Osimertinib

Cytostatic · Kinase Inhibitor

Indications

As adjuvant treatment after tumour resection in adult patients with non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. First-line treatment of adult patients with metastatic NSCLC whose tumours have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. 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 TKI therapy.

Dosage

Adults: 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 yrs. Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. For patients who have difficulty swallowing solids: Disperse tablet in 60 mL (2 ounces) of non-carbonated water only. Stir until tablet is dispersed into small pieces (the tablet will not completely dissolve) and swallow immediately. Do not crush, heat, or ultrasonicate during preparation. Rinse the container with 120 mL to 240 mL (4 to 8 ounces) of water and immediately drink. If administration via nasogastric tube is required, disperse the tablet as above in 15 mL of non-carbonated water, and then use an additional 15 mL of water to transfer any residues to the syringe. The resulting 30 mL liquid should…

Adverse Effects

Leucopenia, lymphopenia, thrombocytopenia, diarrhoea, anaemia, rash, musculoskeletal pain, nail toxicity, neutropenia, dry skin, stomatitis, fatigue and cough.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Interstitial Lung Disease (ILD). Pneumonitis. Erythema multiforme. Stevens-Johnson Syndrome. Cutaneous vasculitis. Precautions: Prolonged QTc interval. Conduct cardiac monitoring, including left ventricular ejection fraction (LVEF) assessment in patients with cardiac risk factors before initiating treatment and during treatment. Keratitis.

Interactions

Strong CYP3A inducers. Breast cancer resistant protein (BCRP) or P-glycoprotein (P-gp) substrate.

Advice to Patient

Take with or without meals. Females of reproductive potential must use effective contraception during treatment and for 6 wks after final dose. Lactating mothers should avoid nursing babies during treatment and for 2 weeks after the final dose. Male patients with females of reproductive potential must use effective contraception during treatment and 4 months after the last dose. Report if any of the following symptoms occur: Dizziness, lightheadedness, syncope, eye symptoms (eye inflammation, lacrimation, light sensitivity, eye pain, red eye or changes in vision), multiple non-blanching red papules on forearms, lower legs, or buttocks, or large hives on trunk that do not go away within 24 hrs and development of a bruised appearance.

Pharmacokinetics

Metabolism: Hepatic. Half-life elimination: 48 hrs. Time to peak: 6 hrs (range: 3-24 hrs). Excretion: Faeces (68%). Urine (14%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.