Thalidomide analogues as anticancer drugs

Jeanny B. Aragon-Ching, Haiqing Li, Erin R. Gardner, William D. Figg*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

66 Scopus citations


The evolution of thalidomide as an effective treatment in several neoplasms has led to the search for compounds with increased antiangiogenic and anti-tumor effects, but decreased side-effects. The development of thalidomide analogues which retain the immunomodulatory effects of the parent compound, while minimizing the adverse reactions, brought about a class of agents termed the immunomodulatory drugs (IMiDs), The IMiDS have undergone significant advances in recent years as evidenced by the recent FDA-approvals of one of the lead compounds, CC-5013 (lenalidomide), for 5q- myelodysplasia and for multiple myeloma (MM). Actimid (CC-4047), another IMiD lead compound, has also undergone clinical testing in MM. Apart from hematologic malignancies, these drugs are actively under investigation in solid tumor malignancies including prostate cancer, melanoma, and gliomas, in which potent activity has been demonstrated. The preclinical and clinical data relating to these analogues, as well as ENMD-0995, are reviewed herein. Encouraging results with these thalidomide analogues brought forth synthesis and screening of additional novel thalidomide analogues in the N-substituted and tetrafluorinated classes, including CPS11 and CPS49. This review also discusses the patents and preclinical findings for these agents.

Original languageEnglish
Pages (from-to)167-174
Number of pages8
JournalRecent Patents on Anti-Cancer Drug Discovery
Issue number2
StatePublished - Jun 2007
Externally publishedYes


  • CC-4047
  • CC-5013
  • CPS11
  • CPS49
  • Lenalidomide
  • Multiple myeloma
  • Prostate cancer
  • Thalidomide analogues


Dive into the research topics of 'Thalidomide analogues as anticancer drugs'. Together they form a unique fingerprint.

Cite this