Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Entrectinib
Drug ID BADD_D02553
Description Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor.[L8081] It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors.[L8207] Entrectinib's approved use is meant as a last line of therapy due to its accelerated approval based on early trial data. This therapy offers benefit over similar ALK inhibitors such as [alectinib], [ceritinib], and [lorlatinib] due to a wider range of targets.[A183929]
Indications and Usage Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults.[L8081] Entrectinib is also indicated in adults and children over 12 years old for the treatment of NTRK gene fusion-positive solid tumors which have metastasized or for which surgical resection is likely to result in severe morbidity and for which has progressed on previous therapies or for which no comparable alternative therapies are available.
Marketing Status approved; investigational
ATC Code L01EX14
DrugBank ID DB11986
KEGG ID D10926
MeSH ID C000607349
PubChem ID 25141092
TTD Drug ID D0O0LS
NDC Product Code 11014-0563; 50242-094; 11014-0551; 11014-0562; 50242-091; 11014-0550
UNII L5ORF0AN1I
Synonyms entrectinib | N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide | Rozlytrek | RXDX-101 | NMS-E628
Chemical Information
Molecular Formula C31H34F2N6O2
CAS Registry Number 1108743-60-7
SMILES CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
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)
Hypoaesthesia17.02.06.023; 23.03.03.0810.000358%Not Available
Hypotension24.06.03.0020.000224%
Interstitial lung disease22.01.02.003; 10.02.01.0330.000504%Not Available
Liver disorder09.01.08.0010.000112%Not Available
Loss of consciousness17.02.04.0040.000112%Not Available
Memory impairment19.20.01.003; 17.03.02.0030.000470%
Mental impairment19.21.02.003; 17.03.03.0020.000112%Not Available
Metastases to liver16.22.02.001; 09.04.02.0040.000112%Not Available
Muscular weakness17.05.03.005; 15.05.06.0010.000224%
Myocardial infarction24.04.04.009; 02.02.02.0070.000168%
Myocarditis02.04.03.0010.000280%
Neuropathy peripheral17.09.03.0030.000437%Not Available
Oedema14.05.06.010; 08.01.07.0060.000336%Not Available
Oedema peripheral14.05.06.011; 08.01.07.007; 02.05.04.0070.000582%
Pain of skin23.03.03.0030.000302%
Pericardial effusion02.06.01.0020.000168%
Pleural effusion22.05.02.0020.000224%
Pneumonitis22.01.01.0060.000302%
Pulmonary embolism24.01.06.001; 22.06.02.0010.000112%Not Available
Pulmonary hypertension24.08.03.002; 22.06.01.0010.000112%
Pyrexia08.05.02.0030.000560%
Rash23.03.13.0010.000963%Not Available
Renal disorder20.01.02.0020.000560%Not Available
Renal failure20.01.03.0050.000112%Not Available
Seizure17.12.03.0010.000224%
Shock24.06.02.0020.000112%Not Available
Syncope17.02.04.008; 02.11.04.015; 24.06.02.0120.000280%
Tremor17.01.06.0020.000246%
Urinary incontinence20.02.02.010; 17.05.01.0080.000112%
Urinary retention20.02.02.0110.000224%
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