|Other names||LOXO-101, ARRY-470|
|Drug class||Tyrosine kinase inhibitor|
|Side effects||Liver problems, low red blood cells, muscle pain, tiredness, low white blood cells, diarrhea, nausea, fever|
|Typical dose||100 mg BID|
|Chemical and physical data|
|Molar mass||428.444 g·mol−1|
|3D model (JSmol)|
Larotrectinib, sold under the brand name Vitrakvi, is a medication used to treat cancer. Specifically it is used for cases that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion. It is taken by mouth.
Common side effects include liver problems, low red blood cells, muscle pain, tiredness, low white blood cells, diarrhea, nausea, and fever. Other side effects may include numbness, tremor, and delirium. Use in pregnancy may harm the baby. It is a tyrosine kinase inhibitor of TrkA, TrkB, and TrkC.
Larotrectinib was approved for medical use in the United States in 2018, Europe in 2019, and Australia in 2020. In the United Kingdom it costs the NHS about £15,000 a month as of 2021. In the United States this amount is about 34,000 USD.
In two thirds of people it decreased the size of their cancer to less than half.
It is generally taken at a dose of 100 mg twice per day.
It was discovered by Array BioPharma and licensed to Loxo Oncology in 2013. Larotrectinib was initially awarded orphan drug status in 2015, for soft tissue sarcoma, and breakthrough therapy designation in 2016 for the treatment of metastatic solid tumors with NTRK fusion. Some clinical trial results were announced in 2017.
Larotrectinib was the first drug to be specifically developed and approved to treat any cancer containing certain mutations, as opposed to cancers of specific tissues (i.e., the approval is "tissue agnostic"). Several earlier drugs, including pembrolizumab, were eventually approved by the FDA for treatment of specific mutations independent of the type of cancer, but those drugs had been initially developed for specific cancer types. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.
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