- March 15, 2022
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Brand Name :
Gleevec
Synonyms :
imatinib
Class :
Antineoplastics and Tyrosine Kinase Inhibitor
Dosage Forms & Strengths
Tablet
100mg
400mg
chronic Myelogenous leukemia (CML)
400 mg given orally per day for chronic phase
600 mg given orally per day for accelerated phase or blast crisis
An increased dose is given to patients if there is no severe adverse drug reaction or severe non-leukemia as in the below areas:
the disease progression fails to reach satisfactory hematologic response after at least three months of treatment, failure to achieve a cytogenetic response after 6-12 months of treatment or loss of a previously completed hematologic or cytogenetic response
600 mg orally once a day for disease progression chronic phase
400 mg orally two times a day for disease progression accelerated phase or blast crisis
continue the treatment until there is no progressive disease or unacceptable toxicity occurs
acute lymphoblastic leukemia(All)
600
mg
Orally
once a day
; continue the treatment until there is no progressive disease or unacceptable toxicity occurs
400
mg
Orally
once a day
; continue the treatment until there is no progressive disease or unacceptable toxicity occurs
400
mg
Orally
once a day
; continue the treatment until there is no progressive disease or unacceptable toxicity occurs occurs
400
mg
Orally
daily for patients with HES/CEL
100 mg orally given daily for patients with HES/CEL with demonstrated FIP1L1-PDGFR alpha fusion kinase
An increased dose of 100 mg to 400 mg can be considered for those patients if no adverse drug reactions are seen or if assessments demonstrate an insufficient response to therapy
continue the treatment until there is no progressive disease or unacceptable toxicity occurs
400 mg orally daily for patients with HES/CEL
100 mg orally given daily for patients with HES/CEL with demonstrated FIP1L1-PDGFR alpha fusion kinase
An increased dose of 100 mg to 400 mg can be considered for those patients if no adverse drug reactions are seen and if assessments demonstrate an insufficient response to therapy
continue the treatment until there is no progressive disease or unacceptable toxicity occurs
dermatofibrosarcoma Protuberans
100 - mg
Orally
once a day
; continue the treatment until there is no progressive disease or unacceptable toxicity occurs
Dosage Forms & Strengths
tablet
100mg
400mg
chronic Myelogenous leukemia (CML)
Age:>1 year
340 mg per m2 given orally per day or 170 mg per m2 given orally twice a day
The maximum dose given is 600 mg daily
continue the treatment until there is no progressive disease or unacceptable toxicity occurs
Age: <1year
Safety and efficacy not established
acute lymphoblastic leukemia(All)
Age:>1 year
340 mg per m2 given orally per day or 170 mg per m2 given orally twice a day
The maximum dose given is 600 mg daily
continue the treatment until there is no progressive disease or unacceptable toxicity occurs
Age: <1year <
Safety and efficacy not established
Refer adult dosing
when both drugs are combined, there may be an increased effect of cobimetinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of conivaptan by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of dihydroergotamine by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of dihydroergotamine intranasal by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of flibanserin by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of cobimetinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of ivabradine by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of lomitapide by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of lonafarnib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of lurasidone by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of naloxegol by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of regorafenib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of venetoclax by affecting hepatic or intestinal enzyme cyp3a4 metabolism
may diminish the serum concentration when combined with imatinib
may enhance the QTc-prolonging effect of each other when combined
when both drugs are combined, there may be an increased effect of acalabrutinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of ado-trastuzumab emtansine by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased risk of adverse effects
when both drugs are combined, there may be an increased effect of apalutamide by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of avanafil by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of avapritinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of axitinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of bedaquiline by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of bosutinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of brigatinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased effect of cabazitaxel by affecting hepatic or intestinal enzyme cyp3a4 metabolism
It may enhance when combined with oxycodone by affecting CYP3A4 metabolism
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
the effect of imatinib is increased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of imatinib
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may enhance the serum concentration of tafamidis
when both drugs are combined, there may be an increased effect of abemaciclib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be a decreased levels of acetaminophen by decreasing hepatic clearance
when both drugs are combined, there may be a decreased levels of acetaminophen iv by decreasing hepatic clearance
when both drugs are combined, there may be an increased risk of adverse effects
when both drugs are combined, there may be a decreased level or effect of imatinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
imatinib: they may diminish the serum concentration of CYP3A4 Inducers
imatinib: they may diminish the serum concentration of CYP3A4 Inducers
imatinib: they may diminish the serum concentration of CYP3A4 Inducers
imatinib: they may diminish the serum concentration of CYP3A4 Inducers
imatinib: they may diminish the serum concentration of CYP3A4 Inducers
It may enhance the effect when combined with tafamidis meglumine
when bromazepam and imatinib are used together, there is a potential reduction in the bromazepam's metabolism
when both drugs are combined, there may be a decreased metabolism of etoposide
when both the drugs are combined, the risk or severity of adverse effects increases
when both drugs are combined, there may be an increased risk or severity of adverse effects
when both drugs are combined, there may be an increased risk or severity of adverse effects
is having a negative effect over brentuximab vedotin, by showing altered intestinal/hepatic CYP3A4 enzyme metabolism.
when both drugs are combined, there may be an increased effect of abemaciclib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
it enhances by affecting the hepatic enzyme CYP2C9 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
it increases by affecting the hepatic enzyme CYP3A4 metabolism
may enhance the serum concentration of CYP3A4 inhibitors
may increase the hepatotoxic effect of acetaminophen
may increase the risk or severity of toxic effects when combined
may have an increased hepatotoxic effect when combined with imatinib
acetaminophen: they may increase the hepatotoxic effect of imatinib
imatinib, when taken with ixazomib, alters the intestinal/hepatic CYP3A4 enzyme metabolism
The actions of imatinib include:
Inhibition of tyrosine kinase: Imatinib binds to the ATP-binding site of tyrosine kinase, preventing it from phosphorylating target proteins that lead to cancer cell growth and proliferation.
Induction of apoptosis: Imatinib triggers programmed cell death, or apoptosis, in cancer cells.
Inhibition of angiogenesis: Imatinib can prevent the formation of new blood vessels that tumors need to grow and survive.
The spectrum of imatinib includes:
Chronic Myeloid Leukemia (CML): Imatinib is the first-line treatment for CML. It is effective in indcing remission and improving overall survival in patients with CML.
Gastrointestinal stromal tumors (GISTs): Imatinib is also used to treat GISTs. It can shrink the tumors and delay disease progression.
Other cancers: Imatinib has been studied for use in other cancers such as acute lymphoblastic leukemia (ALL), myelodysplastic syndrome (MDS), and dermatofibrosarcoma protuberans (DFSP). It has shown some effectiveness in these diseases, although it is not yet approved for these indications.
Adverse drug reactions:
Frequency defined
>10%
All grades
Decreased hemoglobin
Fluid retention
Cough
Dizziness
Flatulence
Dyspepsia
Increased lacrimation
Pharyngeal pain
Pyrexia
Anorexia
Infection
Pruritus
Constipation
Dizziness
Asthenia
Hypoalbuminemia
Sinusitis
Alopecia
Decreased platelets
Increased bilirubin
Bone pain
Cough
Increased blood alkaline phosphate
Blurred vision
Decreased weight
<10%
Hyperglycemia
Dysgeusia
Rash
Constipation
Abdominal distension
Back pain
Pain in extremity
Hypokalemia
Facial edema
Dry skin
Upper abdominal pain
Peripheral neuropathy
Hypocalcemia
Paresthesia
Conjunctivitis
Palpitations
Leukopenia
Stomatitis
Photosensitivity reaction
Depression
Hemorrhage
Nasopharyngitis
≥3
Abdominal pain
Exfoliative rash
Increased ALT
Vomiting
Nausea
Blurred vision
Flatulence
<1%
Pain in extremity
Vomiting
Hypokalemia
Depression
Rash
Insomnia
Stomatitis
Back pain
Hyperglycemia
Pruritus
Hemorrhage
Dizziness
Dyspnea
Abdominal distension
Peripheral edema
Muscle spasms
Diarrhea
Periorbital edema
Decreased hemoglobin
Leukopenia
Hypocalcemia
Upper abdominal pain
Facial edema
Abdominal distension
Black Box Warning:
Black Box Warning associated with imatinib is related to its potential for causing severe liver damage.
Contraindication / Caution:
Contraindications:
Caution should be exercised in the following situations:
Pregnancy warnings:
Breastfeeding warnings:
Pregnancy Categories:
Pharmacology:
Imatinib is a tyrosine kinase inhibitor that selectively targets the BCR-ABL fusion protein, which is characteristic of chronic myeloid leukemia (CML), as well as c-Kit and PDGFRA tyrosine kinases. It was first approved by the US FDA in 2001 for the treatment of CML and later for gastrointestinal stromal tumors (GISTs).
Pharmacodynamics:
Imatinib works by binding to the ATP-binding site of the tyrosine kinase, preventing the phosphorylation of downstream signaling molecules, and thereby inhibiting the growth and survival of cancer cells that depend on these kinases for proliferation.
Pharmacokinetics:
Absorption
Imatinib is taken orally, and its absorption is not affected by food. The peak plasma concentration is reached within 2-4 hours after administration.
Distribution
Imatinib is highly protein-bound, with about 95% of the drug bound to plasma proteins. It has a large volume of distribution, indicating that it distributes extensively into tissues.
Metabolism
Imatinib is primarily metabolized by the liver, mainly through the cytochrome P450 (CYP) 3A4 enzyme. It undergoes oxidative metabolism to form an active metabolite, N-desmethyl imatinib, which also has activity against the target proteins. Imatinib also undergoes glucuronidation and sulfation.
Elimination and excretion
The elimination half-life of imatinib is around 18 hours. The drug and its metabolites are primarily eliminated in the feces, with only a small amount eliminated in the urine. The drug is eliminated mainly through biliary excretion.
Administration:
imatinib is typically taken orally in the form of tablets. The dose and duration of treatment will depend on the type and stage of cancer being treated, as well as other individual factors such as age, weight, and overall health.
Here are some general guidelines for the administration of imatinib:
imatinib should be taken with a full glass of water, either with or without food, as directed by your healthcare provider.
Do not crush or break the tablets. Swallow them whole.
If you miss a dose, take it as soon as you remember. If it is close to the time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not take a double dose to make up for a missed one.
Patient information leaflet
Generic Name: imatinib
Why do we use imatinib?
imatinib is a medication used to treat certain types of cancer, particularly chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GIST).
CML is a type of cancer that affects the blood and bone marrow and is caused by a specific genetic abnormality called the Philadelphia chromosome. Imatinib works by inhibiting the activity of an enzyme called tyrosine kinase, which is produced by the abnormal gene. This blocks the growth and division of cancer cells in the bone marrow.
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