Adverse Drug Reaction Classification System

Pharmaceutical Information
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
Chemical Information
Molecular Formula C21H22F2N6O2
CAS Registry Number 1223403-58-4
SMILES C1CC(N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CCC(C4)O)C5=C(C=CC(=C5)F)F
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal distension07.01.04.0010.000437%
Abdominal pain07.01.05.0020.000224%
Abdominal pain upper07.01.05.0030.000548%
Adenocarcinoma16.16.01.0040.000112%Not Available
Amnesia19.20.01.001; 17.03.02.0010.000246%
Anaemia01.03.02.0010.000548%
Arthralgia15.01.02.0010.000470%
Astrocytoma17.20.01.002; 16.30.01.0020.000112%Not Available
Breast cancer21.05.01.003; 16.10.01.0010.000112%Not Available
Burning sensation17.02.06.001; 08.01.09.0290.000112%Not Available
Chest discomfort02.02.02.009; 22.12.02.002; 08.01.08.0190.000112%Not Available
Confusional state19.13.01.001; 17.02.03.0050.000302%
Constipation07.02.02.0010.000851%
Coordination abnormal17.02.02.0040.000112%Not Available
Cough22.02.03.0010.000627%
Dizziness02.11.04.006; 24.06.02.007; 17.02.05.0030.002250%
Drug ineffective08.06.01.0060.002541%Not Available
Dyspepsia07.01.02.0010.000246%
Dysphagia07.01.06.0030.000246%
Dyspnoea22.02.01.004; 02.11.05.0030.000772%
Fatigue08.01.01.0020.001892%
Feeling abnormal08.01.09.0140.000358%Not Available
Fluid retention20.01.02.003; 14.05.06.0020.000112%Not Available
Gait disturbance15.03.05.013; 17.02.05.016; 08.01.02.0020.000168%
Gastrointestinal disorder07.11.01.0010.000246%Not Available
Gastrointestinal haemorrhage24.07.02.009; 07.12.02.0010.000168%Not Available
Glioblastoma17.20.02.002; 16.30.02.0020.000280%Not Available
Glioblastoma multiforme17.20.02.001; 16.30.02.0010.000168%Not Available
Glioma17.20.01.004; 16.30.01.0040.000168%Not Available
Haematochezia24.07.02.012; 07.12.02.0030.000246%Not Available
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