Antitumor activity of HER-2 inhibitors.
Activation of intracellular mitogenic signal transduction pathways driven by the ErbB family of receptor tyrosine kinases has been implicated in a variety of cancers. Amongst these, the tumorigenic roles of the Epidermal Growth Factor receptor (EGFR) and HER-2 have been most extensively studied. Therapeutic antibodies and small molecule kinase inhibitors targeting EGFR have recently received regulatory agency approval for the treatment of colon and lung cancer, respectively. In this review, I briefly describe these agents and their potential use in inhibiting the growth of tumors that overexpress HER-2. I also discuss other therapeutics currently available or being developed specifically to target HER-2 dependent tumors.
Rabindran
Sridhar K
SK
Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. rabinds@wyeth.com
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D019008:Drug Resistance, Neoplasm; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D006801:Humans; D047908:Intracellular Signaling Peptides and Proteins / Q000627:therapeutic use*; D000077341:Lapatinib; D009369:Neoplasms / Q000188:drug therapy; D011743:Pyrimidines / Q000627:therapeutic use; D011758:Pyrroles / Q000627:therapeutic use; D011799:Quinazolines / Q000627:therapeutic use; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000032:analysis / Q000037:antagonists & inhibitors* / Q000502:physiology
D000970:Antineoplastic Agents; D066246:ErbB Receptors; D047908:Intracellular Signaling Peptides and Proteins; D000077341:Lapatinib; D011743:Pyrimidines; D011758:Pyrroles; D011799:Quinazolines; D018719:Erb-b2 Receptor Tyrosine Kinases; C015482:protein kinase modulator; C410026:PKI 166