CMTTdb

An integrated database for cancer molecular targeted thearpies

Entry Detail


General information
Database:DB00161
Objective:Resistance to chemotherapyinduced apoptosis represents a major obstacle to cancer control. Overexpression of Bcl2 is seen in multiple tumor types and targeting Bcl2 may provide therapeutic benefit. a phase I study of navitoclax, a novel inhibitor of Bcl2 family proteins, was conducted to evaluate safety, pharmacokinetics, and preliminary efficacy in patients with solid tumors.
Authors:Gandhi L, et al
Title:Phase I study of Navitoclax (ABT263), a novel Bcl2 family inhibitor, in patients with smallcell lung cancer and other solid tumors.
Journal:J Clin Oncol
Year:2011
PMID:21282543
Trial Design
Clinical Trial Id:NCT00445198
Agent:navitoclax
Target:Bcl2like protein 2
Antiapoptotic protein BCLXL
Apoptosis regulator Bcl2
Cancer Type:advanced solid tumors
Cancer Subtype:advanced solid tumors
Therapy Type:mono
Therapeutic Combination Type:NA
Therapeutic Combination Content:NA
Study Type:a phase I doseescalation study
Key Patients Feature:in patients with relapsed or refractory SCLC and other solid tumors.
Biomarker:Progastrin releasing peptide (proGRP) was identified as a surrogate marker of Bcl2 amplification and changes correlated with changes in tumor volume.
Biomark Analysis:Progastrin releasing peptide (proGRP) was identified as a surrogate marker of Bcl2 amplification and changes correlated with changes in tumor volume.
Control Group Info:single arm
Treatment Info:Patients enrolled to intermittent dosing cohorts received navitoclax on day 3, follotheyd by dosing on days 1 to 14 of a 21day cycle. Patients on continuous dosing received a 1week leadin dose of 150 mg follotheyd by continuous daily administration.
Primary End Point:safety (with particular attention to platelet dynamics), pharmacokinetics, and preliminary efficacy
Secondary End Point:NA
Patients Number:47
Trial Results
DLT_MTD: A leadin dose of 150 mg was chosen, as this was the dose level at which the mean maximal platelet drop of approximately 60% from baseline was expected based on observations in other concurrent studies of navitoclax as a single agent.
Objective Response Rate:NA
Disease Control Rate:One patient with SCLC had a confirmed partial response lasting longer than 2 years, and eight patients with SCLC or carcinoid had stable disease (one remained on study for 13 months).
Median Time to Progression:NA
Median PFS A vs. C:NA
Median OS A vs. C:NA
Adverse Event(agent arm):Primary toxicities included diarrhea (40%), nausea (34%), vomiting (36%), and fatigue (34%); most were grade 1 or 2. Dose and scheduledependent thrombocytopenia was seen in all patients.
Conclusions:Navitoclax is safe and well tolerated, with dosedependent thrombocytopenia as the major adverse effect. Preliminary efficacy data are encouraging in SCLC. Efficacy in SCLC and the utility of proGRP as a marker of treatment response will be further evaluated inphase II studies