Iressa Film-Coated Tab.250mg-仿單-中文 doc

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呼伦成
7 years ago
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1 250 IRESSA Film-Coated Tablets 250 mg IRESSA mg gefitinib IRESSA IRESSA 250mg ( ) ( 10 ) IRESSA mg

2 Iressa (ILD) / / / / Iressa Iressa 3159 Iressa 12 (ILD) Iressa PS 2 50% 6 55 IRESSA CYP3A4 gefitinib CYP3A4 phenytoin carbamazepine rifampicin St John s warfarin (INR) / warfarin (PT) INR ph gefitinib

3 IRESSA brain stem glioma incompletely resected supratentorial malignant glioma ependymoma IRESSA IRESSA IRESSA vinorelbine IRESSA vinorelbine gefitinib CYP3A4 rifampicin( 3A4 ) gefitinib AUC rifampicin 83% itraconazole CYP3A4 gefitinib AUC 80% ph 5 gefitinib AUC 47% IRESSA gefitinib IRESSA

4 IRESSA 20% 8% ADR (Common Toxicity Criteria CTC) 3 4 3% ADR ADR (>10%) CTC 1 2 CTC 3 4 CTC 1 CTC 1 2 (>1-10%) CTC 1 2 CTC 1 CTC 1 2 CTC 1 CTC 1 2 CTC 1 * CTC 1

5 (>0.1-1%) (>0.01-1%) warfarin (INR) / (CTC 3-4 ) (< 1%) Stevens Johnson syndrome * IRESSA expanded access / compassionate use ILD 0.3% phase III 1692 IRESSA BSC 1 2 ILD 1% ILD IRESSA IRESSA ILD 3% 4% 3350 ILD IRESSA 5.8% 12 ILD Iressa 4.0% 2.1% Iressa ILD OR % CI

6 Iressa ILD % CI % CI IRESSA 1000mg Gefitinib (epidermal growth factor receptor EGFR) (tyrosine kinase) EGFR gefitinib IRESSA phase II NSCLC IRESSA phase III IRESSA 1 2 IRESSA HR 0.89, CI , p=0.09, gefitinib HR 0.84, CI , p=0.09, gefitinib IRESSA IRESSA HR=0.66, CI , p=0.01, HR=0.67, CI , p=0.01, EGFR gene copy number IRESSA gene copy number gene

7 copy number interaction p-value= gene copy number IRESSA 0.61 N=114, 95% CI , p=0.067 gene copy number 1.16 N=256, 95% CI , p=0.42 EGFR gene copy number N=1322, HR=0.85, CI , p=0.032 EGFR gene copy number fluorescence in situ hybridisation LSI EGFR SpetrumOrange / CEP 7 SpetrumGreen probe 40% 4 copies EGFR / 2 10% EGFR 15 copies EGFR IRESSA EGFR N=264, HR=0.77; CI , p=0.13 EGFR N=115, HR=1.57; CI , p=0.14 EGFR EGFR N=1313, HR=0.84; CI , p=0.03 HR EGFR DAKO pharmdx TM EGFR EGFR pharmdx TM 1% 10% EGFR EGFR IRESSA EGFR gene copy number IRESSA EGFR gene copy numberegrf gefitinib Gefitinib

8 IRESSA gefitinib % gefitinib (exposure) 5 gefitinib 47% gefitinib 1400L 90% Gefitinib 1- P450 CYP3A4 gefitinib gefitinib CYP2D6 gefitinib metoprolol CYP2D6 metoprolol (35%) Gefitinib P450 Gefitinib N-propylmorpholino quinazoline O-desmethyl gefitinib 14% 8 o-desmethyl gefitinib EGFR gefitinib 14 gefitinib O-desmethyl gefitinib CYP2D6 CYP2D6 CYP2D6 gefitinib O-desmethyl gefitinib Gefitinib

9 gefitinib CYP2D6 Gefitinib 500 / 4% phase I open-label gefitinib 250mg Child-Pugh 3.1 gefitinib gefitinib Gefitinib mg IRESSA Cmaxss AUC24ss 4 Gefitinib gefitinib 20mg 30mg 20mg 20mg gefitinib

10 gefitinib QT rat 10mg/kg/day mice 50mg/kg/day 90mg/kg/day mg/kg/day AstraZeneca AstraZeneca UK Limited Silk Road, Business Park, Macclesfield, Cheshire, SK10 2NA England

11 AstraZeneca Pty. Ltd Khartoum Road, North Ryde, New South Wales, 2113, Australia (02)

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