PF-00299804, a small molecule, is an orally available irreversible pan-HER inhibitor1,2
- Found in many types of epithelial cells, the HER family of receptor tyrosine kinases, also referred to as the ErbB family, includes 4 receptors3:
- Epidermal growth factor receptor (EGFR, ErbB1)
- HER2/neu (ErbB2)
- HER3 (ErbB3)
- HER4 (ErbB4)
- HER receptors are implicated in the growth and spread of solid tumors because they regulate several important cellular processes, including growth, proliferation, differentiation, and migration3
- HER receptors often function in concert to transmit their signals, and these combinations may have implications for cancer therapies that target individual receptors3
- PF-00299804 irreversibly inhibits the kinase signaling of EGFR, ErbB2, and ErbB4 receptors1
- PF-00299804 has also been shown to block the signaling that results from all known EGFR-activating mutations that may result from previous cancer therapy1
Learn more about clinical trials involving PF-00299804.
PF-00299804 is an investigational compound.
Information in the Oncology Investigational Pipeline relates to therapies currently being researched.
References: 1. Data on file. Pfizer Inc, New York, NY. 2. Schellens JH, Britten CD, Camidge DR, et al. First-in-human study of the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of PF-00299804, a small molecule irreversible panHER inhibitor in patients with advanced cancer. Presented at: 43rd Annual Meeting of the American Society of Clinical Oncology (ASCO); June 1-5, 2007; Chicago, Ill. Abstract 3599. 3. Britten CD. Targeting ErbB receptor signaling: a pan-ErbB approach to cancer. Mol Cancer Ther. 2004;3:1335-1342. 4. Pollak MN, Lacy MQ, Lipton A, et al. Pharmacodynamic properties of the anti-IGF-IR monoclonal antibody CP-751,871 in cancer patients. Presented at: 43rd Annual Meeting of the American Society of Clinical Oncology (ASCO); June 1-5, 2007; Chicago, Ill. Abstract 3587. 5. Cohen BD, Baker DA, Soderstrom C, et al. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871. Clin Cancer Res. 2005;11:2063-2073.
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