Small-molecule inhibitors of the human epidermal receptor family

Corey A. Carter, Ronan J. Kelly, Giuseppe Giaccone

Research output: Contribution to journalReview articlepeer-review

24 Scopus citations


Background: Small molecule inhibitors of human epidermal receptors (HER) have become an integral part of the armamentarium available to the medical oncologist in the treatment of solid tumor malignancies. At present, there are two small-molecule inhibitors (erlotinib and lapatinib) approved by the FDA in the USA, and a third inhibitor, gefitinib, is approved in other countries. Objective: To summarize the current standards of care for these new agents in solid tumors, and to discuss ongoing clinical trials; to review the known mechanisms of action of these inhibitors as well as to discuss both the known predictive markers for response and likely mechanisms of resistance. Methods: We reviewed key presentations and recent publications on smallmolecule inhibitors targeting the HER family in solid tumors. Conclusions: Recent data have highlighted the importance of mutations and amplifications of receptors within the HER family. Amplification of HER2 often translates into responses in anti-HER2 therapy. Mutations either enhance sensitivity or confer resistance to small-molecule inhibitors. Other mechanisms of resistance are being elucidated which should lead to the ability to predict both responses and resistance to HER family inhibitors and should translate into improvements in patient care.

Original languageEnglish (US)
Pages (from-to)1829-1842
Number of pages14
JournalExpert Opinion on Investigational Drugs
Issue number12
StatePublished - Dec 2009
Externally publishedYes


  • EGFR inhibitors
  • ErbB1
  • ErbB2
  • ErbB3
  • ErbB4
  • HER family
  • HER2 inhibitors

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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