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Repotrectinib (TPX-0005) is a next-generation ROS1/TRK/ALK inhibitor that potently inhibit ROS1/TRK/ALK solvent-front mutations
DC Field | Value | Language |
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dc.contributor.author | Drilon, Alexander | - |
dc.contributor.author | Ou, Sai-Hong Ignatius | - |
dc.contributor.author | Cho, Byoung Chul | - |
dc.contributor.author | Kim, Dong-Wan | - |
dc.contributor.author | Lees, Jeeyun | - |
dc.contributor.author | Lin, Jessica J. | - |
dc.contributor.author | Zhu, Viola W. | - |
dc.contributor.author | Ahns, Myung-Ju | - |
dc.contributor.author | Camidge, D. Ross | - |
dc.contributor.author | Nguyen, Judy | - |
dc.contributor.author | Zhai, Dayong | - |
dc.contributor.author | Deng, Wei | - |
dc.contributor.author | Huang, Zhongdong | - |
dc.contributor.author | Rogers, Evan | - |
dc.contributor.author | Liu, Juliet | - |
dc.contributor.author | Whitten, Jeff | - |
dc.contributor.author | Lim, John K. | - |
dc.contributor.author | Stopatschinskaja, Shanna | - |
dc.contributor.author | Hyman, David M. | - |
dc.contributor.author | Doebele, Robert C. | - |
dc.contributor.author | Cui, J. Jean | - |
dc.contributor.author | Shaw, Alice T. | - |
dc.date.accessioned | 2020-04-27T11:03:21Z | - |
dc.date.available | 2020-04-27T11:03:21Z | - |
dc.date.created | 2019-06-24 | - |
dc.date.issued | 2018-10 | - |
dc.identifier.citation | Cancer Discovery, Vol.8 No.10, pp.1227-1236 | - |
dc.identifier.issn | 2159-8274 | - |
dc.identifier.other | 76462 | - |
dc.identifier.uri | https://hdl.handle.net/10371/165233 | - |
dc.description.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, ROSI, 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 ALK(G1202R), ROS1(G2032R) or ROS1(D2033N), TRKA(G595R), 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 solventfront 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 fusionpositive 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-, NTRKI-3-, or ALK-rearranged malignancies who have progressed on earlier-generation TKIs. (C) 2018 AACR. | - |
dc.language | 영어 | - |
dc.publisher | American Association for Cancer Research Inc. | - |
dc.title | Repotrectinib (TPX-0005) is a next-generation ROS1/TRK/ALK inhibitor that potently inhibit ROS1/TRK/ALK solvent-front mutations | - |
dc.type | Article | - |
dc.contributor.AlternativeAuthor | 김동완 | - |
dc.identifier.doi | 10.1158/2159-8290.CD-18-0484 | - |
dc.citation.journaltitle | Cancer Discovery | - |
dc.identifier.wosid | 000446398800005 | - |
dc.identifier.scopusid | 2-s2.0-85054377858 | - |
dc.citation.endpage | 1236 | - |
dc.citation.number | 10 | - |
dc.citation.startpage | 1227 | - |
dc.citation.volume | 8 | - |
dc.identifier.sci | 000446398800005 | - |
dc.description.isOpenAccess | Y | - |
dc.contributor.affiliatedAuthor | Kim, Dong-Wan | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | CELL LUNG-CANCER | - |
dc.subject.keywordPlus | OVERCOMES CRIZOTINIB RESISTANCE | - |
dc.subject.keywordPlus | ACQUIRED-RESISTANCE | - |
dc.subject.keywordPlus | KINASE INHIBITION | - |
dc.subject.keywordPlus | SOLID TUMORS | - |
dc.subject.keywordPlus | ALK | - |
dc.subject.keywordPlus | ROS1 | - |
dc.subject.keywordPlus | TRK | - |
dc.subject.keywordPlus | ENTRECTINIB | - |
dc.subject.keywordPlus | ALECTINIB | - |
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