001115 (2017)
  12. Emerging therapies for non-small cell lung cancer. Zhang C, Leighl NB, Wu YL, Zhong WZ. J Hematol Oncol 12 45 (2019)
  13. Novel ALK inhibitors in clinical use and development. Iragavarapu C, Mustafa M, Akinleye A, Furqan M, Mittal V, Cang S, Liu D. J Hematol Oncol 8 17 (2015)
  14. ALK inhibitors in non-small cell lung cancer: the latest evidence and developments. Sullivan I, Planchard D. Ther Adv Med Oncol 8 32-47 (2016)
  15. Nucleophosmin-anaplastic lymphoma kinase: the ultimate oncogene and therapeutic target. Werner MT, Zhao C, Zhang Q, Wasik MA. Blood 129 823-831 (2017)
  16. Molecular mechanisms that underpin EML4-ALK driven cancers and their response to targeted drugs. Bayliss R, Choi J, Fennell DA, Fry AM, Richards MW. Cell Mol Life Sci 73 1209-1224 (2016)
  17. Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management. Cooper AJ, Sequist LV, Lin JJ. Nat Rev Clin Oncol 19 499-514 (2022)
  18. Future options for ALK-positive non-small cell lung cancer. Iacono D, Chiari R, Metro G, Bennati C, Bellezza G, Cenci M, Ricciuti B, Sidoni A, Baglivo S, Minotti V, Crinò L. Lung Cancer 87 211-219 (2015)
  19. Targeted Therapy in Advanced and Metastatic Non-Small Cell Lung Cancer. An Update on Treatment of the Most Important Actionable Oncogenic Driver Alterations. König D, Savic Prince S, Rothschild SI. Cancers (Basel) 13 804 (2021)
  20. Tumor Resistance against ALK Targeted Therapy-Where It Comes From and Where It Goes. Sharma GG, Mota I, Mologni L, Patrucco E, Gambacorti-Passerini C, Chiarle R. Cancers (Basel) 10 E62 (2018)
  21. Anaplastic lymphoma kinase (ALK) inhibitors in the treatment of ALK-driven lung cancers. Roskoski R. Pharmacol Res 117 343-356 (2017)
  22. Anaplastic Lymphoma Kinase as a Cancer Target in Pediatric Malignancies. Mossé YP. Clin Cancer Res 22 546-552 (2016)
  23. Barriers to Effective Drug Treatment for Brain Metastases: A Multifactorial Problem in the Delivery of Precision Medicine. Kim M, Kizilbash SH, Laramy JK, Gampa G, Parrish KE, Sarkaria JN, Elmquist WF. Pharm Res 35 177 (2018)
  24. First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib. Basit S, Ashraf Z, Lee K, Latif M. Eur J Med Chem 134 348-356 (2017)
  25. Therapeutic Sequencing in ALK+ NSCLC. Elsayed M, Christopoulos P. Pharmaceuticals (Basel) 14 80 (2021)
  26. Anaplastic lymphoma kinase fusions: Roles in cancer and therapeutic perspectives. Cao Z, Gao Q, Fu M, Ni N, Pei Y, Ou WB. Oncol Lett 17 2020-2030 (2019)
  27. Management of brain metastasized non-small cell lung cancer (NSCLC) - From local treatment to new systemic therapies. Tsakonas G, De Petris L, Ekman S. Cancer Treat Rev 54 122-131 (2017)
  28. Beyond EGFR and ALK inhibition: unravelling and exploiting novel genetic alterations in advanced non small-cell lung cancer. Califano R, Abidin A, Tariq NU, Economopoulou P, Metro G, Mountzios G. Cancer Treat Rev 41 401-411 (2015)
  29. Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview. Fischer PM. Med Res Rev 37 314-367 (2017)
  30. Optimal management of ALK-positive NSCLC progressing on crizotinib. Metro G, Tazza M, Matocci R, Chiari R, Crinò L. Lung Cancer 106 58-66 (2017)
  31. Spotlight on lorlatinib and its potential in the treatment of NSCLC: the evidence to date. Akamine T, Toyokawa G, Tagawa T, Seto T. Onco Targets Ther 11 5093-5101 (2018)
  32. Transporter and Lysosomal Mediated (Multi)drug Resistance to Tyrosine Kinase Inhibitors and Potential Strategies to Overcome Resistance. de Klerk DJ, Honeywell RJ, Jansen G, Peters GJ. Cancers (Basel) 10 E503 (2018)
  33. Tackling Crizotinib Resistance: The Pathway from Drug Discovery to the Pediatric Clinic. Tucker ER, Danielson LS, Innocenti P, Chesler L. Cancer Res 75 2770-2774 (2015)
  34. The next-generation ALK inhibitors. Pall G. Curr Opin Oncol 27 118-124 (2015)
  35. The ALK receptor in sympathetic neuron development and neuroblastoma. Janoueix-Lerosey I, Lopez-Delisle L, Delattre O, Rohrer H. Cell Tissue Res 372 325-337 (2018)
  36. Therapeutic advances in non-small cell lung cancer: Focus on clinical development of targeted therapy and immunotherapy. Cheng Y, Zhang T, Xu Q. MedComm (2020) 2 692-729 (2021)
  37. Therapeutic strategies and mechanisms of drug resistance in anaplastic lymphoma kinase (ALK)-rearranged lung cancer. Katayama R. Pharmacol Ther 177 1-8 (2017)
  38. Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels. Heffron TP. Neuro Oncol 20 307-312 (2018)
  39. Impact of the Protein Data Bank on antineoplastic approvals. Westbrook JD, Soskind R, Hudson BP, Burley SK. Drug Discov Today 25 837-850 (2020)
  40. New Treatment Options for ALK-Rearranged Non-Small Cell Lung Cancer. Cameron L, Solomon B. Curr Treat Options Oncol 16 49 (2015)
  41. Turning liabilities into opportunities: Off-target based drug repurposing in cancer. Palve V, Liao Y, Remsing Rix LL, Rix U. Semin Cancer Biol 68 209-229 (2021)
  42. ALK and ROS1 as targeted therapy paradigms and clinical implications to overcome crizotinib resistance. Ye M, Zhang X, Li N, Zhang Y, Jing P, Chang N, Wu J, Ren X, Zhang J. Oncotarget 7 12289-12304 (2016)
  43. Current and developing therapies for the treatment of non-small cell lung cancer with ALK abnormalities: update and perspectives for clinical practice. Caccese M, Ferrara R, Pilotto S, Carbognin L, Grizzi G, Caliò A, Brunelli M, Cuppone F, Petraglia S, Scarpa A, Tortora G, Bria E. Expert Opin Pharmacother 17 2253-2266 (2016)
  44. Small molecule inhibitors targeting the cancers. Liu GH, Chen T, Zhang X, Ma XL, Shi HS. MedComm (2020) 3 e181 (2022)
  45. Tackling ALK in non-small cell lung cancer: the role of novel inhibitors. Facchinetti F, Tiseo M, Di Maio M, Graziano P, Bria E, Rossi G, Rossi G, Novello S. Transl Lung Cancer Res 5 301-321 (2016)
  46. Personalized treatment in advanced ALK-positive non-small cell lung cancer: from bench to clinical practice. Passaro A, Lazzari C, Karachaliou N, Spitaleri G, Pochesci A, Catania C, Rosell R, de Marinis F. Onco Targets Ther 9 6361-6376 (2016)
  47. Re-Evaluating Progression in an Era of Progress: A Review of First- and Second-Line Treatment Options in Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer. Castellanos EH, Horn L. Oncologist 21 755-761 (2016)
  48. Precision medicine against ALK-positive non-small cell lung cancer: beyond crizotinib. Ricciuti B, De Giglio A, Mecca C, Arcuri C, Marini S, Metro G, Baglivo S, Sidoni A, Bellezza G, Crinò L, Chiari R. Med Oncol 35 72 (2018)
  49. Treatment of ALK-Rearranged Non-Small Cell Lung Cancer: Recent Progress and Future Directions. Cameron L, Solomon B. Drugs 75 1059-1070 (2015)
  50. ALK alterations and inhibition in lung cancer. Le T, Gerber DE. Semin Cancer Biol 42 81-88 (2017)
  51. Central nervous system involvement in ALK-rearranged NSCLC: promising strategies to overcome crizotinib resistance. Russo A, Franchina T, Ricciardi GR, Ferraro G, Scimone A, Bronte G, Russo A, Rolfo C, Adamo V. Expert Rev Anticancer Ther 16 615-623 (2016)
  52. Treating ALK-positive non-small cell lung cancer. Ziogas DC, Tsiara A, Tsironis G, Lykka M, Liontos M, Bamias A, Dimopoulos MA. Ann Transl Med 6 141 (2018)
  53. Treating patients with ALK-positive non-small cell lung cancer: latest evidence and management strategy. Liao BC, Lin CC, Shih JY, Yang JC. Ther Adv Med Oncol 7 274-290 (2015)
  54. Canadian perspectives: update on inhibition of ALK-positive tumours in advanced non-small-cell lung cancer. Melosky B, Cheema P, Agulnik J, Albadine R, Bebb DG, Blais N, Burkes R, Butts C, Card PB, Chan AMY, Hirsh V, Ionescu DN, Juergens R, Morzycki W, Poonja Z, Sangha R, Tehfe M, Tsao MS, Vincent M, Xu Z, Liu G. Curr Oncol 25 317-328 (2018)
  55. Established, emerging and elusive molecular targets in the treatment of lung cancer. Gallant JN, Lovly CM. J Pathol 244 565-577 (2018)
  56. Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies. Wang X, Wang Y, Li X, Yu Z, Song C, Du Y. RSC Med Chem 12 1650-1671 (2021)
  57. Spotlight on ceritinib in the treatment of ALK+ NSCLC: design, development and place in therapy. Santarpia M, Daffinà MG, D'Aveni A, Marabello G, Liguori A, Giovannetti E, Karachaliou N, Gonzalez Cao M, Rosell R, Altavilla G. Drug Des Devel Ther 11 2047-2063 (2017)
  58. The Exploration of Chirality for Improved Druggability within the Human Kinome. Saha D, Kharbanda A, Yan W, Lakkaniga NR, Frett B, Li HY. J Med Chem 63 441-469 (2020)
  59. Treatment modalities for advanced ALK-rearranged non-small-cell lung cancer. Sullivan I, Planchard D. Future Oncol 12 945-961 (2016)
  60. Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I. Bailey JJ, Schirrmacher R, Farrell K, Bernard-Gauthier V. Expert Opin Ther Pat 27 733-751 (2017)
  61. Novel Treatment Strategies for Brain Metastases in Non-small-cell Lung Cancer. Bui N, Woodward B, Johnson A, Husain H. Curr Treat Options Oncol 17 25 (2016)
  62. The accelerated path of ceritinib: Translating pre-clinical development into clinical efficacy. Mok TSK, Crino L, Felip E, Salgia R, De Pas T, Tan DSW, Chow LQM. Cancer Treat Rev 55 181-189 (2017)
  63. Anaplastic lymphoma kinase inhibitors in phase I and phase II clinical trials for non-small cell lung cancer. Karachaliou N, Santarpia M, Gonzalez Cao M, Teixido C, Sosa AE, Berenguer J, Rodriguez Capote A, Altavilla G, Rosell R. Expert Opin Investig Drugs 26 713-722 (2017)
  64. Combating acquired resistance to tyrosine kinase inhibitors in lung cancer. Lovly CM. Am Soc Clin Oncol Educ Book e165-73 (2015)
  65. New generation anaplastic lymphoma kinase inhibitors. Delmonte A, Burgio MA, Verlicchi A, Bronte G, Cravero P, Ulivi P, Martinelli G, Crinò L. Transl Lung Cancer Res 8 S280-S289 (2019)
  66. Oncogene addicted non-small-cell lung cancer: current standard and hot topics. Vecchiarelli S, Bennati C. Future Oncol 14 3-17 (2018)
  67. Comparative Efficacy and Safety of Lorlatinib and Alectinib for ALK-Rearrangement Positive Advanced Non-Small Cell Lung Cancer in Asian and Non-Asian Patients: A Systematic Review and Network Meta-Analysis. Ando K, Manabe R, Kishino Y, Kusumoto S, Yamaoka T, Tanaka A, Ohmori T, Sagara H. Cancers (Basel) 13 3704 (2021)
  68. Enigmas in tumor resistance to kinase inhibitors and calculation of the drug resistance index for cancer (DRIC). Smith CIE. Semin Cancer Biol 45 36-49 (2017)
  69. Systemic Therapy of Lung Cancer CNS Metastases Using Molecularly Targeted Agents and Immune Checkpoint Inhibitors. O'Kane GM, Leighl NB. CNS Drugs 32 527-542 (2018)
  70. Systemic therapies in the treatment of non-small-cell lung cancer brain metastases. Lukas RV, Kumthekar P, Rizvi S, Salgia R. Future Oncol 12 1045-1058 (2016)
  71. Emerging Gene Fusion Drivers in Primary and Metastatic Central Nervous System Malignancies: A Review of Available Evidence for Systemic Targeted Therapies. Brastianos PK, Ippen FM, Hafeez U, Gan HK. Oncologist 23 1063-1075 (2018)
  72. Macrocycles in Drug Discovery─Learning from the Past for the Future. Garcia Jimenez D, Poongavanam V, Kihlberg J. J Med Chem 66 5377-5396 (2023)
  73. Molecular and clinical features of second-generation anaplastic lymphoma kinase inhibitors: ceritinib. De Pas T, Pala L, Catania C, Conforti F. Future Oncol 13 2629-2644 (2017)
  74. 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. Signal Transduct Target Ther 6 423 (2021)
  75. Optimal Care for Patients with Anaplastic Lymphoma Kinase (ALK)-Positive Non-Small Cell Lung Cancer: A Review on the Role and Utility of ALK Inhibitors. Singh A, Chen H. Cancer Manag Res 12 6615-6628 (2020)
  76. Brain Metastasis Treatment: The Place of Tyrosine Kinase Inhibitors and How to Facilitate Their Diffusion across the Blood-Brain Barrier. Angeli E, Bousquet G. Pharmaceutics 13 1446 (2021)
  77. Current Knowledge about Mechanisms of Drug Resistance against ALK Inhibitors in Non-Small Cell Lung Cancer. Smolle E, Taucher V, Lindenmann J, Jost PJ, Pichler M. Cancers (Basel) 13 699 (2021)
  78. Lorlatinib for the treatment of anaplastic lymphoma kinase-positive non-small cell lung cancer. Yang J, Gong W. Expert Rev Clin Pharmacol 12 173-178 (2019)
  79. New systemic strategies for overcoming resistance to targeted therapies in non-small cell lung cancer. Genova C, Rijavec E, Biello F, Rossi G, Barletta G, Dal Bello MG, Vanni I, Coco S, Alama A, Grossi F. Expert Opin Pharmacother 18 19-33 (2017)
  80. Synthetic Heterocyclic Derivatives as Kinase Inhibitors Tested for the Treatment of Neuroblastoma. Musumeci F, Cianciusi A, D'Agostino I, Grossi G, Carbone A, Schenone S. Molecules 26 7069 (2021)
  81. Update on Lorlatinib: Role in Reducing the Risk of Disease Progression in ALK-Positive NSCLC. Yun KM, Bazhenova LA. Cancer Manag Res 14 843-850 (2022)
  82. Upfront Management of ALK-Rearranged Metastatic Non-small Cell Lung Cancer: One Inhibitor Fits All? Tabbò F, Passiglia F, Novello S. Curr Oncol Rep 23 10 (2021)
  83. An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review. Liang Y, Fang R, Rao Q. Molecules 27 2837 (2022)
  84. Non-small-cell lung cancer: how to manage ALK-, ROS1- and NTRK-rearranged disease. Marinelli D, Siringo M, Metro G, Ricciuti B, Gelibter AJ. Drugs Context 11 (2022)
  85. Targeting MYCN and ALK in resistant and relapsing neuroblastoma. Tucker ER, Poon E, Chesler L. Cancer Drug Resist 2 803-812 (2019)
  86. [Pharmacology and Clinical Evaluation of Ensartinib Hydrochloride Capsule]. Wang Y, Yuan X, Xiong J, Hao Z, Peng X, Chen W, Cui L, Li H, Wang X, He X, Yang M, Liang C, Ma Y, Ding L, Mao L. Zhongguo Fei Ai Za Zhi 23 719-729 (2020)
  87. 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. Ando K, Manabe R, Kishino Y, Kusumoto S, Yamaoka T, Tanaka A, Ohmori T, Sagara H. Int J Mol Sci 24 2242 (2023)
  88. Harnessing the cyclization strategy for new drug discovery. Tang K, Wang S, Gao W, Song Y, Yu B. Acta Pharm Sin B 12 4309-4326 (2022)
  89. How selecting best upfront therapy for metastatic disease?-Focus on ROS1-rearranged disease. Landi L, Cappuzzo F. Transl Lung Cancer Res 9 2686-2695 (2020)
  90. Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies. Li G, Cheng Y, Han C, Song C, Huang N, Du Y. RSC Med Chem 13 1300-1321 (2022)
  91. Diverse Neutrophil Functions in Cancer and Promising Neutrophil-Based Cancer Therapies. Sounbuli K, Mironova N, Alekseeva L. Int J Mol Sci 23 15827 (2022)
  92. Drugging Hijacked Kinase Pathways in Pediatric Oncology: Opportunities and Current Scenario. Candido MF, Medeiros M, Veronez LC, Bastos D, Oliveira KL, Pezuk JA, Valera ET, Brassesco MS. Pharmaceutics 15 664 (2023)
  93. Evolution strategy of ROS1 kinase inhibitors for use in cancer therapy. Liu S, Yang H, Jiang Y, Zhang T, Yan R, Zhang J. Future Med Chem 10 1705-1720 (2018)
  94. Targeting EGFR and ALK in NSCLC: current evidence and future perspective. Bennati C, Paglialunga L, Ricciuti B, Metro G, Marcomigni L, Gili A, Crinò L. Lung Cancer Manag 5 79-90 (2016)
  95. The role of histone lysine demethylases in cancer cells' resistance to tyrosine kinase inhibitors. White JC, Pucci P, Crea F. Cancer Drug Resist 2 326-334 (2019)
  96. Agents in the preclinical development stage for non-small cell lung cancer. Sacco PC, Sgambato A, Casaluce F, Maione P, Rossi A, Palazzolo G, Napolitano A, Gridelli C. Expert Rev Anticancer Ther 15 1361-1366 (2015)
  97. An Intriguing Purview on the Design of Macrocyclic Inhibitors for Unexplored Protein Kinases through Their Binding Site Comparison. Bhujbal SP, Hah JM. Pharmaceuticals (Basel) 16 1009 (2023)
  98. Biology and impact of lineage plasticity in ALK-positive NSCLC: a narrative review. Meador CB, Piotrowska Z. Transl Lung Cancer Res 12 837-856 (2023)
  99. Heck Macrocyclization in Forging Non-Natural Large Rings including Macrocyclic Drugs. Cai J, Sun B, Yu S, Zhang H, Zhang W. Int J Mol Sci 24 8252 (2023)
  100. Importance of ROS1 gene fusions in non-small cell lung cancer. Muminovic M, Carracedo Uribe CR, Alvarez-Pinzon A, Shan K, Raez LE. Cancer Drug Resist 6 332-344 (2023)
  101. Latest perspectives of orally bioavailable 2,4-diarylaminopyrimidine analogues (DAAPalogues) as anaplastic lymphoma kinase inhibitors: discovery and clinical developments. Latif M, Ashraf Z, Basit S, Ghaffar A, Ghaffar A, Zafar MS, Saeed A, Meo SA. RSC Adv 8 16470-16493 (2018)
  102. Metastasis manners and the underlying mechanisms of ALK and ROS1 rearrangement lung cancer and current possible therapeutic strategies. Chang X, Liu Z, Man S, Roys A, Li Z, Zuo D, Wu Y. RSC Adv 9 17921-17932 (2019)
  103. Novel Targets, Novel Treatments: The Changing Landscape of Non-Small Cell Lung Cancer. de Jong D, Das JP, Ma H, Pailey Valiplackal J, Prendergast C, Roa T, Braumuller B, Deng A, Dercle L, Yeh R, Salvatore MM, Capaccione KM. Cancers (Basel) 15 2855 (2023)
  104. Recent Advances in the Management of Adverse Events Associated with Lorlatinib. Liao D, Zhang J, Yan T, Chen S, Li W, Shangguan D, She Z. Onco Targets Ther 16 731-738 (2023)

Articles citing this publication (129)



Quick links