| Drug Name |
Larotrectinib |
| Drug ID |
BADD_D02526 |
| Description |
Larotrectinib is an orally administered tropomyosin receptor kinase (Trk) inhibitor with demonstrated antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
Originally discovered by Array BioPharma, the agent was ultimately licensed to Loxo Oncology in 2013. Larotrectinib is another example of innovative new cancer therapy medications that target key, specific genetic biomarker drivers of cancer rather than particular types of tumors [L4847]. |
| Indications and Usage |
Larotrectinib is a tyrosine kinase inhibitor that is currently indicated for the treatment of adult and pediatric patients with solid tumors that either a) have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, b) are metastatic or where surgical resection is likely to result in severe morbidity, and c) have no satisfactory alternative treatments or that have progressed following treatment [FDA Label].
At the moment, these uses of larotrectinib are only approved under the auspices of an accelerated approval by the US FDA based on overall response rate and duration of response and continuation of support for these indications may be contingent upon the verification and description of continued clinical benefit in confirmatory trials [FDA Label]. |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EX12 |
| DrugBank ID |
DB14723
|
| KEGG ID |
D11137
|
| MeSH ID |
C000609083
|
| PubChem ID |
46188928
|
| TTD Drug ID |
D07TOK
|
| NDC Product Code |
63069-390; 50419-392; 71777-390; 71777-391; 50419-390; 71777-392; 50419-391; 50419-393 |
| UNII |
PF9462I9HX
|
| Synonyms |
larotrectinib | (3S)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide | N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide | BAY-2757556 | BAY2757556 | LOXO-101 | LOXO101 | ARRY-470 | ARRY470 | Vitrakvi |
