CMTTdb

An integrated database for cancer molecular targeted thearpies

Entry Detail


General information
Database:DB00890
Objective:The highly effective treatment of human epidermal growth factor receptor (HER) 2amplified breast cancer has proven challenging because of a signal buffering capacity inherent in the functionally relevant human epidermal growth factor receptor 2HER3 target. human epidermal growth factor receptor 2HER3 signaling can be inactivated by doses of lapatinib that fully inactivate the human epidermal growth factor receptor 2 kinase. In mouse models, such doses are not tolerable in continuous administration, but they are tolerable and highly effective in intermittent dosing. they pursued the clinical translation of this treatment hypothesis.
Authors:Chien AJ, et al
Title:Phase I doseescalation study of 5day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2overexpressing breast cancer.
Journal:J Clin Oncol.
Year:2014
PMID:24711549
Trial Design
Clinical Trial Id:NCT00544804
Agent:lapatinib
Target:Epidermal growth factor receptor
Receptor proteintyrosine kinase erbB2
Cancer Type:breast cancer
Cancer Subtype:human epidermal growth factor receptor 2positive advanced breast cancer
Therapy Type:mono
Therapeutic Combination Type:NA
Therapeutic Combination Content:NA
Study Type:Phase I doseescalation study
Key Patients Feature:women with advanced human epidermal growth factor receptor 2overexpressing breast cancer
Biomarker:NA
Biomark Analysis:NA
Control Group Info:single arm
Treatment Info: Lapatinib was administered on days 1 through 5 of repeating 14day cycles. Dose escalation was conducted using a 3+3 design with plasma lapatinib level monitoring.
Primary End Point:DLT, MDT, toxicity
Secondary End Point:NA
Patients Number:40
Trial Results
DLT_MTD:DLT was defined as toxicity occurring during the first cycle (14 days) of therapy attributable to lapatinib. DLTs were defined as any grade 3 or greater toxicity. In the case of diarrhea and nausea and vomiting, DLT was defined as grade 3 or greater toxicity on 3 consecutive days despite maximal use of supportive medications. In patients with liver metastases, DLT was defined as grade 3 or greater transaminitis with a more than and equal to twofold increase over baseline. Grade 3 fatigue was a DLT if it persisted at the start of cycle 2.MTD was not defined or pursued for this 5day intermittent regimen.
Objective Response Rate:NA
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):NA
Conclusions:Lapatinib exposure can be safely and significantly increased through intermittent dosing but reaches a ceiling that currently impedes clinical translation of the treatment hypothesis. Preliminary efficacy data suggest that exposures approaching those seen in mouse models can result in highly significant tumor responses.