What is inhibited by lapatinib?

What is inhibited by lapatinib?

Lapatinib is an oral dual tyrosine kinase inhibitor that targets epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER2), both frequently overexpressed in human cancer.

How effective are EGFR inhibitors?

Our main finding was that the addition of EGFR MAb drugs to standard treatment in people whose tumours were KRAS wild type reduces the risk of disease progression by 30%. The risk of death is reduced by 12% (i.e. patients live longer overall), and the chance of tumour shrinkage is increased from 31% to 46%.

How long do EGFR inhibitors work?

EGFR inhibitors that target cells with the T790M mutation EGFR inhibitors can often shrink tumors for several months or more. But eventually these drugs stop working for most people, usually because the cancer cells develop another mutation in the EGFR gene. One such mutation is known as T790M.

What drugs are anti EGFR?

Currently, there are five FDA-approved drugs that inhibit EGFR: 3 TKIs (erlotinib [Tarceva, Genentech, South San Francisco, CA/OSI Pharmaceuticals, Melville, NY], gefitinib [Iressa, AstraZeneca, Wilmington, DE], and lapatinib [Tykerb, GlaxoSmithKline, Middlesex, England]) and two mAbs (cetuximab [Erbitux, ImClone …

Is lapatinib a monoclonal antibody?

Unlike the large monoclonal antibodies targeting the Her2 pathway, lapatinib is able to cross the blood–brain barrier and has demonstrated activity in patients with brain metastasis.

Is lapatinib tyrosine kinase inhibitor?

Lapatinib is a human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor (TKI) that has clinical activity in HER2-amplified breast cancer. In vitro studies have shown that lapatinib enhances the effects of the monoclonal antibody trastuzumab suggesting partially non-overlapping mechanisms of action.

What is EGFR inhibitor therapy?

What are EGFR inhibitors? Epidermal growth factor receptor (EGFR, also known as ErbB-1 or HER-1) inhibitors are medicines that bind to certain parts of the EGFR and slow down or stop cell growth.

How does EGFR TKI work?

The working mechanism of first-generation EGFR-TKIs is to block the activation of downstream signaling induced by EGFR through binding to the ATP-binding sites.

Why does Tagrisso stop working?

Recent clinical research has shown that some EGFR+ patients who develop Tagrisso resistance also may develop a new mutation in their tumor that may play a role in Tagrisso no longer working.

How common are EGFR mutations in Nsclc?

Introduction. Activating mutations in the epidermal growth factor receptor (EGFR) gene occur in 10–20% of Caucasian and at least 50% of Asian non-small cell lung cancer (NSCLC) patients [[1], [2], [3], [4]].

How does anti EGFR therapy work?

Its main pharmacological mechanism is to inhibit the phosphorylation of EGFR tyrosine kinase caused by the ligands binding and then block a series of reactions such as gene transcription and cell proliferation induced by the activation of the phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) …

What is lapatinib used for?

Generic Name: lapatinib Lapatinib is used to treat a certain type of breast cancer (HER2-positive). It works by slowing or stopping the growth of cancer cells.