431
Views
7
CrossRef citations to date
0
Altmetric
Drug Evaluation

Evaluating entrectinib as a treatment option for non-small cell lung cancer

, , , , , , & show all
Pages 1935-1942 | Received 13 May 2020, Accepted 17 Jul 2020, Published online: 31 Jul 2020

References

  • Sgambato A, Casaluce F, Maione P, et al. Targeted therapies in non-small cell lung cancer: a focus on ALK/ROS1 tyrosine kinase inhibitors. Expert Rev Anticancer Ther. 2018;18(1):71–80. .
  • Kheder ES, Hong DS. Emerging targeted therapy for tumors with NTRK fusion proteins. Clin Cancer Res. 2018;24:5807–5814.
  • Pulciani S, Santos E, Lauver AV, et al. Oncogenes in solid human tumours. Nature. 1982;300:539–542.
  • Ardini E, Menichincheri M, Banfi P, et al. Entrectinib, a pan-TRK, ROS1, and ALK inhibitor with activity in multiple molecularly defined cancer indications. Mol Cancer Ther. 2016;15:628–639.
  • Vaishnavi A, Capelletti M, Le AT, et al. Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer. Nat Med. 2013;19:1469–1472.
  • Barbacid M, Lamballe F, Pulido D, et al. The trk family of tyrosine protein kinase receptors. Biochim Biophys Acta. 1991;1072:115–127.
  • Gambella A, Senetta R, Collemi G, et al. NTRK fusions in central nervous system tumors: a rare, but worthy target. Int J Mol Sci. 2020;21:753.
  • Liu D, Offin M, Harnicar S, et al. Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors. Ther Clin Risk Manag. 2018;14:1247–1252.
  • Cocco E, Scaltriti M, Drilon A. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol. 2018;15:731–747.
  • Amatu A, Sartore-Bianchi A, Siena S. NTRK gene fusions as novel targets of cancer therapy across multiple tumour types. ESMO Open. 2016;1:e000023.
  • Menichincheri M, Ardini E, Magnaghi P, et al. Discovery of entrectinib: a new 3-aminoindazole as a potent anaplastic lymphoma kinase (ALK), c-ros oncogene 1 kinase (ROS1), and pan-tropomyosin receptor kinases (Pan-TRKs) inhibitor. J Med Chem. 2016;59:3392–3408.
  • Drilon A, Siena S, Ou SI, et al. 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). Cancer Discov. 2017;7:400–409.
  • Rolfo C, Ruiz R, Giovannetti E, et al. Entrectinib: a potent new TRK, ROS1, and ALK inhibitor. Expert Opin Investig Drugs. 2015;24:1493–1500.
  • Drilon A, Siena S, Dziadziuszko R, et al. Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three phase 1-2 trials. Lancet Oncol. 2020;21:261–270.
  • Doebele RC, Drilon A, Paz-Ares L, et al. Entrectinib in patients with advanced or metastatic NTRK fusion-positive solid tumours: integrated analysis of three phase 1-2 trials. Lancet Oncol. 2020;21:271–282.
  • Al-Salama ZT, Keam SJ. Entrectinib: first global approval. Drugs. 2019;79:1477–1483.
  • Rudzinski ER, Lockwood CM, Stohr BA, et al. Pan-Trk immunohistochemistry identifies ntrk rearrangements in pediatric mesenchymal tumors. Am J Surg Pathol. 2018;42:927–935.
  • Märkl B, Hirschbühl K, Dhillon C. NTRK-fusions - A new kid on the block. Pathol Res Pract. 2019;215:152572.
  • Paz-Ares L, Doebele RC, Farago AF, et al. Entrectinib in NTRK fusion-positive non-small cell lung cancer (NSCLC): integrated analysis of patients (pts) enrolled in STARTRK-2, STARTRK-1 and ALKA-372-001. Ann Oncol. 2019;30:ii48-ii49.
  • Rangaraju S, Farago A, Heym KM, et al. P14.19 preclinical and clinical efficacy of entrectinib in primary and metastatic brain tumors harboring NTRK, ROS1, or ALK gene fusions. Neuro Oncol. 2017;19:iii106-iii106.
  • Lim SM, Kim HR, Lee JS, et al. Open-label, multicenter, phase II study of ceritinib in patients with non-small-cell lung cancer harboring ROS1 rearrangement. J Clin Oncol. 2017;35:2613–2618.
  • Costa DB, Kobayashi S, Pandya SS, et al. CSF concentration of the anaplastic lymphoma kinase inhibitor crizotinib. J Clin Oncol. 2011;29:e443–445.
  • Park S, Ahn BC, Lim SW, et al. Characteristics and outcome of ROS1-positive non-small cell lung cancer patients in routine clinical practice. J Thorac Oncol. 2018;13:1373–1382.
  • Tan AC, Itchins M, Khasraw M. Brain metastases in lung cancers with emerging targetable fusion drivers. Int J Mol Sci. 2020;21:1416.
  • Patil T, Smith DE, Bunn PA, et al. The Incidence of brain metastases in stage IV ROS1-rearranged non-small cell lung cancer and rate of central nervous system progression on crizotinib. J Thorac Oncol. 2018;13:1717–1726.
  • Siena S, Doebele RC, Shaw AT, et al. Efficacy of entrectinib in patients (pts) with solid tumors and central nervous system (CNS) metastases: integrated analysis from three clinical trials. J clin oncol. 2019;37:3017.
  • Lin X, DeAngelis LM. Treatment of Brain Metastases. J Clin Oncol. 2015;33:3475–3484.
  • Shaw AT, Solomon BJ. Crizotinib in ROS1-rearranged non-small-cell lung cancer. N Engl J Med. 2015;372:683–684.
  • Shaw AT, Riely GJ, Bang YJ, et al. Crizotinib in ROS1-rearranged advanced non-small-cell lung cancer (NSCLC): updated results, including overall survival, from PROFILE 1001. Ann Oncol. 2019;30:1121–1126.
  • Socinski MA. Cytotoxic chemotherapy in advanced non-small cell lung cancer: a review of standard treatment paradigms. Clin Cancer Res. 2004;10:4210s–4214s.
  • Drilon A, Laetsch TW, Kummar S, et al. Efficacy of Larotrectinib in TRK Fusion-Positive Cancers in Adults and Children. N Engl J Med. 2018;378:731–739.
  • Drilon A, Kummar S, Moreno V, et al. Activity of larotrectinib in TRK fusion lung cancer. Ann Oncol. 2019;30:ii48-ii49.
  • Drilon AE, DuBois SG, Farago AF, et al. Activity of larotrectinib in TRK fusion cancer patients with brain metastases or primary central nervous system tumors. J clin oncol. 2019;37:2006.
  • Drilon A. TRK inhibitors in TRK fusion-positive cancers. Ann Oncol. 2019;30:viii23–viii30.
  • Peters S, Camidge DR, Shaw AT, et al. Alectinib versus crizotinib in untreated ALK-positive non-small-cell lung cancer. N Engl J Med. 2017;377:829–838.
  • Gainor JF, Dardaei L, Yoda S, et al. Molecular mechanisms of resistance to first- and second-generation ALK Inhibitors in ALK-rearranged lung cancer. Cancer Discov. 2016;6:1118–1133.
  • Syed YY. Lorlatinib: first global approval. Drugs. 2019;79:93–98.
  • Ku BM, Bae YH, Lee KY, et al. Entrectinib resistance mechanisms in ROS1-rearranged non-small cell lung cancer. Invest New Drugs. 2020;38:360–368.
  • Gainor JF, Tseng D, Yoda S, et al. Patterns of metastatic spread and mechanisms of resistance to crizotinib in ROS1-positive non-small-cell lung cancer. JCO Precis Oncol. 2017;2017:10.1200/PO.17.00063.
  • Facchinetti F, Friboulet L. Profile of entrectinib and its potential in the treatment of ROS1-positive NSCLC: evidence to date. Lung Cancer (Auckl). 2019;10:87–94.
  • Katayama R, Gong B, Togashi N, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10:3604.
  • Drilon A, Ou SI, Cho BC, et al. Repotrectinib (TPX-0005) is a next-generation ROS1/TRK/ALK inhibitor that potently inhibits ROS1/TRK/ALK solvent- front mutations. Cancer Discov. 2018;8:1227–1236.
  • Cho BC, Drilon AE, Doebele RC, et al. Safety and preliminary clinical activity of repotrectinib in patients with advanced ROS1 fusion-positive non-small cell lung cancer (TRIDENT-1 study). J clin oncol. 2019;37:9011.
  • Shaw AT, Solomon BJ, Chiari R, et al. Lorlatinib in advanced ROS1-positive non-small-cell lung cancer: a multicentre, open-label, single-arm, phase 1-2 trial. Lancet Oncol. 2019;20:1691–1701.
  • Russo M, Misale S, Wei G, et al. Acquired resistance to the TRK inhibitor entrectinib in colorectal cancer. Cancer Discov. 2016;6:36–44.
  • Drilon A, Li G, Dogan S, et al. What hides behind the MASC: clinical response and acquired resistance to entrectinib after ETV6-NTRK3 identification in a mammary analogue secretory carcinoma (MASC). Ann Oncol. 2016;27:920–926.
  • Scott LJ. Larotrectinib: first global approval. Drugs. 2019;79:201–206.
  • Farago A, Kummar S, Moreno V, et al. MA09.07 Activity of Larotrectinib in TRK Fusion Lung Cancer. J Thorac Oncol. 2019;14:S283–S284.
  • Jin W. Roles of TrkC signaling in the regulation of tumorigenicity and metastasis of cancer. Cancers (Basel). 2020;12(1):147.
  • Hyman D, Kummar S, Farago A, et al. Abstract CT127: phase I and expanded access experience of LOXO-195 (BAY 2731954), a selective next-generation TRK inhibitor (TRKi). Cancer Res. 2019;79:CT127–CT127.

Reprints and Corporate Permissions

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

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

Academic Permissions

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

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

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