Last update 08 Mar 2025

Repotrectinib

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
Repotrectinib (USAN), Ropotrectinib, 洛普替尼
+ [12]
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
RegulationBreakthrough Therapy (US), Fast Track (US), Orphan Drug (US), Priority Review (CN), Breakthrough Therapy (CN), Conditional marketing approval (CN), Priority Review (US), Accelerated Approval (US)
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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
US
13 Jun 2024
Reactive oxygen species 1 positive non-small cell lung cancer
US
15 Nov 2023
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
HR Positive/HER2 Negative Lobular CarcinomaPhase 2
US
08 Aug 2024
KRAS G12D mutation Solid TumorsPhase 2
US
23 Sep 2021
KRAS mutation-related tumorsPhase 2
US
23 Sep 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
CN
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
CN
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
HK
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
HK
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
TW
10 May 2021
NTRK fusion-positive Non-small Cell Lung CancerPhase 2
TW
10 May 2021
Anaplastic Large-Cell LymphomaPhase 2
US
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)
spqjhfiifi(lfdocwxytx) = yddadogskn qujodltumu (zpativpmov, 41 - 73)
Positive
13 Jun 2024
(TKI-Pretreated Patients)
spqjhfiifi(lfdocwxytx) = xqfhozbned qujodltumu (zpativpmov, 35 - 65)
Phase 1/2
127
(ROS1 Inhibitor Naïve Patients)
qzhpqmhfpc(ktmpinotra) = mkggsdynla zswdxlepcr (cmwlhsjodb, 68 - 88)
Positive
13 Jun 2024
(ROS1 Inhibitor Pretreated Patients)
qzhpqmhfpc(ktmpinotra) = yomhodcwkv zswdxlepcr (cmwlhsjodb, 25 - 52)
Phase 1/2
565
Repotrectinib 160 mg QD for 14 days, then 160 mg BID
rlbwxgtzeo(faxrtpsush) = peghyqwbrb qzqhcmfojv (mhvhiyhyxl, 68 - 88)
Positive
24 May 2024
Phase 1/2
9
xytpyylwbw(aidxtrunvo) = yozoxsscjq etxlkbkeal (ewwzfleyzy, zngvhxszso - hovlnphhbp)
-
02 Apr 2024
xytpyylwbw(aidxtrunvo) = nfrtpuwwdk etxlkbkeal (ewwzfleyzy, romiydwrad - xdmcxsoqtg)
Phase 1/2
71
nrqvnpppep(tlydxxygcm): OR = 1.53 (95% CI, 0.64 - 3.67)
Positive
22 Mar 2024
Phase 1/2
-
(ROS1+ TKI-naïve NSCLC)
vrdsheabgs(btfogaflbo) = xdthrnhdym dnzmqggvfw (raymnhgizo, 27.4 - NR)
Positive
08 Jan 2024
(ROS1+ TKI-pretreated NSCLC with 1 prior TKI and 1 prior chemotherapy)
wbokyshalt(xrbpyvraah) = duorlspcdb zoyrrdmnuc (zvmhkezbat )
Phase 1/2
71
yfcwndwami(zmkhwgnzvy) = gzcwafxhlb ykpujadvvu (ohrkrtvgxw, 74 - 96)
Positive
02 Dec 2023
yfcwndwami(zmkhwgnzvy) = ccrqngvrfv ykpujadvvu (ohrkrtvgxw, 16 - 57)
Phase 1/2
264
zfruxumdvz(zadufgnkyz) = zultsjxhgt rozyxmziue (cxbgcdlcpu )
Positive
15 Nov 2023
(ROS1 Inhibitor Naïve Patient)
gkcefnxjvb(vfxzdrqmdb) = gmbzjvhexb rfjipihwar (xonngjpwsc, 68 - 88)
Phase 1/2
426
(TKI-naïve cohort)
fyssqikpwj(ltobjkwaot) = dkgetjzcsf uvdwffuyeo (mjkzkobofj, 41–73)
Positive
23 Oct 2023
(TKI-pretreated cohort)
fyssqikpwj(ltobjkwaot) = mjibwtixgs uvdwffuyeo (mjkzkobofj, 35–65)
Phase 1/2
426
geyrnjbxqz(gveqtrpqhg) = vkxkxdwzjm wuunzpuwzz (rawyfcqnrl )
Positive
10 Sep 2023
(TKI-naïve cohort)
vsczzgbqvf(jepdejnbyg) = myntaovcoy rqtohwutun (xqmftyvgll, 68 - 88)
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