Evaluation of the pharmacokinetics, preclinical, and clinical efficacy of lenalidomide for the treatment of multiple myeloma

Expert Opin Drug Metab Toxicol. 2012 Sep;8(9):1209-22. doi: 10.1517/17425255.2012.712685. Epub 2012 Aug 3.


Introduction: Lenalidomide is an oral immunomodulatory drug, which was recently introduced for the treatment of multiple myeloma (MM). It has been used for the treatment of newly diagnosed and relapsed MM patients, as both maintenance and preventive therapy. Available data show a progression-free survival and overall survival improvement associated with this drug.

Areas covered: Efficacy results of lenalidomide in Phase I, II, and III trials in MM are reported herein. The recent use of lenalidomide as maintenance and preventive therapy is described. An overview of the most important adverse events is also presented, such as myelosuppression, thromboembolic events, fatigue, dermatologic toxicity, infections, teratogenic potential, and second primary malignancies. The literature reviewed consists of clinical trials published from 2001 to 2012.

Expert opinion: Lenalidomide is one of the most important therapeutic agents for MM treatment. Various trials have confirmed its remarkable anticancer activity, alone or combined with high- or low-dose dexamethasone, or other drugs. Lenalidomide-related adverse events can be controlled with dose reductions, supportive therapy, and appropriate prophylaxis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Clinical Trials as Topic
  • Dexamethasone / therapeutic use
  • Disease-Free Survival
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Drug Interactions
  • Humans
  • Immunologic Factors / pharmacokinetics*
  • Immunologic Factors / therapeutic use*
  • Lenalidomide
  • Multiple Myeloma / drug therapy*
  • Thalidomide / analogs & derivatives*
  • Thalidomide / pharmacokinetics
  • Thalidomide / therapeutic use


  • Immunologic Factors
  • Thalidomide
  • Dexamethasone
  • Lenalidomide