CMTTdb

An integrated database for cancer molecular targeted thearpies

Entry Detail


General information
Database:DB00147
Objective:Thisphase Ib trial investigated the safety, tolerability, and recommendedphase II dose and schedule of the MEK inhibitor trametinib in combination with the mammalian target of rapamycin (mTOR) inhibitor everolimus. pharmacokinetic (PK) characterization and evaluation of clinical activity.
Authors:Tolcher AW, et al
Title:a phase IB trial of the oral MEK inhibitor trametinib (GSK1120212) in combination with everolimus in patients with advanced solid tumors.
Journal:Ann Oncol.
Year:2015, Jan.
PMID:25344362
Trial Design
Clinical Trial Id:NCT00955773
Agent:trametinib
Target:MEK2
Dual specificity mitogenactivated protein kinase kinase 1
Cancer Type:advanced solid tumors
Cancer Subtype:advanced solid tumors
Therapy Type:com
Therapeutic Combination Type:1
Therapeutic Combination Content:trametinib+everolimus
Study Type:an openlabel, singlearm, doseescalationphase IB trial
Key Patients Feature:patients with advanced solid tumors
Biomarker:NA
Biomark Analysis:NA
Control Group Info:single arm
Treatment Info:Dose escalation followed a 3 + 3 design. patients were assigned to one of 10 different cohorts, involving either daily dosing with both agents or daily dosing with trametinib and intermittent everolimus dosing. This included an expansion cohort comprising patients with pancreatic tumors. PKs samples were collected predose, as well as 1, 2, 4, and 6 h postdose on day 15 of the first treatment cycle.
Primary End Point:the safety, tolerability, and recommendedphase II dose.
Secondary End Point:pharmacokinetic (PK) characterization and evaluation of clinical activity.
Patients Number:67
Trial Results
DLT_MTD:The majority of changes to dose and schedule were designed to reduce the incidence and severity of mucosal inflammation/stomatitis, which was the major hindrance for tolerability.
Objective Response Rate:NA
Disease Control Rate:5 (7%) achieved partial response (PR) to treatment and 21 (31%) displayed stable disease (SD). Among the 21 patients with pancreatic cancer, PR was observed in 1 patient (5%) and SD in 6 patients (29%).
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 AEs regardless of relationship to treatment were fatigue (61%), diarrhea (45%), mucosal inflammation (42%), nausea (40%), and vomiting (37%).
Conclusions:This study was unable to identify a recommendedphase II dose and schedule of trametinib in combination with everolimus that provided an acceptable tolerability and adequate drug exposure.