osimertinib (Tagrisso)
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Indications
- treatment of advanced EGFR-mutant non-small cell lung cancer (NSCLC) possibly including brain metastasis[6]
Contraindications
Dosage
Tablet: 40 mg, 80 mg PO
Pharmacokinetics
- crosses blood-brain barrier
Adverse effects
- most common
- other
- inflammation of the lungs
- injury to the heart
- may harm a developing fetus
- drug adverse effects of tyrosine kinase inhibitor(s)
- drug adverse effects of EGF receptor inhibitors
Mechanism of action
- blocks activity of EGFR
Complications
- loss of EGFR T790M associated with acquired resistance to osimertinib
More general terms
References
- ↑ Greig SL Osimertinib: First Global Approval. Drugs. 2016 Feb;76(2):263-73 PMID: https://www.ncbi.nlm.nih.gov/pubmed/26729184
- ↑ FDA News Release. November 13, 2015 FDA approves new pill to treat certain patients with non-Small-Cell Lung Cancer. small cell lung cancer. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm472525.htm
- ↑ 3.0 3.1 Soria JC, Ohe Y, Vansteenkiste J et al Osimertinib in Untreated EGFR-Mutated Advanced non-Small-Cell Lung Cancer. N Engl J Med. 2018;378:113-125. Online: Nov 18, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29151359 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1713137
- ↑ Oxnard GR, Hu Y, Mileham KF et al Assessment of Resistance Mechanisms and Clinical Implications in Patients With EGFR T790M-Positive Lung Cancer and Acquired Resistance to Osimertinib. JAMA Oncol. Published online August 2, 2018 PMID: https://www.ncbi.nlm.nih.gov/pubmed/30073261 https://jamanetwork.com/journals/jamaoncology/fullarticle/2694879
- ↑ Ramalingam SS, Vansteenkiste J, Planchard Det al Overall Survival with Osimertinib in Untreated, EGFR-Mutated Advanced NSCLC. N Engl J Med 2020; 382:41-50. Jan 2. PMID: https://www.ncbi.nlm.nih.gov/pubmed/31751012 https://www.nejm.org/doi/full/10.1056/NEJMoa1913662?
- ↑ 6.0 6.1 Erickson AW, Brastianos PK, Das S Assessment of Effectiveness and Safety of Osimertinib for Patients With Intracranial Metastatic DiseaseA Systematic Review and Meta-analysis. JAMA Netw Open. 2020;3(3):e201617 PMID: https://www.ncbi.nlm.nih.gov/pubmed/32211870 Free PMC Article https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2763239