Table 1.

Drug summary box.

Name	AZD9291, osimertinib, Tagrisso™
Chemical structure
Biochemical name	N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2- yl]amino]phenyl]prop-2-enamide
Pharmacodynamics	Irreversible, covalent bond and inhibition of sensitizing mutation (exon 19 deletion, L858R) and double mutants harboring T790M
Pharmacokinetics	Median time to Cmax = 6 h Mean volume of distribution Vss = 986 l Oral clearance = 14.2 l/h Mean half-life = 38 h Time to steady state: 22 days Elimination: 68% fecal and 14% urinary
Drug interaction	CYP3A inhibitors or inducers, substrates of CYP3A, BCRP and CYP1A2
Adverse events	Any grade ⩾5%: diarrhea, rash, dry skin, nail toxicity, decreased appetite Select toxicities of special interest: ILD/pneumonitis, QTc interval prolongation, cardiomyopathy, hyperglycemia

ILD, interstitial lung disease