Osimertinib

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at approximately 9-fold lower concentrations than wild-type. Two pharmacologically-active metabolites (AZ7550 and AZ5104 circulating at approximately 10% of the parent) with similar inhibitory profiles to osimertinib have been identified in the plasma after oral administration of osimertinib.

• TAGRISSO is a kinase inhibitor indicated for: • adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. ( 1.1 , 2.2 ) • the treatment of adult patients with locally advanced, unresectable (stage III) NSCLC whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.ICD-10: C34.90

• None. None.contraindicated

Adjuvant treatment of early-stage NSCLC: 80 mg orally once daily, with or without food, until disease recurrence, or unacceptable toxicity, or for up to 3 years. ( 2.3 ) Locally advanced, unresectable (stage III) NSCLC: Following platinum-based chemoradiation therapy, 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. ( 2.3 ) Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. ( 2.3 ) Locally advanced or metastatic NSCLC: 80 mg orally once daily administered in combination with pemetrexed and platinum-based chemotherapy, with or without food, until disease progression or unacceptable toxicity due to TAGRISSO. ( 2.3 ) 2.1 Recommended Evaluation and Testing Before Initiating TAGRISSO TAGRISSO Monotherapy • Before initiating TAGRISSO monotherapy in patients with cardiac risk factors, conduct cardiac monitoring, including assessment of left ventricular ejection fraction (LVEF) [see Warnings and Precautions (5.3) ] . • Before initiating TAGRISSO, perform complete blood count with differential [see Warnings and Precautions (5.7) ] . TAGRISSO in Combination with Pemetrexed and Platinum-based Chemotherapy • Before initiating TAGRISSO in combination with pemetrexed and platinum-based chemotherapy, conduct cardiac monitoring in all patients, including assessment of left ventricular ejection fraction (LVEF) [see Warnings and Precautions (5.3) ] . • Before initiating TAGRISSO, perform complete blood count with differential [see Warnings and Precautions (5.7) ] .

• Interstitial Lung Disease (ILD)/Pneumonitis : Monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. For patients receiving TAGRISSO who have not received recent definite platinum-based chemoradiation therapy, permanently discontinue TAGRISSO in patients diagnosed with ILD/Pneumonitis. For patients who received recent definitive platinum-based chemoradiation therapy with Grade 1 ILD/pneumonitis continue TAGRISSO or interrupt and restart, as appropriate. Permanently discontinue TAGRISSO in patients diagnosed with Grade ≥2 ILD/pneumonitis. ( 2.5 , 5.1 ) • QTc Interval Prolongation : Monitor electrocardiograms and electrolytes in patients who have a history or predisposition for QTc prolongation, or those who are taking medications that are known to prolong the QTc interval. Withhold, then restart at a reduced dose or permanently discontinue TAGRISSO based on severity. ( 2.5 , 5.2 ) • Cardiomyopathy : Occurred in 3.8% of patients. Conduct cardiac monitoring, including left ventricular ejection fraction (LVEF) assessment in patients with cardiac risk factors. ( 2.5 , 5.3 ) • Keratitis : Promptly refer patients with signs and symptoms of keratitis to an ophthalmologist for evaluation. ( 5.4 ) • Erythema Multiforme Major, Stevens-Johnson Syndrome, and Toxic Epidermal Necrolysis : Withhold TAGRISSO if erythema multiforme major (EMM), Stevens-Johnson syndrome (SJS), or toxic epidermal necrolysis (TEN) is suspected and permanently discontinue if confirmed.

The following adverse reactions are discussed in greater detail in other sections of the labeling: • Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.1 )] • QTc Interval Prolongation [see Warnings and Precautions (5.2) ] • Cardiomyopathy [see Warnings and Precautions (5.3) ] • Keratitis [see Warnings and Precautions (5.4) ] • Erythema multiforme, Stevens-Johnson syndrome, and Toxic epidermal necrolysis [see Warnings and Precautions (5.5) ] • Cutaneous Vasculitis [see Warnings and Precautions (5.6) ] • Aplastic Anemia [see Warnings and Precautions (5.7) ] Most common (≥20%) adverse reactions, including laboratory abnormalities, were: • TAGRISSO monotherapy: leukopenia, lymphopenia, thrombocytopenia, anemia, diarrhea, rash, musculoskeletal pain, neutropenia, nail toxicity, dry skin, stomatitis, and fatigue. ( 6.1 ) • TAGRISSO monotherapy following platinum-based chemoradiation therapy: lymphopenia, leukopenia, ILD/pneumonitis, thrombocytopenia, neutropenia, rash, diarrhea, nail toxicity, musculoskeletal pain, cough and COVID-19. ( 6.1 ) • TAGRISSO in combination with pemetrexed and platinum-based chemotherapy: leukopenia, thrombocytopenia, neutropenia, lymphopenia, rash, diarrhea, stomatitis, nail toxicity, dry skin, and increased blood creatinine. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AstraZeneca at 1-800-236-9933 or www.TAGRISSO.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Lactation: Do not breastfeed. (8.2 ) 8.1 Pregnancy Risk Summary Based on data from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , TAGRISSO can cause fetal harm when administered to a pregnant woman. There are no available data on TAGRISSO use in pregnant women. Administration of osimertinib to pregnant rats was associated with embryolethality and reduced fetal growth at plasma exposures 1.5 times the exposure at the recommended clinical dose (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data When administered to pregnant rats prior to embryonic implantation through the end of organogenesis (gestation days 2-20) at a dose of 20 mg/kg/day, which produced plasma exposures of approximately 1.5 times the clinical exposure, osimertinib caused post-implantation loss and early embryonic death.

Metabolism

The area under the plasma concentration-time curve (AUC) and maximal plasma concentration (C max ) of osimertinib increased dose proportionally over 20 to 240 mg dose range (i.e., 0.25 to 3 times the recommended dosage) after oral administration and exhibited linear pharmacokinetics (PK). Administration of TAGRISSO orally once daily resulted in approximately 3-fold accumulation with steady-state exposures achieved after 15 days of dosing.

• Nov 13, 2015NDANDA208065Astrazeneca

1. 1Death11,12036%
2. 2Malignant Neoplasm Progression3,14210%
3. 3Diarrhoea1,5935.2%
4. 4Drug Resistance1,0823.6%
5. 5Fatigue9683.2%
6. 6Rash8842.9%
7. 7Off Label Use7572.5%
8. 8Decreased Appetite7562.5%
9. 9Drug Ineffective7172.4%
10. 10Dyspnoea7122.3%
11. 11Disease Progression7112.3%
12. 12Nausea6802.2%
13. 13Metastases To Central Nervous System6422.1%
14. 14Asthenia5851.9%
15. 15Interstitial Lung Disease5791.9%

The 10 most recently updated of 378 ClinicalTrials.gov registrations naming Osimertinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Phase 2 Study of Poziotinib in Participants With NSCLC Having EGFR or HER2 Exon 20 Insertion Mutation
  Terminated · Phase 2 · Interventional · 648 enrolled · Spectrum Pharmaceuticals, Inc
  NCT03318939updated 2026-06-12
• Osimertinib With or Without Bevacizumab as Initial Treatment for Patients With EGFR-Mutant Lung Cancer
  Recruiting · Phase 3 · Interventional · 300 enrolled · National Cancer Institute (NCI)
  NCT04181060updated 2026-06-12
• A Study to Investigate Safety and Efficacy of Osimertinib and Amivantamab in Participants With Non-small Cell Lung Cancer With Common Epidermal Growth Factor Receptor Mutations
  Active not recruiting · Phase 2 · Interventional · 60 enrolled · AstraZeneca
  NCT05801029updated 2026-06-12
• A Study Comparing BL-B01D1 in Combination With Osimertinib Versus Osimertinib Alone in Patients With Locally Advanced, Unresectable EGFR-mutated Non-small Cell Lung Cancer(Stage III) Whose Disease Has Not Progressed Following Definitive Platinum-based Chemoradiation Therapy(PANKU-Lung08)
  Not yet recruiting · Phase 3 · Interventional · 418 enrolled · Sichuan Baili Pharmaceutical Co., Ltd.
  NCT07640789updated 2026-06-11
• Testing the Combination of MLN0128 (TAK-228) and AZD9291 in Advanced EGFR (Epidermal Growth Factor Receptor) Mutation Positive Non-small Cell Lung Cancer
  Active not recruiting · Phase 1 · Interventional · 36 enrolled · National Cancer Institute (NCI)
  NCT02503722updated 2026-06-11
• A Study of BL-B01D1 in Combination With Osimertinib as Perioperative Therapy in Patients With EGFR-mutated Resectable Non-small Cell Lung Cancer(PANKU-Lung09)
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 90 enrolled · Sichuan Baili Pharmaceutical Co., Ltd.
  NCT07642024updated 2026-06-11
• First in Human Study of AZD9592 in Solid Tumors
  Active not recruiting · Phase 1 · Interventional · 167 enrolled · AstraZeneca
  NCT05647122updated 2026-06-11
• Study to Allow Patients Previously Participating in a Novartis Sponsored Trial to Continue Receiving Capmatinib Treatment as Single Agent or in Combination With Other Treatments or the Combination Treatment Alone
  Active not recruiting · Phase 2 · Interventional · 29 enrolled · Novartis Pharmaceuticals
  NCT03040973updated 2026-06-11
• Testing Osimertinib as a Treatment for Lung Cancers With an EGFR Exon 20 Change
  Recruiting · Phase 2 · Interventional · 46 enrolled · National Cancer Institute (NCI)
  NCT03191149updated 2026-06-11
• Clinical Study on Savolitinib + Osimertinib in Treatment of EGFRm+/MET+ Locally Advanced or Metastatic NSCLC
  Active not recruiting · Phase 3 · Interventional · 412 enrolled · Hutchison Medipharma Limited
  NCT05009836updated 2026-06-10

Frequently asked questions

How does Osimertinib work?

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at approximately 9-fold lower concentrations than wild-type. Two pharmacologically-active metabolites (AZ7550 and AZ5104 circulating at approximately 10% of the parent) with similar inhibitory profiles to osimertinib have been identified in the plasma after oral administration of osimertinib.

What is Osimertinib used for?

According to FDA labeling, Osimertinib carries indications including: TAGRISSO is a kinase inhibitor indicated for: • adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. ( 1.1 , 2.2 ) • the treatment of adult patients with locally advanced, unresectable (stage III) NSCLC whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Osimertinib?

Osimertinib is classified as Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, Kinase Inhibitor, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 1A2 Inducers, Cytochrome P450 3A Inhibitors, Cytochrome P450 3A4 Inducers, Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Osimertinib?

Osimertinib is marketed under brand names including Tagrisso.

What are the contraindications for Osimertinib?

Osimertinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.