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)
Pulmonary oedema02.05.02.003; 22.01.03.0030.000728%
Purpura01.01.04.003; 23.06.01.004; 24.07.06.0050.000392%
Pyrexia08.05.02.0030.004466%
Rash23.03.13.0010.011741%-
Rash erythematous23.03.13.0290.000795%-
Rash maculo-papular23.03.13.0040.000795%
Renal failure20.01.03.005---
Respiratory disorder22.02.07.002---
Respiratory failure14.01.04.003; 22.02.06.0020.002071%
Retinal artery occlusion06.10.01.005; 24.01.07.0030.000112%-
Retinal detachment06.09.03.003; 12.01.04.0040.000280%
Rhabdomyolysis15.05.05.0020.000728%
Right ventricular failure02.05.03.0020.000168%-
Skin disorder23.03.03.0070.002888%-
Skin fissures23.03.03.0080.000851%-
Skin lesion23.03.03.0100.000548%-
Skin reaction10.01.03.019; 23.03.03.0130.000168%-
Skin ulcer23.07.03.003; 24.04.03.0070.000862%
Small cell lung cancer16.19.08.003; 22.08.01.0130.000951%-
Squamous cell carcinoma16.16.01.0020.000224%-
Stevens-Johnson syndrome10.01.01.045; 11.07.01.005; 12.03.01.014; 23.03.01.0070.000448%
Stomatitis07.05.06.0050.006548%
Sudden death02.03.04.013; 08.04.01.0030.000280%
Supraventricular extrasystoles02.03.03.0110.000168%-
Supraventricular tachycardia02.03.03.0120.000280%
Thrombocytopenia01.08.01.0020.004421%-
Thrombophlebitis24.01.02.0010.000112%-
Toxic epidermal necrolysis10.01.01.006; 11.07.01.006; 12.03.01.015; 23.03.01.0080.000448%
Tumour flare16.32.03.0010.000168%-
Tumour lysis syndrome14.05.01.004; 16.32.03.0020.000112%
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