Veenat

NATCO PHARMA LTD

GENERIC NAME : IMATINIB MESYLATE TAB 100MG

What is Veenat 100 mg and why it is prescribed ?

Veenat 100 mg, sold under the brand names Veenat 100mg , is a medication used to treat cancer. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph ) and certain types of gastrointestinal stromal tumors (GIST), systemic mastocytosis and myelodysplastic syndrome It is taken by mouth.

Its is prescribed to patients having:

• Chronic myelogenous leukemia
• Gastrointestinal stromal tumors

How Veenat 100mg works ?

Veenat 100 mg is a 2-phenyl amino pyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes. It occupies the TK active site, leading to a decrease in activity.There are a large number of TK enzymes in the body, including the insulin receptor. Veenat 100 mg is specific for the TK domain in abl (the Abelson proto-oncogene), c-kit and PDGF-R (platelet-derived growth factorreceptor).

In chronic myelogenous leukemia, the Philadelphia chromosome leads to a fusion protein of abl with bcr(breakpoint cluster region), termed bcr-abl. As this is now a constitutively active tyrosine kinase, Veenat 100 mg is used to decrease bcr-abl activity.

The active sites of tyrosine kinases each have a binding site for ATP. The enzymatic activity catalyzed by a tyrosine kinase is the transfer of the terminal phosphate from ATP to tyrosine residues on its substrates, a process known as protein tyrosine phosphorylation. Veenat 100 mg works by binding close to the ATP binding site of bcr-abl, locking it in a closed or self-inhibited conformation, and therefore inhibiting the enzyme activity of the protein semi-competitively. This fact explains why many BCR-ABL mutations can cause resistance to Veenat 100 mg by shifting its equilibrium toward the open or active conformation.

Veenat 100 mg is quite selective for bcr-abl, though it does also inhibit other targets mentioned above (c-kit and PDGF-R), as well as ABL2 (ARG) and DDR1 tyrosine kinases and NQO2 – an oxidoreductase. Veenat 100 mg also inhibits the abl protein of non-cancer cells, but these cells normally have additional redundant tyrosine kinases, which allows them to continue to function even if abl tyrosine kinase is inhibited. Some tumor cells, however, have a dependence on bcr-abl. Inhibition of the bcr-abl tyrosine kinase also stimulates its entry in to the nucleus, where it is unable to perform any of its normal anti-apoptopicfunctions, leading to tumor cell death.

Various Contradictions of Veenat 100 mg :

• Hepatic impairment
• Risk of severe CHF or left ventricular dysfunction, especially in patients with comorbidities
• Pregnancy, risk of embryo-fetal toxicity
• Risk of fluid retention
• Risk of growth stunting in children or adolescents