Tagrisso (Osimerinib) Guidelines+ Monographs

Published: May 19, 2025

Tagrisso (osimerinib) is a kinase inhibitor for patients with non-small cell lung cancer. Oral tablets (80mg and 40mg) of Tagrisso were approved by the FDA in 2015. Across the board, common adverse reactions, including laboratory abnormalities, were leukopenia, lymphopenia, thrombocytopenia, diarrhea, rash, neutropenia, and nail toxicity.

Read on to discover Tagrisso’s indications, adverse reactions, drug interactions, warnings, and more.

Medication Overview:

Brand Name: Tagrisso
Generic Name: Osimerinib
Treatment for: Non-Small Cell Lung Cancer
Manufacturer(s): AstraZeneca
FDA Approval: 2015 (initial approval)

Indicated Condition	Indicated	Age	Date Approved
Locally Advanced, Unresectable (Stage III) EGFR Mutation-Positive NSCLC	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.	adult patients	2024
EGFR Mutation-Positive Locally Advanced or Metastatic NSCLC	In combination with pemetrexed and platinum-based chemotherapy is indicated for the first-line treatment of adult patients with locally advanced or metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.	adult patients	2024
EGFR Mutation-Positive Non-Small Cell Lung Cancer (NSCLC)	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.	adult patients	2020
EGFR Mutation-Positive Metastatic NSCLC	First-line treatment of adult patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.	adult patients	2018
Previously Treated EGFR T790M Mutation-Positive Metastatic NSCLC	Treatment of adult patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, whose disease has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.	adult patients	2015

WARNINGS:

See full prescribing information for complete boxed warning.

Interstitial Lung Disease (ILD)/Pneumonitis: Occurred in 4% of patients. Permanently discontinue Tagrisso in patients diagnosed with ILD/Pneumonitis.
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.
Cardiomyopathy: Occurred in 3.8% of patients. Conduct cardiac monitoring, including left ventricular ejection fraction assessment in patients with cardiac risk factors.
Keratitis: Promptly refer patients with signs and symptoms of keratitis to an ophthalmologist for evaluation.
Erythema Multiforme Major, Stevens-Johnson Syndrome, and Toxic
Epidermal Necrolysis: Withhold Tagrisso if erythema multiforme major, Stevens-Johnson syndrome, or toxic epidermal necrolysis is suspected and permanently discontinue if confirmed.
Cutaneous Vasculitis: Withhold Tagrisso if cutaneous vasculitis is suspected, evaluate for systemic involvement, and consider dermatology consultation. If no other etiology can be identified, consider permanent discontinuation based on severity.
Aplastic Anemia: Withhold Tagrisso if aplastic anemia is suspected and permanently discontinue Tagrisso if confirmed.
Embryo-Fetal Toxicity: Tagrisso can cause fetal harm. Advise females of potential risk to the fetus and to use effective contraception during treatment with Tagrisso and for six weeks after final dose. Advise males to use effective contraception for four months, after the last dose of Tagrisso.

Dosage and Administration

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 three years.
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.
Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.
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.

Contraindications:

None

Drug Interactions:

Strong CYP3A Inducers: Avoid concomitant use. If not possible, increase Tagrisso to 160mg daily in patients receiving a strong CYP3A4 inducer.

Adverse Reactions:

Tagrisso Monotherapy: leukopenia, lymphopenia, thrombocytopenia anemia, diarrhea, rash, musculoskeletal pain, neutropenia, nail toxicity, dry skin, stomatitis, and fatigue.
Tagrisso in Combination with Pemetrexed and Platinum-based Chemotherapy: leukopenia, thrombocytopenia, neutropenia, lymphopenia, rash, diarrhea, and stomatiti.

Examples of Osimertinib in Guidelines

Therapy for Stage IV Non-Small-Cell Lung Cancer with Driver Alterations
American Society of Clinical Oncology

Published: February 27, 2025
Recommendation 1.1.1: Clinicians may offer osimertinib with platinum doublet chemotherapy or amivantamab plus lazertinib (Evidence quality: Moderate; Strength of recommendation: Weak).
Recommendation 2.2: For patients whose disease has progressed on osimertinib or other EGFR TKIs without emergent T790M or other targetable alterations, clinicians may offer platinum-based chemotherapy with or without amivantamab (Evidence quality: Moderate; Strength of recommendation: Strong).

Management of Stage III Non-Small Cell Lung Cancer
American Society of Clinical Oncology

Published: July 23, 2024
Recommendation 5.8: Patients with unresectable stage III NSCLC with an EGFR exon 19 deletion or exon 21 L858R mutation may be offered consolidation osimertinib after definitive chemoradiotherapy (platinum-based chemotherapy and thoracic radiation given concurrently or sequentially; Evidence quality: Moderate; Strength of recommendation: Strong).

Adjuvant Systemic Therapy and Adjuvant Radiation Therapy for Stage I-IIIA Completely Resected Non-Small-Cell Lung Cancer
American Society of Clinical Oncology

Published: February 15, 2022
Recommendation 1.2: Stage IB (3 < T ≤ 4 cm, N0M0): Adjuvant osimertinib is recommended for patients with sensitizing EGFR (Ex19del or L858R) mutations (Type: evidence based; Evidence quality: high; Strength of recommendation: Strong).

Treatment of Adults with Metastatic Brain Tumors
Congress of Neurological Surgeons

Published: March 17, 2025
Recommendation: In patients with leptomeningeal disease from NSCLC with EGFR mutations, it is suggested that EGFR TKIs be used to increase median survival, specifically the third-generation TKI osimertinib for patients with EGFR-mutant NSCLC and the second-generation ALK-TKI alectinib for the treatment of leptomeningeal metastases in ALK-positive NSCLC. (Level III)

Please note: This article is current as of May 12, 2025. Consult our clinical guidelines library or drug information tool to ensure you always have the most up-to-date information.