Logo image
Pharmacodynamic study of axitinib in patients with advanced malignancies assessed with F-18-3'deoxy-3'fluoro-L-thymidine positron emission tomography/computed tomography
Journal article   Peer reviewed

Pharmacodynamic study of axitinib in patients with advanced malignancies assessed with F-18-3'deoxy-3'fluoro-L-thymidine positron emission tomography/computed tomography

Justine Yang Bruce, Peter Colin Scully, Lakeesha L. Carmichael, Jens C. Eickhoff, Scott B. Perlman, Jill Marie Kolesar, Jennifer L. Heideman, Robert Jeraj and Glenn Liu
Cancer chemotherapy and pharmacology, Vol.76(1), pp.187-195
07/01/2015
DOI: 10.1007/s00280-015-2779-7
PMCID: PMC4499265
PMID: 26021741
url
https://www.ncbi.nlm.nih.gov/pmc/articles/4499265View
Open Access

Abstract

Rapid disease progression associated with increased tumor proliferation has been observed during withdrawal of anti-angiogenic therapy. We characterize the dynamics of withdrawal flare for axitinib. Thirty patients with metastatic solid malignancies received axitinib for 2 weeks, followed by a 1-week drug holiday. Twenty patients suitable for PET imaging received scans with F-18-3'deoxy-3'fluoro-l-thymidine (FLT), a marker of proliferation. Plasma VEGF and axitinib pharmacokinetic levels were also assessed at specified time points. During axitinib withdrawal, significant increases in both SUVmax (+22 %; p = 0.006) and SUVmean (+20 %; p = 0.001) were observed. Significant increases relative to peak axitinib concentration were observed at day 2 withdrawal for SUVmax and SUVmean, with no further significant increase from day 2 to day 7 of withdrawal. No significant change in SUVmax or SUVmean was observed during the treatment period, relative to baseline. VEGF concentration significantly increased when on drug (p < 0.001) and decreased back to a level indistinguishable from baseline by day 7 of drug washout (p = 0.448). No correlation between change in VEGF and change in imaging metrics was observed. A significant increase in tumor proliferation was observed during withdrawal of axitinib therapy, and this flare occurred within 2 days of axitinib withdrawal. An exploratory analysis indicated that this flare may be associated with poor clinical outcome.
Life Sciences & Biomedicine Oncology Pharmacology & Pharmacy Science & Technology

Details

Metrics

Logo image