ATC Group: L01EH Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors

The World Health Organization's ATC classification organizes medical drugs based on therapeutic properties, chemical composition, and anatomy. It helps make essential medicines readily available globally and is widely used in the pharmaceutical industry.

Position of L01EH in the ATC hierarchy

Level Code Title
1 L Antineoplastic and immunomodulating agents
2 L01 Antineoplastic agents
3 L01E Protein kinase inhibitors
4 L01EH Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors

Group L01EH contents

Code Title
L01EH01 Lapatinib
L01EH02
L01EH03

Active ingredients in L01EH

Active Ingredient Description
Lapatinib

Lapatinib, a 4-anilinoquinazoline, is an inhibitor of the intracellular tyrosine kinase domains of both EGFR (ErbB1) and of HER2 (ErbB2) receptors (estimated Kiapp values of 3nM and 13nM, respectively) with a slow off-rate from these receptors (half-life greater than or equal to 300 minutes). Lapatinib inhibits ErbB-driven tumour cell growth in vitro and in various animal models.

Neratinib

Neratinib is an irreversible pan–erythroblastic leukaemia viral oncogene homolog (ERBB) tyrosine kinase inhibitor (TKI) that blocks mitogenic growth factor signal transduction through covalent, high affinity binding to the ATP binding site of 3 epidermal growth factor receptors (EGFRs): EGFR (encoded by ERBB1), HER2 (encoded by ERBB2), and HER4 (encoded by ERBB4) or their active heterodimers with HER3 (encoded by ERBB3). This results in sustained inhibition of these growth promoting pathways with HER2-amplified or over-expressed, or HER2-mutant breast cancers.

Tucatinib

Tucatinib is a tyrosine kinase inhibitor of HER2. It is used in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer.

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