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.

Is Lapatinib a 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.

Is Lapatinib a small molecule inhibitor?

Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer.

Is lapatinib cytotoxic?

In conclusion, lapatinib induced cytotoxic and genotoxic effects on MDA-MB-231 cell line. However, laptinib reduced the EGFR protein expression and EGFR signals, it raised the apoptotic cells and TP53 gene signals, which triggered extensive DNA damage.

What do tyrosine kinase inhibitors do?

Tyrosine kinase inhibitors (TKIs) are a type of 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.

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 effect of ErbB2 inhibitor lapatinib on this pathway?

ErbB2 inhibition by lapatinib promotes degradation of mutant p53 protein in cancer cells.

How do tyrosine kinase receptors work?

Like the GPCRs, receptor tyrosine kinases bind a signal, then pass the message on through a series of intracellular molecules, the last of which acts on target proteins to change the state of the cell. As the name suggests, a receptor tyrosine kinase is a cell surface receptor that also has a tyrosine kinase activity.

What does tyrosine kinase do in CML?

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.

What drug class is lapatinib?

Lapatinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply.

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.

How do receptor tyrosine kinases activate G proteins?

Receptor tyrosine kinases activate heterotrimeric G proteins via phosphorylation within the interdomain cleft of Gαi.