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

A J Barker; K H Gibson; W Grundy; A A Godfrey; J J Barlow; M P Healy; J R Woodburn; S E Ashton; B J Curry; L Scarlett; L Henthorn; L Richards

doi:10.1016/s0960-894x(01)00344-4

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

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1911-4. doi: 10.1016/s0960-894x(01)00344-4.

Authors

A J Barker¹, K H Gibson, W Grundy, A A Godfrey, J J Barlow, M P Healy, J R Woodburn, S E Ashton, B J Curry, L Scarlett, L Henthorn, L Richards

Affiliation

¹ AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK.

PMID: 11459659
DOI: 10.1016/s0960-894x(01)00344-4

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.

MeSH terms

Administration, Oral
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Carcinoma, Squamous Cell / metabolism
ErbB Receptors / antagonists & inhibitors*
Gefitinib
Humans
KB Cells / cytology
Quinazolines / chemical synthesis
Quinazolines / pharmacology*
Sensitivity and Specificity
Tumor Cells, Cultured / cytology
Tumor Cells, Cultured / metabolism

Substances

Antineoplastic Agents
Quinazolines
ErbB Receptors
Gefitinib