Contents
What are tyrosine kinase inhibitors used for?
Tyrosine kinases are a part of many cell functions, including cell signaling, growth, and division. These enzymes may be too active or found at high levels in some types of cancer cells, and blocking them may help keep cancer cells from growing. Some tyrosine kinase inhibitors are used to treat cancer.
Why are tyrosine kinase inhibitors considered a targeted therapy?
TKIs come as pills, taken orally. A targeted therapy identifies and attacks specific types of cancer cells while causing less damage to normal cells. In CML, TKIs target the abnormal BCR-ABL1 protein that causes uncontrolled CML cell growth and block its function, causing the CML cells to die.
What is a EGFR tyrosine kinase inhibitor?
A substance that blocks the activity of a protein called epidermal growth factor receptor (EGFR). EGFR is found on the surface of some normal cells and is involved in cell growth.
What is EGFR TKI therapy?
Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) have been first-line therapy in the treatment of non-small cell lung cancer (NSCLC) harboring EGFR sensitive mutations.
How do EGFR inhibitors work?
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. EGFR is a protein that is found on the surface of some cells that causes cells to divide when epidermal growth factor binds to it.
Is TKI therapy chemotherapy?
Any drug used to treat cancer (including tyrosine kinase inhibitors or TKIs) can be considered chemo, but here chemo is used to mean treatment with conventional cytotoxic (cell-killing) drugs that mainly kill cells that are growing and dividing rapidly. Chemo was once one of the main treatments for CML.
Is TKI chemotherapy?
How do 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.
What is the role of EGFR?
Normal Function The EGFR gene provides instructions for making a receptor protein called the epidermal growth factor receptor, which spans the cell membrane so that one end of the protein remains inside the cell and the other end projects from the outer surface of the cell.
What inhibits EGFR?
Two predominant classes of EGFR inhibitors have been developed including monoclonal antibodies (mAbs) that target the extracellular domain of EGFR, such as cetuximab (Erbitux), and small molecule tyrosine kinase inhibitors (TKIs) that target the receptor catalytic domain of EGFR, such as gefitinib (Iressa) and …
How do TKI work?
TKIs are a type of targeted therapy. They work by switching off (inhibiting) the tyrosine kinase made by the BCR-ABL1 gene in leukaemia cells. This slows or stops the bone marrow from making abnormal white blood cells. It also allows the leukaemia cells to mature and die.
Who makes lapatinib?
Pharmaceutical company GlaxoSmithKline (GSK) markets the drug under the propriety names Tykerb (mostly U.S.) and Tyverb (mostly Europe and Russia).
What is the purpose of the EGFR TKI study?
The aim of the present study was to investigate the efficacy of first-line epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) treatment in elderly patients and the outcomes of subsequent salvage chemotherapy after disease progression.
What are the members of the EGFR family?
EGFR is a receptor tyrosine kinase that belongs to the EGFR family, consisting of four members: EGFR, ERBB2, ERBB3, and ERBB4.
How many adenocarcinoma patients have egfrmutation?
Data on patient age, type of tumor EGFRmutation, response to first-line EGFR-tyrosine kinase inhibitor (TKI) treatment, type of salvage chemotherapy, and efficacy of EGFR-TKI and salvage chemotherapy were collected. Results. In all, 473 of 1,230 stage IV adenocarcinoma patients had an EGFRmutation, and 330 of them received first-line TKI treatment.
How many adenocarcinoma patients are treated with TKI?
In all, 473 of 1,230 stage IV adenocarcinoma patients had an EGFRmutation, and 330 of them received first-line TKI treatment. Of the 330 patients, 160 were ≥70 years old (elderly group) and 170 were <70 years old (younger group).