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Glivec: Full Drug Profile

Medically reviewed by Dr. Otari Nergadze, Neurosurgeon | Updated: January 2026

Glivec - General Information

Glivec is a drug used to treat certain types of 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). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.
It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.

 

Pharmacology of Glivec

Glivec is an antineoplastic agent used to treat chronic myelogenous leukemia. Glivec is a 2-phenylaminopyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes. 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 continuously active tyrosine kinase, Glivec is used to decrease Bcr-Abl activity.

 

Glivec for patients

 

Glivec Interactions

Drugs that may alter imatinib plasma concentrations

Drugs that may increase imatinib plasma concentrations:
Caution is recommended when administering Gleevec with inhibitors of the CYP3A4 family (e.g., ketoconazole, itraconazole, erythromycin, clarithromycin). Substances that inhibit the cytochrome P450 isoenzyme (CYP3A4) activity may decrease metabolism and increase imatinib concentrations. There is a significant increase in exposure to imatinib when Gleevec is coadministered with ketoconazole (CYP3A4 inhibitor).

Drugs that may decrease imatinib plasma concentrations:
Substances that are inducers of CYP3A4 activity may increase metabolism and decrease imatinib plasma concentrations. Co-medications that induce CYP3A4 (e.g., dexamethasone, phenytoin, carbamazepine, rifampin, phenobarbital or St. John's Wort) may significantly reduce exposure to Gleevec. Pretreatment of healthy volunteers with multiple doses of rifampin followed by a single dose of Gleevec, increased Gleevec oral-dose clearance by 3.8-fold, which significantly (p<0.05) decreased mean cmax and AUC(0-8). In patients where rifampin or other CYP3A4 inducers are indicated, alternative therapeutic agents with less enzyme induction potential should be considered.

Drugs that may have their plasma concentration altered by Gleevec

Gleevec increases the mean cmax and AUC of simvastatin (CYP3A4 substrate) 2- and 3.5-fold, respectively, suggesting an inhibition of the CYP3A4 by Gleevec. Particular caution is recommended when administering Gleevec with CYP3A4 substrates that have a narrow therapeutic window (e.g., cyclosporine or pimozide). Gleevec will increase plasmaconcentration of other CYP3A4 metabolized drugs (e.g., triazolo-benzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, etc.).

Because warfarin is metabolized by CYP2C9 and CYP3A4, patients who require anticoagulation should receive low-molecular weight or standard heparin.

in vitro, Gleevec inhibits the cytochrome P450 isoenzyme CYP2D6 activity at similar concentrations that affect CYP3A4 activity. Systemic exposure to substrates of CYP2D6 is expected to be increased when coadministered with Gleevec. No specific studies have been performed and caution is recommended.

in vitro, Gleevec inhibits acetaminophen O-glucuronidation (Ki value of 58.5 µM) at therapeutic levels. Systemic exposure to acetaminophen is expected to be increased when coadministered with Gleevec. No specific studies in humans have been performed and caution is recommended.

 

Glivec Contraindications

Use of Gleevec® (imatinib mesylate) is contraindicated in patients with hypersensitivity to imatinib or to any other component of Gleevec.

 

Additional information about Glivec

Glivec Indication: For the treatment of newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (CML). Also indicated for the treatment of pediatric patients with Ph+ chronic phase CML whose disease has recurred after stem cell transplant or who are resistant to interferon-alpha therapy. Also indicated with unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST). Mechanism Of Action: Glivec 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). It inhibits proliferation and induces apoptosis in Bcr-Abl positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Glivec also inhibits the receptor tyrosine kinases for platelet derived growth factor (PDGF) and stem cell factor (SCF) - called c-kit. Glivec was identified in the late 1990s by Dr Brian J. Druker. Its development is an excellent example of rational drug design. Soon after identification of the bcr-abl target, the search for an inhibitor began. Chemists used a high-throughput screen of chemical libraries to identify the molecule 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib. Drug Interactions: Acetaminophen Increased hepatic toxicity of both agentsAnisindione Glivec increases the anticoagulant effectDicumarol Glivec increases the anticoagulant effectAcenocoumarol Glivec increases the anticoagulant effectWarfarin Glivec increases the anticoagulant effectAprepitant Aprepitant may change levels of chemotherapy agentAtorvastatin Increases the effect and toxicity of atorvastatinCarbamazepine Carbamazepine decreases levels of imatinibCerivastatin Glivec increases the effect and toxicity of statinCyclosporine Glivec increases the effect and toxicity of cyclosporineDexamethasone Dexamethasone decreases levels of imatinibLovastatin Glivec increases the effect and toxicity of statinSimvastatin Glivec increases the effect and toxicity of statinSt. John's Wort St. John's Wort decreases levels of imatinibRifampin Rifampin decreases levels of imatinibPimozide Increases the effect and toxicity of pimozidePhenobarbital Phenobarbital decreases levels of imatinibNifedipine Glivec increases the effect and toxicity of nifedipineClarithromycin The macrolide increases levels of imatinibErythromycin The macrolide increases levels of imatinibJosamycin The macrolide increases levels of imatinibKetoconazole The imidazole increases the levels of imatinibItraconazole The imidazole increases the levels of imatinibEthotoin The hydantoin decreases the levels of imatinibFosphenytoin The hydantoin decreases the levels of imatinibMephenytoin The hydantoin decreases the levels of imatinibPhenytoin The hydantoin decreases the levels of imatinib Food Interactions: Take with food to reduce the incidence of gastric irritation. Follow with a large glass of water. A lipid rich meal will slightly reduce and delay absorption. Avoid grapefruit and grapefruit juice throughout treatment, grapefruit can significantly increase serum levels of this product. Generic Name: Imatinib Synonyms: Imatinib Mesylate; Imatinib Methansulfonate Drug Category: Antineoplastic Agents; Protein Kinase Inhibitors Drug Type: Small Molecule; Approved Other Brand Names containing Imatinib: Gleevec; Glivec; Absorption: Imatinib is well absorbed with mean absolute bioavailability is 98% with maximum levels achieved within 2-4 hours of dosing Toxicity (Overdose): Side effects include nausea, vomiting, diarrhea, loss of appetite, dry skin, hair loss, swelling (especially in the legs or around the eyes) and muscle cramps Protein Binding: Very high (95%) Biotransformation: Primarily hepatic via CYP3A4. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. Half Life: 18 hours for Imatinib, 40 hours for its major active metabolite, the N-desmethyl derivative Dosage Forms of Glivec: Tablet OralCapsule Oral Chemical IUPAC Name: 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide Chemical Formula: C29H31N7O Imatinib on Wikipedia: https://en.wikipedia.org/wiki/Imatinib Organisms Affected: Humans and other mammals