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Lapatinib as a Chemotherapeutic Drug

[ Vol. 4 , Issue. 3 ]


Oluwakemi Obajimi   Pages 216 - 226 ( 11 )


Human epidermal growth factor receptor (HER) signaling is frequently associated with the development and progression of several types of cancers. Both the MAPK and the PI3K/Akt pathways have been implicated as effectors of HER signaling by promoting anti-apoptotic and pro-proliferative effects in cancer cells. As a result, many anti-HER drugs have been developed and patented for use in cancer therapy. One such drug that was recently approved for clinical trials is lapatinib (Tykerb, GW572016). Lapatinib is a small molecule inhibitor that is active at the ATP binding site of the tyrosine kinase involved in HER signaling. Importantly, this drug has dual specificity acting at the ATP binding sites of both HER-2 and HER-1 (EGFR). This review therefore summarizes the current knowledge based on pre-clinical and clinical evidence of the therapeutic effects of lapatinib against cancer and the promising strategy of combination therapy with the possibility of circumventing the problems of drug resistance commonly faced by chemotherapeutic drugs.


ErbB1, EGFR, ErbB2, HER-2, lapatinib, GW572016, cancer treatment, PI3K, Akt, MAPK


University of Medicine and Dentistry of New Jersey, Robert Wood Johnson Medical School, 401 Haddon Avenue, Camden, NJ 08103, USA.

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