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osimertinib (Tagrisso)

Indications: - treatment of advanced EGFR-mutant non-small cell lung cancer (NSCLC) possibly including brain metastasis [6] Contraindications: - pregnancy Dosage: - 80 mg QD (NSCLC) [3] Tablet: 40 mg, 80 mg PO Pharmacokinetics: - crosses blood-brain barrier Adverse effects: - most common - diarrhea - xeroderma, rash ,paronychia - other - inflammation of the lungs - injury to the heart - may harm a developing fetus Complications: - loss of EGFR T790M associated with acquired resistance to osimertinib Mechanism of action: - blocks activity of EGFR

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

small inhibitory antineoplastic agent (ib drug) EGF receptor (EGFR) inhibitor

References

  1. Greig SL Osimertinib: First Global Approval. Drugs. 2016 Feb;76(2):263-73 PMID: 26729184
  2. 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. 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 PMID: 29151359 http://www.nejm.org/doi/full/10.1056/NEJMoa1713137
  4. 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: 30073261 https://jamanetwork.com/journals/jamaoncology/fullarticle/2694879
  5. 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: 31751012 https://www.nejm.org/doi/full/10.1056/NEJMoa1913662?
  6. 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: 32211870 Free PMC Article https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2763239