Drug Type Small molecule drug |
Synonyms Repotrectinib (USAN), Ropotrectinib, 洛普替尼 + [13] |
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) |
Therapeutic Areas |
Originator Organization |
Active Organization |
Inactive Organization |
Drug Highest PhaseApproved |
First Approval Date United States (15 Nov 2023), |
RegulationPriority Review (United States), Breakthrough Therapy (United States), Fast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Orphan Drug (Japan), Orphan Drug (South Korea), Conditional marketing approval (China) |
Molecular FormulaC18H18FN5O2 |
InChIKeyFIKPXCOQUIZNHB-UHFFFAOYSA-N |
CAS Registry1802220-02-5 |
| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| 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 |
| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| HR Positive/HER2 Negative Lobular Carcinoma | Phase 2 | United States | 08 Aug 2024 | |
| KRAS G12D mutation Solid Tumors | Phase 2 | United States | 23 Sep 2021 | |
| KRAS mutation-related tumors | Phase 2 | United States | 23 Sep 2021 | |
| Meningeal Carcinomatosis | Phase 2 | United States | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | China | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | Japan | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | Australia | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | Belgium | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | Canada | 18 May 2021 | |
| Meningeal Carcinomatosis | Phase 2 | Denmark | 18 May 2021 |
Not Applicable | Glioblastoma NOS1AP-NTRK1 fusion-positive | 1 | uxwugxblkz(ppkxwzhzil) = bjwnshkahy thqooekjds (nqqiofvets ) | Positive | 24 Sep 2026 | ||
uxwugxblkz(ppkxwzhzil) = cdysavivhk thqooekjds (nqqiofvets ) | |||||||
Phase 2 | HR Positive/HER2 Negative Lobular Carcinoma HR+ | HER2- | 6 | oymlepfhrv(juyuwxkvzu) = dbvyfnemoj ftpnixvoaj (ufxptlsrvo ) View more | Negative | 07 May 2026 | ||
Phase 2 | ROS1 fusion positive Neoplasms ROS1 rearrangement | 30 | ffxrwxrdgw(gtrfhelxwt) = neutropenia (42.9%) and hypertension (17.6%) adnvwneeij (afosqxzeby ) | Positive | 17 Oct 2025 | ||
Phase 2 | 172 | (TKI-naïve) | tyzbbgcojk(ibykuuvdfi) = fzkockwiiz dxzoscaypj (mogxxmmnuy ) View more | Positive | 17 Oct 2025 | ||
(TKI-pretreated) | tyzbbgcojk(ibykuuvdfi) = lhgxzhcdbf dxzoscaypj (mogxxmmnuy, 7.4 - 13.0) View more | ||||||
Phase 1/2 | 502 | (TKI-naïve cohort) | kogrpesmns(ucwnunubpx) = kspnsslowl grssucmpbx (mqbewavwjl, 68 - 88) View more | Positive | 09 Sep 2025 | ||
(1 prior TKI and no chemo cohort) | kogrpesmns(ucwnunubpx) = drdgjkrgcd grssucmpbx (mqbewavwjl, 28 - 55) View more | ||||||
Phase 2 | 58 | bvlpngvhev(xavkheylrr) = <10% sxxzfqipej (arfbqfzzyw ) View more | Positive | 29 Apr 2025 | |||
Phase 1/2 | 127 | (ROS1 Inhibitor Naïve Patients) | pqplhkfsrz(mrrxgeycza) = jeydsagovj gzndvnosfq (omqpnjtzaa, 68 - 88) View more | Positive | 13 Jun 2024 | ||
(ROS1 Inhibitor Pretreated Patients) | pqplhkfsrz(mrrxgeycza) = rmsjjekndx gzndvnosfq (omqpnjtzaa, 25 - 52) View more | ||||||
Phase 1/2 | NTRK fusion-positive solid tumors NTRK gene fusion-positive | 88 | (TKI-Naïve Patients) | yovinqdzhj(utvfhigysc) = jkcsuxjhbb ewfkmnxwmr (vxoqbhinpy, 41 - 73) View more | Positive | 13 Jun 2024 | |
(TKI-Pretreated Patients) | yovinqdzhj(utvfhigysc) = dfjjjzmlns ewfkmnxwmr (vxoqbhinpy, 35 - 65) View more | ||||||
Phase 1/2 | 565 | Repotrectinib 160 mg QD for 14 days, then 160 mg BID | vaurhtozgc(mvoaqscavo) = aezfkzacuj uymuxnjsia (cywhkpbhmw, 68 - 88) View more | Positive | 24 May 2024 | ||
Phase 1/2 | 9 | (Dose Level 1) | imborgqzqa = hgloxyuhdj mwnvinvxbb (rwwllzljro, kwxiyrvxft - ofiipggwcz) View more | - | 02 Apr 2024 | ||
(Dose Level 2) | imborgqzqa = lrjxmjnxrm mwnvinvxbb (rwwllzljro, scqzqzhbyx - aygkcsftxf) View more |





