Imatinib pharmacokinetics and its correlation with response plasma exposure of imatinib and its correlation with clinical response in the tyrosine kinase inhibitor optimization and selectivity trial.
Larson RA, Druker BJ, Guilhot F, et al. Blood. 2008;111:4022-28.
This phase III randomized study demonstrated that patients who achieved complete cytogenetic response had significantly higher imatinib trough (or Cmin) levels than those who did not. Plasma trough levels of imatinib were a significant prognostic covariate for midterm and long term clinical response: complete cytogenetic response, major molecular response and event-free survival. Patients with the lowest imatinib levels more frequently discontinued imatinib for “unsatisfactory therapeutic effect”.