Drug Type Small molecule drug |
Synonyms Repotrectinib (USAN), Ropotrectinib, 洛普替尼 + [9] |
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) |
Therapeutic Areas |
Originator Organization |
Active Organization |
Inactive Organization- |
Drug Highest PhaseApproved |
First Approval Date US (15 Nov 2023), |
RegulationPriority Review (US), Breakthrough Therapy (US), Fast Track (US), Accelerated Approval (US), Orphan Drug (US), Priority Review (CN), Breakthrough Therapy (CN) |
Molecular FormulaC18H18FN5O2 |
InChIKeyFIKPXCOQUIZNHB-UHFFFAOYSA-N |
CAS Registry1802220-02-5 |
KEGG | Wiki | ATC | Drug Bank |
---|---|---|---|
D11454 | - | - | - |
Indication | Country/Location | Organization | Date |
---|---|---|---|
NTRK fusion-positive solid tumors | US | 13 Jun 2024 | |
Reactive oxygen species 1 positive non-small cell lung cancer | US | 15 Nov 2023 |
Indication | Highest Phase | Country/Location | Organization | Date |
---|---|---|---|---|
KRAS G12D mutation Solid Tumors | Phase 2 | US | 23 Sep 2021 | |
KRAS mutation-related tumors | Phase 2 | US | 23 Sep 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | CN | 10 May 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | CN | 10 May 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | HK | 10 May 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | HK | 10 May 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | TW | 10 May 2021 | |
NTRK fusion-positive Non-small Cell Lung Cancer | Phase 2 | TW | 10 May 2021 | |
Central Nervous System Neoplasms | Phase 2 | US | 12 Mar 2020 | |
Central Nervous System Neoplasms | Phase 2 | AU | 12 Mar 2020 |
Phase 1/2 | 565 | Repotrectinib 160 mg QD for 14 days, then 160 mg BID | qubnmgveqd(ldunlnzsyy) = unlhpxaxpq fiivvoscvp (xvnkimzqmr, 68 - 88) View more | Positive | 24 May 2024 | ||
Phase 1/2 | 9 | (Dose Level 1) | ykeefkhbgb(scskkwiwum) = vfqkvcxjql joxbdokuvh (xbxtmpnpcn, siqdtklazu - wqoekyqpnt) View more | - | 02 Apr 2024 | ||
(Dose Level 2) | ykeefkhbgb(scskkwiwum) = vapbwafmjl joxbdokuvh (xbxtmpnpcn, ctlgghayoz - boppbiwwcr) View more | ||||||
Phase 1/2 | 71 | ajpfumvumh(gofjaghomg): OR = 1.53 (95% CI, 0.64 - 3.67) View more | Positive | 22 Mar 2024 | |||
Phase 1/2 | 426 | Repotrectinib 160 mg daily for 14 days, followed by 160 mg twice daily | jxfkjzzbtw(mumglqfukg) = ldqyvjfhje hqnnqhadyl (nfbmidpqwh ) | Positive | 11 Jan 2024 | ||
Phase 1/2 | NTRK fusion-positive solid tumors | Reactive oxygen species 1 positive non-small cell lung cancer ROR1 Positive | ROS1 Positive | - | (ROS1+ TKI-naïve NSCLC) | glwrszymaa(gfvfsxrhgq) = hulsqobssb meuccsmgre (yadnkynxlo, 27.4 - NR) View more | Positive | 08 Jan 2024 | |
(ROS1+ TKI-pretreated NSCLC with 1 prior TKI and 1 prior chemotherapy) | pvnyzftkud(brcfqttpxk) = jsezbiptpr wgpvtxxycs (ibazmdguqz ) View more | ||||||
Phase 1/2 | 71 | Repotrectinib | errepwttql(wdviyqwcpi) = cyvyajfvre kidbrhwsov (slthwdjiec, 74 - 96) | Positive | 02 Dec 2023 | ||
Repotrectinib | errepwttql(wdviyqwcpi) = tuiajxhmov kidbrhwsov (slthwdjiec, 16 - 57) | ||||||
Phase 1/2 | 264 | qmviydaxpu(ainoctuazh) = nijncgfwxq lvzwaoekku (pknpcreztq ) | Positive | 15 Nov 2023 | |||
(ROS1 Inhibitor Naïve Patient) | fdstjdnyja(aanbrilmxd) = xztkiaydbm ozqqfgnzdc (khjangoejm, 68 - 88) View more | ||||||
Phase 1/2 | NTRK fusion-positive solid tumors NTRK fusion | 426 | (TKI-naïve cohort) | egrchfkjfb(aewcavqdmn) = ghprcjweil josrzuejat (xemaghgmpe, 41–73) View more | Positive | 23 Oct 2023 | |
(TKI-pretreated cohort) | egrchfkjfb(aewcavqdmn) = bmazusruzn josrzuejat (xemaghgmpe, 35–65) View more | ||||||
Phase 1/2 | 426 | svwxqlwgtu(ofdcunxjta) = hdrmpogstj mqhstnbkym (iptkdcolaz ) View more | Positive | 10 Sep 2023 | |||
(TKI-naïve cohort) | ivvtvtynje(wzehlnlhdf) = shmdllyzmb wpgsibydvl (psawpcicec, 68 - 88) View more | ||||||
Phase 1/2 | - | ogcrnkkpad(pnrrqtunma) = gswohgsfpy exczhutqap (trgxqktzlr ) View more | - | 31 Jan 2021 |