Key points
- Osimertinib (Tagrisso) is a targeted tablet that works only in lung cancer with an EGFR mutation, so a genetic test of the tumour is needed [1].
- It is used after surgery, after chemoradiotherapy and in disease that has spread [1].
- One tablet a day, with or without food; if you miss a dose, do not make it up and take the next one on time [1].
- After surgery, osimertinib helped patients live longer [1, 2].
- The most common side effects: diarrhoea, skin spots, muscle pain, nail changes and dry skin; the most important serious side effect is lung inflammation [1].
What is this drug and how does it work?
For physicians
Osimertinib (brand name Tagrisso) is an oral targeted drug from the kinase inhibitor group [1]. In some lung cancers the epidermal growth factor receptor (EGFR) gene is mutated, and the EGFR protein constantly sends growth and proliferation signals to the cancer cell. Osimertinib binds irreversibly to mutant forms of EGFR (T790M, L858R and exon 19 deletion) at concentrations about 9 times lower than for wild-type EGFR [1].
Two active metabolites with a similar inhibitory profile are also found in the blood [1]. In animal studies, osimertinib crossed into the brain (brain-to-plasma exposure ratio about 2) and caused tumour shrinkage in an animal model of brain metastases [1].
Which cancers is it used for?
According to the FDA label, osimertinib is approved only for adults with non-small cell lung cancer whose tumours have an EGFR exon 19 deletion or L858R mutation (or, in previously treated disease, a T790M mutation) detected by an FDA-approved test on a tumour sample or (depending on the indication) plasma [1]. So not every patient with lung cancer is a candidate for this drug. The European Medicines Agency (EMA) has also approved osimertinib as adjuvant treatment after surgery, for unresectable stage III disease, as first-line treatment (alone or with chemotherapy) and for T790M-positive disease, but the exact indications vary between countries [3].
Your doctor may prescribe this drug for:
- Non-small cell lung cancer after surgery [1]
- Stage III non-small cell lung cancer that cannot be removed by surgery [1]
- Non-small cell lung cancer that has spread, first line [1]
- Locally advanced or spread non-small cell lung cancer, first line (combination) [1]
- Non-small cell lung cancer that has spread, with a T790M mutation [1]
Whether it suits you depends on the type and stage of your cancer and your test results. Details of each use are in the section for doctors.
For physicians
| Cancer | Conditions of use |
|---|---|
| Non-small cell lung cancer after surgery | Adjuvant monotherapy after resection, with an exon 19 deletion or L858R mutation, for 3 years [1] |
| Unresectable stage III non-small cell lung cancer | Monotherapy after platinum-based chemoradiotherapy without progression during or after it; exon 19 deletion or L858R mutation [1] |
| Metastatic non-small cell lung cancer, first line | Monotherapy; exon 19 deletion or L858R mutation [1] |
| Locally advanced or metastatic non-small cell lung cancer, first line (combination) | With pemetrexed and platinum-based chemotherapy; exon 19 deletion or L858R mutation [1] |
| Metastatic non-small cell lung cancer with a T790M mutation | Monotherapy after progression during or after treatment with an EGFR tyrosine kinase inhibitor [1] |
Decide with the treating physician whether this drug is appropriate.
| Cancer | Key evidence |
|---|---|
| Non-small cell lung cancer after surgery | ADAURA trial [2]; hazard ratio for recurrence or death 0.17 in stage II to IIIA and hazard ratio for death 0.49 in the whole population compared with placebo [1] |
| Unresectable stage III non-small cell lung cancer | LAURA trial [4]; median progression-free survival 39.1 vs 5.6 months with placebo (hazard ratio 0.16) [1] |
| Metastatic non-small cell lung cancer, first line | FLAURA trial [5, 6]; median progression-free survival 18.9 vs 10.2 months and median overall survival 38.6 vs 31.8 months compared with gefitinib or erlotinib [1] |
| Locally advanced or metastatic non-small cell lung cancer, first line (combination) | FLAURA2 trial [7]; median progression-free survival 25.5 vs 16.7 months and median overall survival 47.5 vs 37.6 months compared with osimertinib alone [1] |
| Metastatic non-small cell lung cancer with a T790M mutation | AURA3 trial [8]; median progression-free survival 10.1 vs 4.4 months compared with chemotherapy [1] |
How it is taken and dosing
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Treatment regimens and doses: index3 regimens
Osimertinib comes as tablets (80 and 40 mg) taken once a day, with or without food [1]. If you find it hard to swallow the tablet, put it only in 60 mL of non-carbonated water and stir until it breaks into small pieces (it will not dissolve completely) and drink it straight away; then rinse the container with 120 to 240 mL of water and drink that too. Do not crush or heat the tablet [1]. There is also a specific method in the drug label for patients with a nasogastric feeding tube, which your treatment team will show you [1]. If you miss a dose, do not make it up; take the next dose at the usual time [1].
Duration: as adjuvant treatment after surgery, the drug is taken for 3 years in total (or until the cancer comes back or side effects cannot be tolerated); in other uses it continues as long as the disease does not progress and side effects are tolerable [1].
Tests:
- Before starting, an EGFR mutation must be confirmed with an approved test on a tumour sample (and in some uses a blood/plasma sample) [1].
- A full blood count before starting and regularly during treatment [1].
- A heart function check (left ventricular ejection fraction or LVEF, for example by echocardiogram) before starting and during treatment in people with heart risk factors, and in all patients on combination treatment with chemotherapy [1].
- Regular ECGs and electrolytes in people with congenital long QT syndrome, heart failure, electrolyte problems or QT-prolonging medicines [1].
- Regular checks of the muscle enzyme CPK, and a pregnancy test before starting in women who could become pregnant [1].
Monitoring (in addition to the baseline and periodic tests above): CBC with differential; LVEF with cardiac symptoms; CPK with unexplained muscle pain; with new respiratory symptoms, withhold and investigate promptly for ILD; refer to an ophthalmologist with symptoms of keratitis [1].
Nasogastric tube: administration via a nasogastric tube is allowed (disperse in 15 mL of water and give within 30 minutes) [1].
Interactions: avoid strong CYP3A4 inducers; if unavoidable, 160 mg daily, returning to 80 mg 3 weeks after stopping the inducer. Moderate or weak inducers need no adjustment. Monitor BCRP and P-gp substrates for toxicity; avoid drugs with a known risk of torsades de pointes that prolong QT where possible, otherwise periodic ECGs [1].
Kidney and liver: CLcr 15 to 89 mL/min and mild to moderate hepatic impairment (Child-Pugh A and B): no adjustment; there is no recommended dose for CLcr below 15 or severe hepatic impairment [1].
Dose modification (only reduction level: 40 mg daily) [1]:
- ILD/pneumonitis without recent definitive chemoradiotherapy: any grade, discontinue permanently. After recent definitive chemoradiotherapy: grade 1 continue or withhold; grade 2 or higher discontinue permanently.
- QTc above 500 ms on at least 2 ECGs: withhold until QTc is below 481 ms (or back to baseline if baseline was 481 or more), then resume at 40 mg. QTc prolongation with signs of life-threatening arrhythmia or symptomatic congestive heart failure: discontinue permanently.
- EMM, SJS or TEN and aplastic anaemia: withhold if suspected and discontinue permanently if confirmed.
- Other grade 3 or higher adverse reactions: withhold for up to 3 weeks; if improved to baseline or grade 0 to 2, resume at 80 or 40 mg; if not improved within 3 weeks, discontinue permanently.
For physicians
Standard dosing (FDA label)
Osimertinib monotherapy — adjuvant
Resected NSCLC with exon 19 deletion or L858R, after surgery (with or without adjuvant chemotherapy)
Resected NSCLC with exon 19 deletion or L858R, after surgery (with or without adjuvant chemotherapy)
Before prescribing: Prescribing notes| Drug | Dose | Route | Schedule |
|---|---|---|---|
| Osimertinib | 80 mg | Oral, with or without food | Once daily, continuously |
As per Table 2 of the FDA label [1].
Osimertinib monotherapy — after chemoradiotherapy, advanced disease or T790M
Unresectable stage III after platinum-based chemoradiotherapy without progression; metastatic first line (exon 19 deletion or L858R); metastatic T790M-positive after a prior TKI
Unresectable stage III after platinum-based chemoradiotherapy without progression; metastatic first line (exon 19 deletion or L858R); metastatic T790M-positive after a prior TKI
Before prescribing: Prescribing notes| Drug | Dose | Route | Schedule |
|---|---|---|---|
| Osimertinib | 80 mg | Oral, with or without food | Once daily, continuously |
As per Table 2 of the FDA label [1].
Osimertinib + pemetrexed + platinum (FLAURA2)
Locally advanced or metastatic NSCLC, first line, exon 19 deletion or L858R
Locally advanced or metastatic NSCLC, first line, exon 19 deletion or L858R
Before prescribing: Prescribing notes| Drug | Dose | Route | Schedule |
|---|---|---|---|
| Osimertinib | 80 mg | Oral | Once daily, continuously |
| Pemetrexed + cisplatin or carboplatin | As per each drug's label | IV | As per each drug's label |
The osimertinib label does not specify pemetrexed and platinum doses and refers to those drugs' labels. For toxicity, each drug's dose is modified separately. LVEF assessment is needed in all patients before starting [1].
Evidence: FLAURA2 (2026), FLAURA2 (2023)
Doses follow the trial protocol, guideline or official drug label (source given in the notes of each regimen). Before prescribing, check blood counts, renal and hepatic function, drug interactions and the patient’s condition, and adjust the dose according to the drug label.
Side effects
The most common side effects:
For physicians
Among 1813 patients with EGFR-mutated NSCLC who received osimertinib monotherapy in clinical trials, the most common adverse reactions (in 20% or more) were [1]:
- Diarrhoea: 47%
- Rash: 46%
- Musculoskeletal pain: 38%
- Nail toxicity (redness, pain, inflammation, brittleness or separation of the nail): 34%
- Dry skin: 32%
- Stomatitis: 24%
- Fatigue: 21%
The most common laboratory abnormalities in the same group were leucopenia (65%), lymphopenia (64%), thrombocytopenia (53%), anaemia (52%) and neutropenia (36%) [1]. These changes usually only show up in blood tests and are followed by the physician.
With pemetrexed and platinum-based chemotherapy (FLAURA2), the most common adverse reactions included leucopenia, thrombocytopenia, neutropenia, rash, diarrhoea, stomatitis, nail toxicity, dry skin and increased blood creatinine [1].
Serious side effects
These are less common but serious; tell your team early if you notice any sign of them:
- Lung inflammation: a new cough, shortness of breath or fever; in about 4 in 100 people, and more often if it is given after radiotherapy to the lung [1].
- Heart problems: shortness of breath, swollen legs, palpitations or fainting; your ECG and heart function are checked [1].
- Eye inflammation: pain, redness or blurred vision [1].
- Severe skin reactions (blisters, mouth sores), severe muscle pain, very low blood counts (rare) and harm to an unborn baby [1].
For physicians
The osimertinib label has no boxed warning but includes these important warnings (frequencies from the FDA label) [1]:
- Interstitial lung disease/pneumonitis: occurred in 4% of 1813 monotherapy patients without recent definitive chemoradiotherapy, fatal in 0.4%; 3.3% with combination treatment in FLAURA2 [1]. In the LAURA trial after chemoradiotherapy, pneumonitis (including radiation pneumonitis) was reported in 56% of patients on osimertinib vs 38% on placebo [1].
- QTc prolongation: QTc above 500 ms in 1.1% of monotherapy patients and 1.8% with combination treatment; no QTc-related arrhythmias were reported [1].
- Cardiomyopathy (including heart failure and reduced ejection fraction): 3.8% with monotherapy (fatal in 0.1%) and 9% with combination treatment in FLAURA2 (fatal in 1.1%) [1].
- Keratitis: 0.6% [1].
- Severe cutaneous reactions (erythema multiforme major, Stevens-Johnson syndrome and toxic epidermal necrolysis) and cutaneous vasculitis have been reported after marketing [1].
- Aplastic anaemia: 0.06% in trials and also after marketing; some cases have been fatal [1].
- Muscle pain or inflammation with raised CPK: myalgia in 4.8% and grade 1 myositis in 0.2%; rhabdomyolysis has been reported after marketing [1].
- Embryo-fetal toxicity: based on animal studies and mechanism of action, the drug can harm a fetus [1].
When should I call my doctor?
Tell your treatment team straight away if you have any of these symptoms [1]:
- New or worsening shortness of breath, cough or fever (lung symptoms can look like symptoms of the lung cancer itself)
- A pounding or racing heartbeat, swollen ankles and legs, dizziness, light-headedness or fainting
- Watery eyes, sensitivity to light, eye pain or redness, or a change in vision
- Ring-shaped (target-like) skin lesions, severe blistering or peeling skin
- Purple or red spots on the forearms, lower legs or buttocks that do not fade when pressed, or large hives on the trunk that last more than 24 hours and turn bruised
- A new or persistent fever (38 °C or higher), bruising easily or bleeding that will not stop, unusual paleness, infection, tiredness or weakness
- Unexplained muscle pain, tenderness or weakness
- Pregnancy or a possible pregnancy
In severe cases (such as severe shortness of breath, chest pain or fainting), call your local emergency number.
Interactions, pregnancy and precautions
Other medicines: give your doctor a list of all your medicines, supplements and herbal products, especially heart and blood pressure medicines [1]. Medicines such as rifampicin (a tuberculosis drug) and epilepsy medicines greatly lower osimertinib levels and should not be taken with it [1]. Antifungal drugs hardly change its level [1]. Osimertinib raises the level of some other medicines, and medicines that upset the heart rhythm should be avoided where possible [1].
Pregnancy and contraception: women who could become pregnant should use effective contraception during treatment and for 6 weeks after the last dose; men whose partner could become pregnant should use effective contraception during treatment and for 4 months after the last dose [1]. Based on animal studies, the drug may reduce fertility in women and men [1].
Breastfeeding: do not breastfeed during treatment and for 2 weeks after the last dose [1].
Vaccines: the FDA label gives no specific advice about vaccines; talk to your treatment team before any vaccination.
Storage: at room temperature (20 to 25 °C) and out of the reach of children [1].
Frequently asked questions
Is osimertinib chemotherapy?
Does osimertinib work on brain metastases?
In a small group of patients with tumours in the brain, osimertinib shrank the brain tumours in more patients than older drugs did [1]. In another study, this tablet with or without chemotherapy shrank brain tumours in most patients [1]. Make decisions about treating brain metastases with your treating doctor.
Scientific evidence
Show detailsHide
Key studies
4 itemsOverall Survival with Osimertinib in Resected EGFR-Mutated NSCLC
Osimertinib after Chemoradiotherapy in Stage III EGFR-Mutated NSCLC
Osimertinib with or without Chemotherapy in EGFR-Mutated Advanced NSCLC
Amivantamab plus Lazertinib in Previously Untreated EGFR-Mutated Advanced NSCLC
Related cancer types
Treatment regimens (physicians)
References
8 referencesShow all references, 6 with a study cardClose the reference list
Numbers in the text, such as [1], refer to these sources. Sources with a “Study card” button are summarised in the site’s evidence library.
- 1TAGRISSO (osimertinib) tablets, for oral use: Prescribing Information
- 2Overall Survival with Osimertinib in Resected EGFR-Mutated NSCLC
- 3Tagrisso (osimertinib): European public assessment report (EPAR)
- 4Osimertinib after Chemoradiotherapy in Stage III EGFR-Mutated NSCLC
- 5Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer
- 6Overall Survival with Osimertinib in Untreated, EGFR-Mutated Advanced NSCLC
- 7Osimertinib with or without Chemotherapy in EGFR-Mutated Advanced NSCLC
- 8Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer
This page is based on reputable scientific sources and was last updated on 27 October 2026. The content of this website is for educational and informational purposes only and does not replace consultation, diagnosis or treatment by a specialist physician. Consult your treating physician about any treatment decision.
Printed from the website; the full and up-to-date version: https://drdabiri.com/en/drugs/osimertinib/
