Lapatinib (Tykerb®/Tyverb®): A Comprehensive Oncological and Pharmacological Review

Executive Summary

Lapatinib is an orally active, small-molecule antineoplastic agent that functions as a potent and reversible dual tyrosine kinase inhibitor (TKI) of the Epidermal Growth Factor Receptor (EGFR, or ErbB1) and the Human Epidermal Growth Factor Receptor 2 (HER2, or ErbB2).[1] Developed by GlaxoSmithKline and now marketed by Novartis under the trade names Tykerb® and Tyverb®, its mechanism involves the competitive blockade of the intracellular ATP-binding site of these receptors, thereby preventing their activation and inhibiting downstream signaling pathways crucial for tumor cell proliferation and survival.[1]

The clinical utility of lapatinib is established within precisely defined subpopulations of patients with breast cancer. Its primary approved indications are as a combination therapy for patients with advanced or metastatic HER2-positive breast cancer. It is used with capecitabine for patients who have progressed on prior therapies, including an anthracycline, a taxane, and trastuzumab; with the aromatase inhibitor letrozole for postmenopausal women with hormone receptor-positive (HR+), HER2-positive disease; and, in the European Union, with trastuzumab for patients with HR-negative, HER2-positive disease that has progressed on prior trastuzumab-based regimens.[1] Pivotal trials have demonstrated its efficacy in significantly delaying disease progression in these settings.[1]