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Larotrectinib (LOXO-101), a highly selective TRK inhibitor, is a CNS active small molecule tyrosine kinase inhibitor of the three TRK protein kinases [1-5]. Larotrectinib pharmacokinetics (PK) are conducive to oral dosing and its pharmacokinetics are similar between adult and paediatric patients [5].

Table 3: Pharmacokinetic Profile of Larotrectinib[5]


Value or characteristic

Maximum plasma concentration

1-hour post-dosing


Similar following single or continuous dosing



Mean clearance

98 L/hour

Half life

2.9 hours


58% recovered in faeces and 39% in urine

aMean absolute bioavailability

Larotrectinib has been approved for clinical use by the US Food and Drug Administration (FDA) [5] for the treatment of adult and paediatric patients with solid tumours that [5]:

  • Have an NTRK gene fusion without a known acquired resistance mutation,
  • Are metastatic or in which surgical resection is likely to cause severe morbidity, and
  • Have no satisfactory alternative treatments or that have progressed following treatment.

Larotectinib is the first therapy to receive a tumour-agnostic indication at the time of initial FDA approval in 2018 via a priority review pathway [5].

Larotrectinib is available as oral capsules or in a liquid formulation [5]. The recommended dose is based on body surface area (BSA):

  • 100 mg orally twice daily for adults and children with a BSA ≥1.0 m2.
  • 100 mg/m2 orally twice daily for paediatric patients with BSA <1.0 m2.

In addition, larotrectinib was granted orphan designation for the treatment of salivary gland cancer by the European Medicines Agency (EMA) in March 2018 [6]. A marketing application for larotrectinib was submitted subsequently to the EMA in August 2018 [7].


  1. Burris HA, Shaw AT, Bauer TM et al. Abstract 4529: Pharmacokinetics (PK) of LOXO-101 during the first-in-human Phase I study in patients with advanced solid tumors: Interim update. Cancer Research 2015; 75: 4529.
  2. Drilon A, Laetsch TW, Kummar S et al. Efficacy of Larotrectinib in TRK Fusion-Positive Cancers in Adults and Children. N Engl J Med 2018; 378: 731-739.
  3. Cocco E, Scaltriti M, Drilon A. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol 2018; 15: 731-747.
  4. Laetsch TW, DuBois SG, Nagasubramanian R et al. A pediatric phase I study of larotrectinib, a highly selective inhibitor of the tropomyosin receptor kinase (TRK) family. Journal of Clinical Oncology 2017; 35: 10510-10510.
  5. Loxo Oncology. VITRAKVI® (larotrectinib) [prescribing information]. In. Stamford, CT: Loxo Oncology, Inc. 2018.
  6. European Medicines Agency. EU/3/18/1995. 2018.
  7. Loxo Oncology. Loxo Oncology Announces Submission of European Marketing Authorization Application for Larotrectinib. 2018.

Clinical Data

Larotrectinib efficacy and safety have been evaluated in three clinical trials in patients with cancers with NTRK gene fusion.

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