Efficacy and safety of larotrectinib in patients with NTRK fusion-positive lung cancer

On March 24, 2022, the journal Targeted Oncology reported the efficacy and safety of larotrectinib in patients with NTRK fusion-positive lung cancer.

TRK, tropomyosin receptor kinase, is an important signaling pathway regulating cell communication and tumor growth, and NTRK is the gene encoding TRK. In rare cases, the NTRK gene is fused with other genes, causing the TRK signaling pathway to become uncontrolled, thereby promoting tumor growth. NTRK gene fusions are structurally active in a variety of adult and pediatric solid tumors and serve as oncogenic drivers. The incidence in non-small cell lung cancer is estimated to be 0.1~1.0%.

Previously, on November 26, 2018, the US FDA approved larotrectinib for adult and pediatric patients with solid tumors fused to NTRK genes (including NTRK1, NTRK2, and NTRK3). This is the the world’s first “broad-spectrum” anticancer drug that has been approved for marketing regardless of tumor type. In June 2019, larotrectinib was listed in Hong Kong, China.

Larotrectinib is a highly potent, highly selective, and central nervous system (CNS) active, European Medicines Agency (EMA) and FDA-approved TRK inhibitor.

Legend: Bengal Everest version larottinib 100mg

Brand name: VITRAKVI p>

Generic name: Larotrectinib (larotrectinib)

Target: NTRK

First U.S. Approval: November 2018

Hong Kong Listing:June 2019

Specifications:25mg/100mg (capsule), 20mg/ml (oral solution)

Approved indications: NTRK gene fusion solid tumors

Recommended dose:

For adult or pediatric patients with a body surface area greater than 1㎡, the recommended dose is 100 mg each time, twice a day, with or without food;

p>

For pediatric patients with body surface area less than 1㎡, the recommended dose is 100 mg/㎡ (calculated based on body surface area) twice a day, with or without food.

Storage conditions: Room temperature 20℃-25℃

Clinical data

Supporting data from Phase I and Phase II trials, mainly To analyze the effect of larotrectinib in adult patients with NTRK gene fusions.

All enrolled patients received larotrectinib 100 mg twice daily for 28 consecutive days. Treatment was allowed beyond the advanced stage if the patient continued to benefit.

Legend: Larotrectinib 25mg, Everest, Bangladesh

A total of 20 patients with lung cancer with NTRK fusion were included in the two trials. Median age was 48.5 years; 90% of patients had an ECOG score of 0 or 1; 50% were female; 95% had adenocarcinoma histology and 5% had neuroendocrine carcinoma. Most patients (n=16) had NTRK1 gene fusions, and the remaining 4 had NTRK3 gene fusions. The median number of previous treatments was 3.

The primary endpoint of the trial was objective response rate (ORR), and secondary endpoints were duration of response (DOR), progression-free survival (PFS) ) and overall survival (OS).

As of July 20, 2020, the objective response rate (ORR) of 15 evaluable patients was 73%. Complete remission (CR) was achieved in 1 (7%) patient, partial response (PR) in 10 (67%) patients, stable disease (SD) in 3 (20%) patients, and in 1 (7%) patient Progression (PD).

At a median follow-up of 17.4 months, the median duration of response (DOR) was 33.9 months; at a median follow-up of 16.6 months, the median no Progression survival (PFS) was 35.4 months; median follow-up time was 16.2 months, and overall survival (OS) was 40.7 months.

In 8 patients with CNS metastases at baseline, the ORR was 63%.

Adverse Reactions

In terms of safety, 16 patients (80%) reported treatment-related adverse events (TRAEs). Most adverse reactions were grade 1 or 2, and the most common adverse reactions were myalgia (50%), constipation (40%), cough strong> (40%) and dizziness (40%).

8 patients experienced grade 3 TRAE. One patient experienced sudden cardiac arrest, which the investigators determined was not related to larotrectinib treatment.

Conclusion

The results of these two trials suggest that larotrectinib has durable responses, survival benefit, and favorable safety profile in patients with advanced lung cancer harboring NTRK gene fusions . Therefore, routine detection of NTRK fusions in lung cancer patients is necessary.

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