Synonyms: (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide [3] | example 14 [US8865698 B2] [3] | LOXO-101 | Vitrakvi®
larotrectinib is an approved drug (FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Larotrectinib (LOXO-101) is an orally available, potent and selective inhibitor of the receptor tyrosine kinases of the TRK family [2-3]. In these referenced patents, data is provided for inhibition of neurotrophic tyrosine kinase, receptor, type 1 (NTRK1, a.k.a. TrkA) .
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
No information available. |
Summary of Clinical Use ![]() |
Larotrectinib (LOXO-101) was evaluated in clinical trial in patients with advanced solid tumours with NTRK fusions (NCT02576431). Larotrectinib showed a significant and durable anti-tumour effect in patients with NTRK fusion-positive cancers in Phase 2 trial [1]. Click here to link to ClinicalTrials.gov's full list of larotrectinib trials. In June 2018, the FDA accepted a New Drug Application (NDA) for larotrectinib, and granted priority review. This led to accelerated approval in November 2018 [4]. Under this approval larotrectinib (Vitrakvi) can be used across a range of different tumour types (i.e. which have arisen from different tissues) so long as they harbour NTRK fusions. Suitable patients (adults and paediatric) will have tumours that are metastatic or are unsuitable for surgical resection, and for which there is no satisfactory alternative treatments. In the European Union, the EMA granted orphan drug designation for larotrectinib's use as a treatment for a number of rare cancers: 2016 (soft tissue sarcoma), 2018 (salivary gland cancer, glioma, papillary thyroid cancer). Full EMA approval was granted in September 2019. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT02122913 | A Study to Test the Safety of the Investigational Drug Larotrectinib in Adults That May Treat Cancer | Phase 1 Interventional | Bayer | ||
NCT02576431 | A Study to Test the Effect of the Drug Larotrectinib in Adults and Children With NTRK-fusion Positive Solid Tumors | Phase 2 Interventional | Bayer |