Target intelligence / Profile preview

Tyrosine Kinase Inhibitor

Molecular classification
Enzyme Inhibitor, Small Molecule
01

Overview

A tyrosine kinase inhibitor (TKI) is a pharmaceutical agent that blocks the activity of enzymes known as tyrosine kinases. These enzymes play a crucial role in various cellular processes, including cell signaling, growth, and division. In certain cancers, tyrosine kinases are overactive or present at abnormally high levels, contributing to uncontrolled cell proliferation. By inhibiting these enzymes, TKIs can help prevent cancer cells from growing and dividing.

Other names
TKI
02

Mechanism of action

Inhibition of tyrosine kinase phosphorylation by binding to the ATP-binding site or allosteric sites of the kinase domain.

03

Biological functions

Cell signaling modulationInhibition of cell growthInhibition of cell divisionRegulation of phosphorylation
04

Disease associations

CancerIdiopathic pulmonary fibrosis
05

Safety considerations

Skin rashCardiovascular issuesHypertensionProteinuriaStevens-Johnson syndromeResistance developmentMutations in kinase domains
06

Interacting drugs

Imatinib mesylate

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