Lapatinib
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Lapatinib. / Nolting, Minna; Schneider-Merck, Tanja; Trepel, Martin.
In: Recent Results Cancer Res, Vol. 201, 2014, p. 125-43.Research output: SCORING: Contribution to journal › SCORING: Review article › Research
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TY - JOUR
T1 - Lapatinib
AU - Nolting, Minna
AU - Schneider-Merck, Tanja
AU - Trepel, Martin
PY - 2014
Y1 - 2014
N2 - The human epidermal growth factor receptor (HER) family of receptor tyrosine kinases plays an important role in the biology of many cancers. In breast and gastric cancer, and maybe also additional tumor types, HER2 and its homo- or heterodimerization with HER1 or HER3 are essential for cancer cell growth and survival. Breast cancer patients overexpressing HER2 have a poor prognosis, which can be substantially improved upon HER2-targeted therapy using the monoclonal antibody trastuzumab. Lapatinib is a dual tyrosine kinase inhibitor (TKI), blocking HER1 and HER2 tyrosine kinase activity by binding to the ATP-binding site of the receptor's intracellular domain. This results in the inhibition of tumor cell growth. In patients, the drug is relatively well tolerated with mostly low-grade adverse effects. In particular and unlike to trastuzumab, it has very little, if any, adverse effects on cardiac function. In 2007, lapatinib has been approved in combination with capecitabine in patients with advanced HER2-positive breast cancer upon progressive disease following standard therapy with anthracyclines, taxanes, and trastuzumab. In 2010, the approval was extended to the treatment of postmenopausal women with advanced, hormone receptor- and HER2-positive breast cancer, for whom hormonal therapy is indicated. Ongoing and future studies will explore its role in the (neo)adjuvant therapy setting, in further drug combinations as well as in the treatment of HER2-positive tumors other than breast cancer.
AB - The human epidermal growth factor receptor (HER) family of receptor tyrosine kinases plays an important role in the biology of many cancers. In breast and gastric cancer, and maybe also additional tumor types, HER2 and its homo- or heterodimerization with HER1 or HER3 are essential for cancer cell growth and survival. Breast cancer patients overexpressing HER2 have a poor prognosis, which can be substantially improved upon HER2-targeted therapy using the monoclonal antibody trastuzumab. Lapatinib is a dual tyrosine kinase inhibitor (TKI), blocking HER1 and HER2 tyrosine kinase activity by binding to the ATP-binding site of the receptor's intracellular domain. This results in the inhibition of tumor cell growth. In patients, the drug is relatively well tolerated with mostly low-grade adverse effects. In particular and unlike to trastuzumab, it has very little, if any, adverse effects on cardiac function. In 2007, lapatinib has been approved in combination with capecitabine in patients with advanced HER2-positive breast cancer upon progressive disease following standard therapy with anthracyclines, taxanes, and trastuzumab. In 2010, the approval was extended to the treatment of postmenopausal women with advanced, hormone receptor- and HER2-positive breast cancer, for whom hormonal therapy is indicated. Ongoing and future studies will explore its role in the (neo)adjuvant therapy setting, in further drug combinations as well as in the treatment of HER2-positive tumors other than breast cancer.
KW - Animals
KW - Antineoplastic Agents
KW - Breast Neoplasms
KW - Female
KW - Humans
KW - Neoplasms
KW - Protein Kinase Inhibitors
KW - Quinazolines
KW - Receptor, Epidermal Growth Factor
KW - Journal Article
KW - Review
U2 - 10.1007/978-3-642-54490-3_7
DO - 10.1007/978-3-642-54490-3_7
M3 - SCORING: Review article
C2 - 24756789
VL - 201
SP - 125
EP - 143
JO - Recent Results Cancer Res
JF - Recent Results Cancer Res
SN - 0080-0015
ER -