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IMPORTANT: the information on this website is based on the European Summary of Product Characteristics. Prescribing Information and indication may vary per country. You must refer to your country prescribing information. Please be aware we do not take responsibility for accessing such information which may not comply with the regulation or usage in your country.

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https://www.pierre-fabre.com/en
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heading-Nerlynx-Neratinib--HER2-Breast-Cancer

Mechanism of action

Reading time: 2 min

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 MOA.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

HER, human epidermal growth factor receptor; MOA, mechanism of action. 

 

 

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This is a simplified illustration of the mechanism of action.

This is a simplified illustration of the mechanism of action.

NERLYNX Mechanism of action video

 

In HER2+/HR+ patients, NERLYNX in combination with endocrine therapy addresses HER-ER crosstalk by targeting both signalling pathways9,12,14-20

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Nerlynx-Neratinib--HER2-Breast-Cancer-Mechanism-of-action-2

This is a simplified illustration of the mechanism of action, that only features one of the HER receptors, HER2.

 

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 hormone therapy blocks the estrogen signalling pathway, this can lead to crosstalk between the estrogen receptor and the HER receptor, which in turn can lead to upregulation of the HER signalling pathway.17-20

The addition of NERLYNX to hormone therapy prevents this crosstalk, forming a dual blockade of both HER and ER signalling pathways, resulting in permanent inhibition of cancer cell growth.9,12,14

ER, estrogen receptor; HER, human epidermal growth factor receptor.

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