Cited by 523Lung Cancer Treatments and MutationsCancer Mechanisms and TherapyCancer Genomics and Diagnostics

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

Drilon, Alexander, Ou, Sai-Hong Ignatius, Cho, Byoung Chul, Kim, Dong-Wan, Lee, Jeeyun, Lin, Jessica J., Zhu, Viola W., Ahn, Myung-Ju, Camidge, D. Ross, Nguyen, Judy, Zhai, Dayong, Deng, Wei, Huang, Zhongdong, Rogers, Evan, Liu, Juliet, Whitten, Jeff, Lim, John K., Stopatschinskaja, Shanna, Hyman, David M., Doebele, Robert C., Cui, J. Jean, Shaw, Alice T.·2018·Cancer Discovery

DOI 10.1158/2159-8290.cd-18-0484

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Abstract

The use of tyrosine kinase inhibitors (TKI) with activity against ALK, ROS1, or TRKA–C can result in significant clinical benefit in patients with diverse tumors harboring ALK, ROS1, or NTRK1–3 rearrangements; however, resistance invariably develops. The emergence of on-target kinase domain mutations represents a major mechanism of acquired resistance. Solvent-front substitutions such as ALKG1202R, ROS1G2032R or ROS1D2033N, TRKAG595R, and TRKCG623R are among the most recalcitrant of these mechanisms. Repotrectinib (TPX-0005) is a rationally designed, low-molecular-weight, macrocyclic TKI that is selective and highly potent against ROS1, TRKA–C, and ALK. Importantly, repotrectinib exhibits activity against a variety of solvent-front substitutions in vitro and in vivo. As clinical proof of concept, in an ongoing first-in-human phase I/II trial, repotrectinib achieved confirmed responses in patients with ROS1 or NTRK3 fusion–positive cancers who had relapsed on earlier-generation TKIs due to ROS1 or TRKC solvent-front substitution-mediated resistance. Significance: Repotrectinib (TPX-0005), a next-generation ROS1, pan-TRK, and ALK TKI, overcomes resistance due to acquired solvent-front mutations involving ROS1, NTRK1–3, and ALK. Repotrectinib may represent an effective therapeutic option for patients with ROS1-, NTRK1–3-, or ALK-rearranged malignancies who have progressed on earlier-generation TKIs. Cancer Discov; 8(10); 1227–36. ©2018 AACR. This article is highlighted in the In This Issue feature, p. 1195

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BackgroundSelf-citation
New pan-ALK inhibitor-resistant EML4::ALK mutations detected by liquid biopsy in lung cancer patients
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“As C1237Y and L1196P mutants appeared to resist all clinical inhibitors, we tested their sensitivity to two novel investigational drugs, zotizalkib (TPX-0131) 16 and repotrectinib (TPX-0005) 17 and compared the compounds activity with their close structural analogue, lorlatinib.”
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Background
ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability
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Background
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BackgroundInfluential
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BackgroundInfluentialSelf-citation
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BackgroundMethodInfluential
ROS1-rearranged Non–small Cell Lung Cancer
Giustini, N., & Bazhenova, L. A. (2020) · Thoracic surgery clinics/Thorac. surg. clin. · doi:10.1016/j.thorsurg.2020.01.007 · Cited by 9
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“Currently, there is no approved NTRK inhibitor to overcome acquired resistance conveyed by the NTRK3 substitution,(14) while the potential of next-generation inhibitors such as LOXO-195 and repotrectinib is investigated in clinical trials.(12,15,26,27) To our knowledge, there are no data on the”
Background
Sequential treatments with TRK inhibitors in a patient with NTRK fusion-positive sarcoma: A case report
Kubota, Y., Kawano, M., Iwasaki, T., Itonaga, I., Tsumura, H., Kaku, N., & Tanaka, K. (2023) · Medicine · doi:10.1097/md.0000000000036232 · Cited by 8
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Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase
Mei, L., Zhuo, L., Xu, H.-C., Huang, W., Hao, G., & Yang, G. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114406 · Cited by 9
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Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
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Discovery of imidazo[1,2-b]pyridazine macrocyclic derivatives as novel ALK inhibitors capable of combating multiple resistant mutants
Xiao, X., Xu, Y., Yu, X., Chen, Y., Zhao, W., Xie, Z., Zhu, X., Xu, H., Yang, Y., & Zhang, P. (2023) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2023.129309 · Cited by 8
Enantioselective and Step-Economic Synthesis of the Chiral Amine Fragment in the Tyrosine Kinase Inhibitor Repotrectinib by Direct Asymmetric Reductive Amination under Batch and Flow
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Dramatic Response to Lorlatinib in a Patient With CD74-ROS1-Positive Lung Adenocarcinoma With Acquired F2004V Mutation
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“Repotrectinib is another potent ROS1 inhibitor with activity against many of these secondary mutations; it is not shown in the figure because the RP2D is not known yet for this drug.(29) Cave values were calculated as the ratio of the area under the curve for 0 to 24 hours to 24 hours of the drug at steady state in pa…”
MethodSelf-citation
Retrospective evaluation of single patient investigational new drug (IND) requests in pediatric oncology
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Background
The oncogenic roles of NTRK fusions and methods of molecular diagnosis
Aref‐Eshghi, E., Lin, F., Li, M. M., & Zhong, Y. (2021) · Cancer Genetics · doi:10.1016/j.cancergen.2021.10.005 · Cited by 8
Recent advances in lung cancer genomics: Application in targeted therapy
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Authors: Drilon, A., Ou, S.-H. I., Cho, B. C., Kim, D.-W., Lee, J., Lin, J. J., Zhu, V. W., Ahn, M.-J., Camidge, D. R., Nguyen, J., Zhai, D., Deng, W., Huang, Z., Rogers, E., Liu, J., Whitten, J., Lim, J. K., Stopatschinskaja, S., Hyman, D. M., Doebele, R. C., Cui, J. J., & Shaw, A. T.
Affiliations: Memorial Sloan Kettering Cancer Center (US)
University of California, Irvine (US)
Yonsei University (KR)
Seoul National University Hospital (KR)
Samsung Medical Center (KR)
Harvard University (US)
University of Colorado Anschutz (US)
8TP Therapeutics Inc., San Diego, California.
Corresponding author: Cui, J. Jean
Shaw, Alice T.
ORCID: Drilon, Alexander
Ou, Sai-Hong Ignatius
Cho, Byoung Chul
Kim, Dong-Wan
Lee, Jeeyun
Lin, Jessica J.
Zhu, Viola W.
Ahn, Myung-Ju
Camidge, D. Ross
Rogers, Evan
Hyman, David M.
Doebele, Robert C.
Cui, J. Jean
Shaw, Alice T.
Venue: Cancer Discovery
Publisher: American Association for Cancer Research (AACR)
Published: 2018-10-01
Volume: 8
Issue: 10
Pages: 1227-1236
ISSN: 2159-8274 (ISSN-L)
2159-8290
DOI: 10.1158/2159-8290.cd-18-0484
OpenAlex: W2885875860
Cited by: 504
References: 23
Citations by year: 2026: 48 · 2025: 64 · 2024: 71 · 2023: 66 · 2022: 69 · 2021: 83 · 2020: 62 · 2019: 37 · 2018: 4
FWCI: 35.60
Type: journal article
Language: en
Open access: closed
Locations: Cancer Discovery (publishedVersion)
PubMed (publishedVersion)
Seoul National University Open Repository (Seoul National University) (submittedVersion)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Mechanisms and Therapy
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Genomics and Diagnostics
Keywords: repotrectinib, ROS1, TRK, anaplastic lymphoma kinase, tyrosine kinase inhibitors, solvent-front mutations, acquired drug resistance, NTRK3 fusion, kinase domain mutations
MeSH terms: Humans, Mutation, Protein-Tyrosine Kinases, Proto-Oncogene Proteins, Protein Kinase Inhibitors

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

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