Adverse Drug Reaction Classification System

         

Pharmaceutical Information
Drug Name Osimertinib
Drug ID BADD_D01629
Description Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy. Development of third-generation EGFR-TKIs, such as osimertinib, has been in response to altered tumour resistance patterns following treatment and toxic side effects that impact patient quality of life. Treatment with first-generation EGFR-TKIs (gefitinib and erlotinib) has been associated with the development of resistance through activating mutations in the EGFR gene. Second-generation EGFR-TKIs (afatinib and dacomitinib) were then developed to be more potent inhibitors, although their use is associated with increased toxicity through nonspecific targeting of wild-type EGFR. In contrast, third-generation inhibitors are specific for the gate-keeper T790M mutations which increases ATP binding activity to EGFR and result in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.
Indications and Usage Osimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.
Marketing Status approved
ATC Code L01EB04
DrugBank ID DB09330
KEGG ID D10766
MeSH ID C000596361
PubChem ID 71496458
TTD Drug ID D0O8GK
NDC Product Code 0310-1353; 0310-1350; 0310-1354; 54864-844; 17228-1349; 17228-1350; 0310-1349
UNII 3C06JJ0Z2O
Synonyms osimertinib | Tagrisso | AZD9291
Chemical Information
Molecular Formula C28H33N7O2
CAS Registry Number 1421373-65-0
SMILES CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
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)
Metastasis16.22.01.0010.000951%Not Available
Renal impairment20.01.03.0100.001981%Not Available
Malignant transformation16.16.01.0130.001511%Not Available
Bone marrow failure01.03.03.0050.001007%
Cytopenia01.03.03.0120.000358%Not Available
Liver injury12.01.17.012; 09.01.07.0220.000504%Not Available
Organising pneumonia22.01.02.0080.000168%Not Available
Tumour compression16.32.03.0210.000112%Not Available
Oropharyngeal pain22.12.03.016; 07.05.05.004--
Drug-induced liver injury12.03.01.044; 09.01.07.0230.001119%Not Available
Cornea verticillata06.06.03.0160.000381%Not Available
Cholangitis acute09.02.01.0060.000112%Not Available
Chronic gastritis10.04.04.011; 07.08.02.005; 11.07.01.0160.000168%Not Available
Drowning12.01.18.003; 08.04.01.0140.000112%Not Available
Lung carcinoma cell type unspecified stage IV22.08.01.019; 16.19.02.0060.000112%Not Available
Lymphadenopathy mediastinal22.09.03.006; 01.09.01.0250.000224%Not Available
Malignant ascites16.32.03.013; 07.07.01.0040.000112%Not Available
Malignant pleural effusion22.05.04.001; 16.32.03.0140.000504%Not Available
Metastases to adrenals16.22.02.012; 05.01.04.0070.000448%Not Available
Metastases to bone16.22.02.005; 15.09.03.0060.002295%Not Available
Metastases to kidney16.22.02.017; 20.01.04.0100.000112%Not Available
Metastases to lymph nodes16.22.02.006; 01.09.01.0150.000672%Not Available
Metastases to pleura22.05.04.002; 16.22.02.0220.000224%Not Available
Metastases to the mediastinum22.09.03.009; 16.22.02.0270.000112%Not Available
Pulmonary artery thrombosis24.01.06.005; 22.06.02.0050.000168%Not Available
Pericardial effusion malignant16.32.03.026; 02.06.01.0090.000168%Not Available
Mechanical ileus07.13.01.0140.000112%Not Available
Metastases to thorax22.08.03.001; 16.22.02.0280.000112%Not Available
Metastases to meninges17.02.10.012; 16.22.02.0030.003470%Not Available
Lymphangiosis carcinomatosa24.09.02.007; 16.22.02.009; 01.09.01.0270.000839%Not Available
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