CMTTdb

An integrated database for cancer molecular targeted thearpies

Entry Detail


General information
Database:DB00707
Objective:This study (EGF10004) assessed the safety/tolerability, pharmacokinetics, and clinical activity of daily oral dosing with lapatinib (GW572016) in patients with ErbB1expressing and/or ErbB2overexpressing advancedstage refractory solid tumors.
Authors:Burris HA 3rd, et al
Title:Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas.
Journal:J Clin Oncol.
Year:2005
PMID:15955900
Trial Design
Clinical Trial Id:NA
Agent:lapatinib
Target:Epidermal growth factor receptor
Receptor proteintyrosine kinase erbB2
Cancer Type:advanced solid tumors
Cancer Subtype:advanced solid tumors
Therapy Type:mono
Therapeutic Combination Type:NA
Therapeutic Combination Content:NA
Study Type:Phase I Safety, Pharmacokinetics, and Clinical ActivityStudy
Key Patients Feature:ibility CriteriaPatients enrolled in this study were males or females age 18years or older with a histologicallyconfirmed diagnosis of cancer;had an archived or fresh biopsy that demonstrated expression ofErbB1(positive byimmunohistochemistry[IHC])and/oroverexpression of ErbB2 (2 or 3 by IHC) or that displayed gene amplification of ErbB2 by fluorescence in situ hybridization; hada Karnofsky performance status $ 70%; had a life expectancyof at least 12 weeks; had a hemoglobin concentration $ 9 g/dL(5 mmol/L), an absolute granulocyte count $ 1, 500/mm3(1.5 109/L), a platelet count $ 100, 000/mm3 (100 109/L);and were able to swallow and retain oral medication.
Biomarker:ErbB1expressing and/or ErbB2overexpressing
Biomark Analysis:NA
Control Group Info:single arm
Treatment Info:pts were randomly assigned to one of five dose cohorts of lapatinib administered once daily. Pharmacokinetic samples were obtained on days 1 and 20. Clinical response was assessed every 8 weeks.
Primary End Point:(1)safety and tolerability; (2) pharmacokinetics; (3)biologic effects;(4) a biologically active dose range;(5)the clinical activity
Secondary End Point:NA
Patients Number:67
Trial Results
DLT_MTD:NA
Objective Response Rate:59 of 67 patients were assessable for diseaseassessment. Four patients experienced partial responses Stable disease(SD) was reported in 24 patients
Disease Control Rate:NA
Median Time to Progression:NA
Median PFS A vs. C:NA
Median OS A vs. C:NA
Adverse Event(agent arm):The most frequently reported drugrelated adverse events were diarrhea (42%) and rash (31%). No grade 4 drugrelated adverse events were reported. Five grade 3 drugrelated toxicities (gastrointestinaleventsandrash)wereexperiencedbyfourpatients.Drugrelatedinterstitialpneumonitisor cardiac dysfunction associated with other ErbBtargeted therapies was not reported.
Conclusions:Lapatinib was well tolerated at doses ranging from 500 to 1,600 mg once daily. Clinical activity was observed in heavily pretreated patients with ErbB1expressing andor ErbB2overexpressing metastatic cancers, including four PRs in patients with trastuzumabresistant breast cancers and prolonged stable disease in 10 patients.