title: Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.
abstract: This paper describes the development of the epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 from a lead series of 4-anilinoquinazoline compounds. ZD1839 has suitable properties for use as a clinically effective drug and shows activity against human tumours. In particular, the use of pharmacokinetic data in the development of ZD1839 is discussed.
authors.affiliation: AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK.
authors.forename: A J
authors.initials: AJ
authors.lastname: Barker
authors.forename: K H
authors.initials: KH
authors.lastname: Gibson
authors.forename: W
authors.initials: W
authors.lastname: Grundy
authors.forename: A A
authors.initials: AA
authors.lastname: Godfrey
authors.forename: J J
authors.initials: JJ
authors.lastname: Barlow
authors.forename: M P
authors.initials: MP
authors.lastname: Healy
authors.forename: J R
authors.initials: JR
authors.lastname: Woodburn
authors.forename: S E
authors.initials: SE
authors.lastname: Ashton
authors.forename: B J
authors.initials: BJ
authors.lastname: Curry
authors.forename: L
authors.initials: L
authors.lastname: Scarlett
authors.forename: L
authors.initials: L
authors.lastname: Henthorn
authors.forename: L
authors.initials: L
authors.lastname: Richards
mesh_terms: D000284:Administration, Oral; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002294:Carcinoma, Squamous Cell / Q000378:metabolism; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D000077156:Gefitinib; D006801:Humans; D007624:KB Cells / Q000166:cytology; D011799:Quinazolines / Q000138:chemical synthesis / Q000494:pharmacology*; D012680:Sensitivity and Specificity; D014407:Tumor Cells, Cultured / Q000166:cytology / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines; D066246:ErbB Receptors; D000077156:Gefitinib