Select a medication above to begin.
Tagrisso
osimertinib
Adult Dosing .
Dosage forms: TAB: 40 mg, 80 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
non-small cell lung CA
- [adjuvant tx, monotherapy]
- Dose: 80 mg PO qd for up to 3y; Start: after tumor resection; Info: for pts w/ EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
- [locally advanced, stage III unresectable dz, monotherapy]
- Dose: 80 mg PO qd; Start: after platinum-based chemoradiation; Info: for pts w/ EGFR exon 19 deletions or exon 21 (L858R) substitution mutations w/o dz progression on or after platinum-based chemoradiation
- [metastatic dz, first-line tx, monotherapy]
- Dose: 80 mg PO qd; Info: for pts w/ EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
- [locally advanced or metastatic dz, first-line tx, combo tx]
- Dose: 80 mg PO qd; Info: for pts w/ EGFR exon 19 deletions or exon 21 (L858R) substitution mutations; part of multi-drug chemo regimen
- [progressive metastatic dz, monotherapy]
- Dose: 80 mg PO qd; Info: for pts w/ EGFR T790M mutations
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class A or B: no adjustment; Child-Pugh Class C: not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- QT prolongation
- avoid: breastfeeding during tx and x2wk after D/C
- caution: electrolyte abnormalities
- caution: long QT syndrome, congenital
- caution: QT prolongation family hx
- caution: torsades de pointes hx
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
- caution: pts 65 yo and older
- caution: female pts of reproductive potential
- caution: male pts of reproductive potential
Drug Interactions .
Overview
osimertinib
kinase inhibitor
- CYP3A4 substrate
- BCRP inhibitor
- P-gp inhibitor, weak
- cardiotoxic effects
- prolongs QT interval (known)
Contraindicated
- cisapride
- colchicine
- domperidone
- dronedarone
- levoketoconazole
- pimozide
- thioridazine
Avoid/Use Alternative
- adagrasib
- alpelisib
- amiodarone
- anagrelide
- apalutamide
- apixaban
- apomorphine
- arsenic trioxide
- artemether/lumefantrine
- asenapine
- azithromycin
- bedaquiline
- butalbital
- cabozantinib
- carbamazepine
- ceritinib
- chloroquine
- citalopram
- cladribine oral
- clarithromycin
- clofazimine
- crizotinib
- dabigatran
- deferiprone
- degarelix
- desflurane
- desipramine
- dexmedetomidine
- dexmedetomidine injection
- dexrazoxane
- disopyramide
- dofetilide
- donepezil
- droperidol
- efavirenz
- encorafenib
- ensartinib
- entrectinib
- enzalutamide
- ephedra
- epirubicin
- eribulin
- erythromycin
- etrasimod
- fexinidazole
- flecainide
- fluorouracil
- fluoxetine
- foscarnet
- fosphenytoin
- futibatinib
- ganciclovir
- gilteritinib
- givinostat
- glasdegib
- goserelin
- grapefruit
- haloperidol
- histrelin
- hydroxychloroquine
- hydroxyzine
- ibutilide
- idarubicin
- iloperidone
- inotuzumab ozogamicin
- isoflurane
- ivabradine
- ivosidenib
- lefamulin
- leuprolide
- levofloxacin
- lofexidine
- lonafarnib
- loperamide
- lopinavir/ritonavir
- lumacaftor/ivacaftor
- macimorelin
- methadone
- mifepristone
- mitotane
- mobocertinib
- moxifloxacin
- neratinib
- nilotinib
- oliceridine
- ondansetron
- oxaliplatin
- ozanimod
- pacritinib
- palifermin
- paliperidone
- palonosetron
- panobinostat
- pasireotide
- pazopanib
- pentamidine
- pentobarbital
- phenobarbital
- phenytoin
- pimavanserin
- pitolisant
- ponesimod
- pralsetinib
- primidone
- procainamide
- propafenone
- quetiapine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- radium Ra 223 dichloride
- relugolix
- repotrectinib
- revumenib
- ribociclib
- rifabutin
- rifampin
- rilpivirine
- rivaroxaban
- romidepsin
- rucaparib
- selpercatinib
- sertraline
- sevoflurane
- siponimod
- sirolimus albumin-bound
- solifenacin
- sorafenib
- sotalol
- St. John's wort
- telavancin
- tetrabenazine
- topotecan
- toremifene
- tramadol
- trazodone
- triclabendazole
- trifluridine
- triptorelin
- valganciclovir
- vandetanib
- vemurafenib
- venetoclax
- ziprasidone
Monitor/Modify Tx
- adalimumab
- ado-trastuzumab emtansine
- afatinib
- albendazole
- albuterol
- albuterol inhaled
- aldesleukin
- alemtuzumab
- alfuzosin
- amisulpride
- amitriptyline
- arformoterol inhaled
- asciminib
- atorvastatin
- avelumab
- axitinib
- azathioprine
- balsalazide
- benznidazole
- berotralstat
- bevacizumab
- bezlotoxumab
- binimetinib
- bortezomib
- buprenorphine
- capecitabine
- carfilzomib
- certolizumab pegol
- chlorpromazine
- ciprofloxacin
- clomipramine
- clozapine
- cyclophosphamide
- cyclosporine
- dabrafenib
- dasatinib
- daunorubicin
- deferasirox
- deutetrabenazine
- digoxin
- doxorubicin
- edoxaban
- eliglustat
- enfortumab vedotin
- escitalopram
- everolimus
- fam-trastuzumab deruxtecan
- fingolimod
- fluconazole
- flucytosine
- fluvastatin
- formoterol inhaled
- fostemsavir
- gemtuzumab ozogamicin
- gepirone
- granisetron
- hydrocodone
- ibrutinib
- ifosfamide
- imatinib
- infliximab
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- irinotecan
- lapatinib
- leflunomide
- lenvatinib
- levalbuterol inhaled
- lumateperone
- lurasidone
- margetuximab
- mavacamten
- mavorixafor
- mefloquine
- meperidine
- mercaptopurine
- mesalamine
- mesalamine rectal
- methotrexate
- metronidazole
- midostaurin
- mirdametinib
- mirtazapine
- mitoxantrone
- morphine
- ofloxacin
- olodaterol inhaled
- osilodrostat
- pegfilgrastim (G-CSF)
- peginterferon beta 1a
- pertuzumab
- pitavastatin
- ponatinib
- posaconazole
- primaquine
- proguanil
- promethazine
- ranolazine
- riociguat
- ripretinib
- rituximab
- rosuvastatin
- sacituzumab govitecan
- salmeterol inhaled
- sargramostim (GM-CSF)
- satralizumab
- selumetinib
- sirolimus
- sitagliptin
- sunitinib
- tacrolimus
- talazoparib
- tazemetostat
- tenofovir alafenamide
- tenofovir disoproxil
- terbutaline
- tivozanib
- tofacitinib
- tolterodine
- trastuzumab
- trimethoprim
- ubrogepant
- valbenazine
- vardenafil
- venlafaxine
- vilanterol inhaled
- voclosporin
- voriconazole
- zanidatamab
- zenocutuzumab
Caution Advised
- bosentan
- cenobamate
- darolutamide
- etravirine
- glecaprevir
- lorlatinib
- mitapivat
- modafinil
- nafcillin
- naldemedine
- pexidartinib
- pibrentasvir
- rifapentine
- seladelpar
- sotorasib
- sulfasalazine
Adverse Reactions .
Serious Reactions
- interstitial lung dz
- pneumonitis
- pulmonary embolism
- pneumonia
- neutropenia
- lymphopenia
- aplastic anemia
- cardiomyopathy
- QT prolongation
- Stevens-Johnson syndrome
- erythema multiforme
- toxic epidermal necrolysis
- cutaneous vasculitis
- keratitis
Common Reactions
- diarrhea
- rash
- nail changes
- xeroderma
- stomatitis
- fatigue
- cough
- appetite decr.
- pruritus
- nausea
- constipation
- URI
- vomiting
- musculoskeletal pain
- epistaxis
- abdominal pain
- alopecia
- dyspnea
- cardiomyopathy
- UTI
- dizziness
- headache
- interstitial lung dz
- pneumonitis
- fever
- QT prolongation
- back pain
- lymphopenia
- thrombocytopenia
- anemia
- neutropenia
- hyperglycemia
- hypermagnesemia
- hyponatremia
- CK incr.
Safety/Monitoring .
Monitoring Parameters
Monotherapy: pregnancy test at baseline; CBC w/ diff at baseline, then periodically, or more frequently if clinically indicated; LVEF at baseline, then during tx if cardiac risk factors; ECG, electrolytes incl. Mg if QT prolongation risk
Combo Tx: pregnancy test at baseline; LVEF at baseline, then during tx; CBC w/ diff at baseline, then periodically, or more frequently if clinically indicated; ECG, electrolytes incl. Mg if QT prolongation risk
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of teratogenicity based on animal data at 0.1x systemic exposure and drug's mechanism of action; risk of embryo-fetal death and decr. fetal growth at 1.5x systemic exposure and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x6wk after D/C in female pts and x4mo after D/C in male pts
Lactation
Clinical Summary
avoid breastfeeding during tx and x2wk after D/C; no human data available to assess risk of infant harm, though possible drug excretion into milk based on drug properties; no human data available to assess effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 3A substrate
Excretion: feces 68% (minimally unchanged), urine 14% (minimally unchanged); Half-life: 48h
Subclass: EGFR Antagonists ; Kinase Inhibitors, EGFR Inhibitors
Mechanism of Action
binds to epidermal growth factor receptor (EGFR), inhibiting kinase activity and cancer cell signal transduction
Formulary .
No Formulary Selected
Join Now to View Patient Handouts!
Create a FREE epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.
Pill Pictures
Join Now to View Pill Pictures!
Create a FREE epocrates Online account to access full-color images of medications within the drug monograph.
Current Members: Sign In.