What is imatinib and how does it work?
Imatinib is an oral medication used for treating chronic myeloid leukemia and acute lymphoblastic leukemia. It is classified as a kinase inhibitor. It is classified as a kinase inhibitor. Kinase inhibitors include dasatinib ( Sprycel ), erlotinib ( Tarceva ), gefitinib (Iressa), nilotinib ( Tasigna ), pazopanib (Votrient), sunitinib (Sutent), and vandetanib (Caprelsa).
Is im imatinib a kinase inhibitor?
Imatinib, sold under the brand names Gleevec and Glivec (both marketed worldwide by Novartis) among others, is an oral chemotherapy 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 +), certain types of gastrointestinal stromal tumors …
When was imatinib approved for first-line treatment of chronic myeloid leukemia (CML)?
The tyrosine kinase inhibitor Imatinib Mesylate has dramatically improved the clinical outcome of chronic myeloid leukemia (CML) patients in the chronic phase of the disease, generating unprecedented rates of complete hematologic and cytogenetic responses and sustained reductions in BCR-ABL transcripts. Here, we present an overview on the ...
What drugs can decrease the effectiveness of imatinib?
Imatinib is an antineoplastic agent and a 2-phenylaminopyrimidine derivative that is used to treat chronic myelogenous leukemia. It works as a specific inhibitor of a …
What is the mechanism of action of imatinib?
Imatinib works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [1]. This process ultimately results in “switching-off” the downstream signaling pathways that promote leukemogenesis.May 6, 2014
Which mechanism of action for imatinib makes it effective in treating chronic myelogenous leukemia?
Imatinib inhibits proliferation and induces apoptosis in cells positive for BCR/ABL. For patients with chronic-phase CML, imatinib at 400 mg/day is the best dosage for primary therapy, because it induces a complete hematologic response in almost all patients and causes a high cytogenetic response rate.Nov 5, 2021
What does the drug imatinib do?
Imatinib is used alone or together with other medicines to treat different types of cancer or bone marrow conditions. It prevents or stops the growth of cancer cells and is called an antineoplastic (cancer) agent. Imatinib is used for these conditions: Aggressive systemic mastocytosis (ASM)
What type of inhibitor is imatinib?
Imatinib is a member of the class of small molecule tyrosine kinase inhibitors with selectivity for the Abl kinase. Imatinib is a potent competitive inhibitor of ATP binding to Abl kinase, as well as to the c-Kit and PDGF receptor tyrosine kinases.
Can imatinib cure leukemia?
Abstract. Imatinib mesylate has transformed the treatment for chronic myeloid leukemia (CML). The vast majority of patients obtain hematologic remission, with a low probability of progression of disease. Yet imatinib rarely cures CML, and current recommendations dictate lifelong treatment with imatinib.
What are the side effects of imatinib?
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. People using this medication may have serious side effects.
What is imatinib target?
Imatinib (Gleevec) was the first drug to specifically target the BCR-ABL tyrosine kinase protein. Almost all CML patients respond to treatment with imatinib, and most of these responses seem to last for many years.Nov 24, 2021
How effective is imatinib?
Among the patients in the imatinib group, the estimated overall survival rate at 10 years was 83.3%. Approximately half the patients (48.3%) who had been randomly assigned to imatinib completed study treatment with imatinib, and 82.8% had a complete cytogenetic response.Mar 9, 2017
Is imatinib an immunosuppressant?
The drug does so by stimulating the bone marrow to make more neutrophils and macrophages, immune cells that are important for resisting bacterial infection. "This was surprising because there are reports that imatinib can be immunosuppressive in some patients," Kalman says.Apr 1, 2015
How is imatinib administered?
The prescribed dose should be administered orally, with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day.
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 made of?
Imatinib 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.
When was imatinib approved?
By reducing the activity of these proteins, growth and survival of cancer cells are reduced. The FDA approved imatinib in April 2003.
What is gleevec used for?
Imatinib (Gleevec) is a kinase inhibitor prescribed for the treatment of chronic myeloid leukemia and acute lymphoblastic leukemia. Side effects, drug interactions, dosing information, and warnings and precautions should be reviewed prior to taking any medication.
What is imatinib used for?
Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malign ancies. In 2006 the FDA expended approved use to include Dermatofibrosarcoma protuberans (DFSP), Myelodysplastic /myeloproliferative diseases (MDS/MPD), Aggressive systemic mastocytosis (ASM).
How does imatinib work?
Imatinib works by stopping the Bcr-Abl tyrosine-kinase. This can slow growth or result in programmed cell death of certain types of cancer cells. Imatinib was approved for medical use in the United States in 2001. It is on the World Health Organization's List of Essential Medicines.
What are the risks of imatinib?
The only known contraindication to imatinib is hypersensitivity to imatinib. Cautions include: 1 Hepatic impairment 2 Risk of severe CHF or left ventricular dysfunction, especially in patients with comorbidities 3 Pregnancy, risk of embryo-fetal toxicity 4 Risk of fluid retention 5 Risk of growth stunting in children or adolescents
When was imatinib first used?
Imatinib was invented in the late 1990s by scientists at Ciba-Geigy (which merged with Sandoz in 1996 to become Novartis ), in a team led by the British biochemist Nicholas Lydon and that included Elisabeth Buchdunger and Jürg Zimmermann, and its use to treat CML was driven by oncologist Brian Druker of Oregon Health & Science University (OHSU). Other major contributions to imatinib development were made by Carlo Gambacorti-Passerini, a physician, scientist, and hematologist at the University of Milano Bicocca, Italy, John Goldman at Hammersmith Hospital in London, and later on by Charles Sawyers of Memorial Sloan Kettering Cancer Center in New York.
What is the FDA approved for imatinib?
The FDA has approved imatinib for use in adults with relapsed or refractory Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), myelodysplastic / myeloproliferative diseases associated with platelet-derived growth factor receptor gene rearrangements, aggressive systemic mastocytosis without or an unknown D816V c-KIT mutation, hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (CHIC2 allele deletion) or FIP1L1-PDGFRα fusion kinase negative or unknown, unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. On 25 January 2013, Gleevec was approved for use in children with Ph+ ALL.
Is imatinib an inhibitor of PDGFR?
As an inhibitor of PDGFR, imatinib mesylate appears to have utility in the treatment of a variety of dermatological diseases. Imatinib has been reported to be an effective treatment for FIP1L1-PDGFRalpha+ mast cell disease, hypereosinophilic syndrome, and dermatofibrosarcoma protuberans.
What is imatinib a derivative of?
Imatinib 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.
What is imatinib used for?
Imatinib is an antineoplastic agent and a 2-phenylaminopyrimidine derivative that is used to treat chronic myelogenous leukemia. It works as a specific inhibitor of a number of tyrosine kinase enzymes.
How long does it take for imatinib to be eliminated?
Imatinib elimination is predominately in the feces, mostly as metabolites. 81% of the dose is eliminated within 7 days, in feces (68% of the dose) and urine (13% of the dose). Unchanged imatinib accounted for 25% of the dose (5% urine, 20% faces), the remainder being metabolites. Half-life.
What is the name of the drug that Novartis is using to treat cancer?
It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally referred to as CGP57148B or STI571 (especially in older publications).
What is imatinib mesylate?
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 abnormal ity in chronic myeloid leukemia (CML).
What is the cytochrome P450 2C19?
Cytochrome P450 2C19. Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im... Details 8. Prostaglandin G/H synthase 1.
What is the best treatment for acute lymphocytic leukemia?
Intrathecal methotrexate is generally the preferred treatment option for patients with acute lymphocytic leukemia, because it is most commonly associated with CNS involvement. Autologous hematopoietic stem cell transplantation (HSCT) is used as a treatment option for patients with acute myelogenous leukemia.
What is the temperature of a neutropenic patient?
Neutropenic fever (greater than 100.4° F [38.1° C]) in a severely neutropenic patient is a medical emergency.
What are the complications of thrombocytopenia?
This occurs due to a decreased number of platelets in blood, which results in excessive bleeding. Fatigue, weakness, and abdominal pain are minor complications of thrombocytopenia.
What is the normal platelet count?
The normal platelet count is in the range of 150,000 to 450,000 platelets/mcL of blood. A decreased blood platelet count indicates thrombocytopenia in the patient. A patient with ITP will have thrombocytopenia because of decreased platelet production.
What does low platelet count mean?
Lightheadedness and nausea. A low platelet count, known as thrombocytopenia, may be accompanied by signs of hemorrhage, such as bruising and petechiae. A normal platelet count is 150,000 to 400,000/mm3. The symptoms listed in the other answer options are not directly associated with thrombocytopenia.
What is Danazol used for?
Danazol is an androgen, which is used along with corticosteroids in some patients with immune thrombocytopenic purpura (ITP). Cyclosporine is used to suppress the immune system in patients with ITP. Protamine sulfate reverses the effects of heparin and is used in the treatment of heparin-induced thrombocytopenia (HIT).
What does a nurse note in a history of an older patient?
The nurse reviews the history of an older patient and notes increased fatigue, headache, pale skin, and glossitis. The nurse suspects the patient has microcytic, hypochromic anemia and should provide what teaching?