
Mechanism of action
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NERLYNX is a small molecule that provides irreversible, intracellular pan-HER signaling inhibition1,9-14
Trastuzumab, pertuzumab and trastuzumab emtansine share a common target, the extracellular domains of the HER2 receptor.1,9-11 NERLYNX has a different mechanism of action.1,9,10
By irreversibly binding to the intracellular domain of all active HER receptors, HER1, HER2 and HER4, NERLYNX ensures steady and prolonged blockade of HER signalling.9-13
NERLYNX Mechanism of action video
In HER2+/HR+ patients, NERLYNX in combination with endocrine therapy addresses HER2-ER crosstalk by targeting both signalling pathways9,12,14-20
The family of human epidermal growth factor receptors (HER1, HER2, HER3 and HER4) play a central role in the pathogenesis of several cancers.14
The estrogen receptor and the HER2 signalling pathways are the dominant drivers of cell proliferation in the majority of breast cancers.16,17
While endocrine therapy blocks the estrogen signalling pathway, this can lead to crosstalk between the estrogen receptor and the HER2 receptor, which in turn can lead to upregulation of the HER2 signalling pathway.17-20
The addition of NERLYNX to endocrine therapy prevents this crosstalk, forming a dual blockade of both HER2 and ER signalling pathways, resulting in permanent inhibition of cancer cell growth.9,12,14