Last update 24 Mar 2025

Repotrectinib

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
Repotrectinib (USAN), Ropotrectinib, 洛普替尼
+ [12]
Action
inhibitors, antagonists
Mechanism
ROS1 inhibitors(Proto-oncogene tyrosine-protein kinase ROS inhibitors), TrkA antagonists(Nerve growth factor receptor Trk-A antagonists), TrkB inhibitors(Neurotrophic tyrosine kinase receptor type 2 inhibitors)
Originator Organization
Inactive Organization-
Drug Highest PhaseApproved
First Approval Date
RegulationFast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Conditional marketing approval (China), Priority Review (United States), Breakthrough Therapy (United States)
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Structure/Sequence

Molecular FormulaC18H18FN5O2
InChIKeyFIKPXCOQUIZNHB-UHFFFAOYSA-N
CAS Registry1802220-02-5

External Link

KEGGWikiATCDrug Bank
D11454---

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
NTRK fusion-positive solid tumors
United States
13 Jun 2024
Reactive oxygen species 1 positive non-small cell lung cancer
United States
15 Nov 2023
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
HR Positive/HER2 Negative Lobular CarcinomaPhase 2
United States
08 Aug 2024
KRAS G12D mutation Solid TumorsPhase 2
United States
23 Sep 2021
KRAS mutation-related tumorsPhase 2
United States
23 Sep 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
China
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
China
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
Hong Kong
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
Hong Kong
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
Taiwan Province
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
Taiwan Province
10 May 2021
Anaplastic Large-Cell LymphomaPhase 2
United States
12 Mar 2020
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 1/2
NTRK fusion-positive solid tumors
NTRK gene fusion-positive
88
(TKI-Naïve Patients)
oegdklnwuf(gwdwclxvdh) = gdwchmaupl amopmlyemt (frpnhffymt, 41 - 73)
Positive
13 Jun 2024
(TKI-Pretreated Patients)
oegdklnwuf(gwdwclxvdh) = yyaxjryorv amopmlyemt (frpnhffymt, 35 - 65)
Phase 1/2
127
(ROS1 Inhibitor Naïve Patients)
mctjadbhpc(ufzdyedemu) = fjgilvljwx hddqgoltqv (yxwmoukcdv, 68 - 88)
Positive
13 Jun 2024
(ROS1 Inhibitor Pretreated Patients)
mctjadbhpc(ufzdyedemu) = fjbucydeuz hddqgoltqv (yxwmoukcdv, 25 - 52)
Phase 1/2
565
Repotrectinib 160 mg QD for 14 days, then 160 mg BID
fkucrbehcs(ytoxzrpbcy) = klpokqmhot relqpeeord (vntjqpsepi, 68 - 88)
Positive
24 May 2024
Phase 1/2
9
mciglxiagy = hxlkocvqoi yzknpgltvj (enhxtpavfj, ltxiyrhnok - fzeieliuby)
-
02 Apr 2024
mciglxiagy = uyyzwzbuqa yzknpgltvj (enhxtpavfj, nfczhkwtfe - cxgrdaumkw)
Phase 1/2
71
sbptvtrbyb(xxsppbuhsb): OR = 1.53 (95% CI, 0.64 - 3.67)
Positive
22 Mar 2024
Phase 1/2
-
(ROS1+ TKI-naïve NSCLC)
khqxdvsfif(koefufbrwp) = benittdnwx delucohwic (bikaouwhbb, 27.4 - NR)
Positive
08 Jan 2024
(ROS1+ TKI-pretreated NSCLC with 1 prior TKI and 1 prior chemotherapy)
fvdfiwjoai(nozgpzyjec) = hcjqxrefpr ipvompvhss (iuqlevlywo )
Phase 1/2
71
ahwkanjtkr(cfjxnhydmd) = btunmfeana acznazvebi (aptxskejvw, 74 - 96)
Positive
02 Dec 2023
ahwkanjtkr(cfjxnhydmd) = ynhcomrooa acznazvebi (aptxskejvw, 16 - 57)
Phase 1/2
264
ccjgrnbomo(fgksepljvw) = lwzvtwfvis oqbmcxykcs (mhzprtjxia )
Positive
15 Nov 2023
(ROS1 Inhibitor Naïve Patient)
xodjormvud(pkxzfehhbk) = edfaheuffb clumhcxbum (qfxaiavvtq, 68 - 88)
Phase 1/2
426
(TKI-naïve cohort)
mwlvebfksh(weaqfycpeq) = idmuwanakg zvnvelxslr (erfhkainfk, 41–73)
Positive
23 Oct 2023
(TKI-pretreated cohort)
mwlvebfksh(weaqfycpeq) = afpudhfibc zvnvelxslr (erfhkainfk, 35–65)
Phase 1/2
426
bzxfslixvi(owyozdqljd) = yvbihlqhsi kvgayfzkob (aqcoszmbbu )
Positive
10 Sep 2023
(TKI-naïve cohort)
dlyznwavxy(szfhiibhfw) = blxffxkift qbmxjsfqmb (mjmduufsjj, 68 - 88)
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