Pharmacology of Imatinib Gleevec Overview Pharmacokinetics Mechanism of action Uses Effects

>> YOUR LINK HERE: ___ http://youtube.com/watch?v=B2CQOJAJJc0

Imatinib, sold under the brand names Gleevec and Glivec, is a targeted therapy medication used to treat various cancers, including chronic myeloid leukemia (CML), gastrointestinal stromal tumors (GISTs), and certain other malignancies. Here are some key points about its pharmacology: • Mechanism of Action • Imatinib is a tyrosine kinase inhibitor that works by blocking the activity of specific enzymes called tyrosine kinases. Its main targets include: • ABL kinase: Inhibits the Bcr-Abl tyrosine kinase, which is responsible for the uncontrolled growth of cancer cells in CML. • KIT: Inhibits the stem cell growth factor receptor, which is involved in GISTs and other cancers. • PDGFR: Inhibits the platelet-derived growth factor receptor, which is involved in various cancers. • Pharmacokinetics • Absorption: Imatinib is well absorbed after oral administration, with an absolute bioavailability of 98%. • Distribution: It has a large volume of distribution, allowing it to reach various tissues. • Metabolism: Primarily metabolized in the liver by cytochrome P450 enzymes, particularly CYP3A4. • Excretion: Excreted mainly in the feces (68%) and to a lesser extent in the urine (13%). • Half-Life: The terminal half-life of imatinib is approximately 18 hours, while its active metabolite has a half-life of about 40 hours. • Clinical Use • Imatinib is used to treat: • Chronic Myeloid Leukemia (CML): Both chronic and accelerated phases, as well as blast crisis. • Gastrointestinal Stromal Tumors (GISTs): Both unresectable and metastatic cases. • Other Conditions: Including dermatofibrosarcoma protuberans (DFSP), myelodysplastic/myeloproliferative diseases (MDS/MPD), aggressive systemic mastocytosis (ASM), and hypereosinophilic syndrome (HES). • Side Effects • Common side effects include: • Gastrointestinal Issues: Nausea, vomiting, diarrhea. • Musculoskeletal Pain: Muscle pain and joint pain. • Neurological Effects: Headache. • Severe Side Effects: Fluid retention, gastrointestinal bleeding, bone marrow suppression, liver problems, and heart failure • #Imatinib

#############################

New on site