What is the mechanism of action for imatinib?

Mechanism of Action Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the bcr-abl tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML).

What is imatinib and how does it work?

Imatinib 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. This helps stop the spread of cancer cells.

What is the target of imatinib?

Imatinib. Imatinib (Gleevec) was the first drug to specifically target the BCR-ABL tyrosine kinase protein, because of this it’s known as a first-generation tyrosine kinase inhibitor. Almost all CML patients respond to treatment with imatinib, and most of these responses seem to last for many years.

Where does imatinib bind to the enzyme?

Imatinib (also called Gleevec or STI571) is a small-molecule inhibitor that binds to the kinase domain of BCR-ABL and stabilizes the protein in its closed, inactive conformation (5), thereby inhibiting its activity, and is now a first-line therapy for the majority of chronic myelogenous leukemia (CML) cases because of …

What is imatinib resistance?

Resistance to imatinib therapy can be defined as one of the following: (1) failure to achieve complete hematologic response and BCR-ABL1 transcript levels less than or equal to 10% (IS) after 3 to 6 months of therapy or partial cytogenetic response by cytogenetics after 3 to 6 months of therapy; (2) failure to achieve …

How long does imatinib stay in your system?

The chemotherapy itself stays in the body within 2 -3 days of treatment but there are short-term and long-term side effects that patients may experience. Not all patients will experience all side effects but many will experience at least a few.

What are side effects of imatinib?

Side Effects Upset stomach, nausea/vomiting, diarrhea, headache, muscle/joint pain, muscle cramps, dizziness, blurred vision, or drowsiness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Is dasatinib better than imatinib?

Dasatinib is 325 times as potent as imatinib in inhibiting unmutated BCR-ABL kinase in vitro. Since increased inhibition of BCR-ABL kinase correlates with a better clinical response,18 administration of dasatinib as the initial therapy may improve responses in patients with newly diagnosed chronic-phase CML.

Does imatinib lower immune system?

Low doses of the anti-cancer drug imatinib can spur the bone marrow to produce more innate immune cells to fight against bacterial infections, Emory researchers have found.

How is imatinib an example of rational drug design?

Imatinib also inhibits the receptor tyrosine kinases for platelet derived growth factor (PDGF) and stem cell factor (SCF) – called c-kit. Imatinib was identified in the late 1990s by Dr Brian J. Druker. Its development is an excellent example of rational drug design.

How is metoprolol related to drug induced liver injury?

Metoprolol has been linked to rare cases of drug induced liver injury. Metoprolol is a propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.

What is the mechanism of action of imatinib?

Imatinib is a Kinase Inhibitor. The mechanism of action of imatinib is as a Protein Kinase Inhibitor. Anatomical main group: L – Antineoplastic and immunomodulating agents Therapeutic subgroup: L01 – Antineoplastic agents Pharmacological subgroup: L01X – Other antineoplastic agents Chemical subgroup: L01XE – Protein kinase inhibitors

What are the side effects of oral metoprolol?

Other GI symptoms such as nausea, gastric pain, constipation, flatulence, digestive tract disorders, heartburn, xerostomia, and hiccups also have been reported with oral metoprolol therapy. Nausea and abdominal pain have occurred in less than 1% of patients with myocardial infarction receiving IV or oral metoprolol.