Imatib 100 Capsules
Imatinib Mesilate 100 mg
What it does
Imatinib is a medication used to treat certain types of cancer by blocking specific signals that allow cancer cells to grow.
Commonly used for: chronic myeloid leukaemia (CML), gastrointestinal stromal tumors (GIST), other cancers as determined by a doctor
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Sourcing - Kenya onlyRegistration & product details
Source: Zambia Medicines Regulatory Authority · fetched 2026-03-12 00:05:29 · updated 2026-10-01 03:39:11
Drug Interactions
148Pharmacodynamic Warnings
Imatinib appears in TABLE 4: Drugs with antiplatelet effects
Imatinib appears in TABLE 15: Drugs that cause myelosuppression
Severe (2)
Antipsychotics, Second Generation - increases exposure
Imatinib is predicted to increase the exposure to antipsychotics, second generation (cariprazine). Avoid.
Imatinib - decreases exposure
Antiepileptics (carbamazepine, fosphenytoin, oxcarbazepine, phenobarbital, phenytoin, primidone) are predicted to decrease the exposure to imatinib. Avoid.
Moderate (34)
Alfentanil - increases exposure
Imatinib is predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Amlodipine - increases exposure
Imatinib is predicted to increase the exposure to calcium channel blockers (amlodipine, felodipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine). Monitor and adjust dose.
Atorvastatin - increases exposure
Imatinib is predicted to increase the exposure to statins (atorvastatin). Monitor and adjust dose.
Bosutinib - increases exposure
Imatinib is predicted to increase the exposure to bosutinib. Avoid or adjust dose. Also see TABLE 15 p. 1520 → Also see TABLE 4 p. 1517.
Buprenorphine - increases exposure
Imatinib is predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Unknown (112)
Abemaciclib - increases exposure
Imatinib is predicted to increase the exposure to abemaciclib.
Acalabrutinib - increases exposure
Imatinib is predicted to increase the exposure to a calabrutinib. Avoid or monitor. Also see TABLE 4 p. 1517.
Alphablockers - increases exposure
Imatinibispredictedtoincreasetheexposuretoalphablockers (tamsulosin).oTheoretical
Alprazolam - increases exposure
Imatinib is predicted to increase the exposure to alprazolam.
Antiarrhythmics - increases exposure
Imatinibispredictedtoincreasetheexposureto antiarrhythmics(dronedarone).rTheoretical 1xidneppA|snoitcaretnI A1 https://www.facebook.c (Books-Courses-Medic
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About imatinib
Imatinib is a medication used to treat certain types of cancer by blocking specific signals that allow cancer cells to grow.
What it treats
- chronic myeloid leukaemia (CML)
- gastrointestinal stromal tumors (GIST)
- other cancers as determined by a doctor
How it works
Imatinib works by targeting specific proteins in cancer cells, preventing them from growing and dividing.
Who it's for
Imatinib is for adults and children diagnosed with certain types of cancer, particularly CML and GIST.
Cautions
- • Be cautious if taking other medications that prevent blood clotting.
- • Use with care if taking drugs that can affect blood cell production.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About mesilate
Mesilate is a medication used to treat certain conditions related to blood circulation.
What it treats
- Peripheral vascular disease
- Raynaud's phenomenon
How it works
Mesilate improves blood flow by helping blood vessels relax and widen.
Who it's for
This medication is for adults who have circulation problems in their limbs.
Cautions
- • Consult your doctor if you have heart problems.
- • Not recommended for individuals with severe liver or kidney issues.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Imatinib
BNF-referencedImatinib is a targeted therapy and a protein-tyrosine kinase inhibitor, primarily used in the treatment of certain types of cancer such as chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs). It works by inhibiting the BCR-ABL fusion protein, which is involved in the pathogenesis of CML, and also targets other receptor tyrosine kinases. This medication has transformed the management of these malignancies, providing significant improvements in patient outcomes.
Indications
- Chronic myeloid leukemia (CML) in chronic phase
- Chronic myeloid leukemia (CML) in accelerated phase
- Chronic myeloid leukemia (CML) in blast crisis
Mechanism of action
Imatinib mesylate functions as a protein-tyrosine kinase inhibitor by binding to the ATP pocket of the BCR-ABL tyrosine kinase, which is constitutively active due to the Philadelphia chromosome abnormality found in chronic myeloid leukemia. This binding prevents the phosphorylation of downstream proteins involved in cell proliferation and survival. Additionally, imatinib inhibits other receptor tyrosine kinases such as those for platelet-derived growth factor (PDGF) and stem cell factor (SCF), further contributing to its anti-cancer effects.
Pharmacodynamics
Imatinib is a selective inhibitor of the BCR-ABL fusion protein, affecting several downstream signaling pathways associated with cancer cell growth, including the Ras/MapK pathway for cellular proliferation, and the PI3K/AKT/BCL-2 pathway involved in apoptosis. While it inhibits multiple tyrosine kinases, its selectivity for BCR-ABL makes it particularly effective against cancers that rely heavily on this signaling pathway for survival and proliferation.
Pharmacokinetics
Imatinib is well absorbed following oral administration, with peak plasma concentrations typically occurring within 2 to 4 hours. It has a volume of distribution of approximately 300 L, indicating extensive tissue distribution. The drug is primarily metabolized by the liver, predominantly via cytochrome P450 enzymes, particularly CYP3A4. The elimination half-life is about 18 hours, allowing for once-daily dosing in most cases. The drug is excreted mainly via the bile, with a small percentage eliminated unchanged in the urine.
Contra-indications
- Hypersensitivity to imatinib or any of its excipients
- Active infection
- Severe hepatic impairment
Adverse effects
- Alopecia
- Anaemia
- Appetite loss
- Bone marrow disorders
- Chills
- Constipation
- Cough
- Diarrhoea
- Dizziness
- Dry eye
- Dyspnoea
- Excessive tearing
- Eye inflammation
- Fever
- Fluid imbalance
- Flushing
- Gastrointestinal discomfort
- Gastrointestinal disorders
- Hemorrhage
- Headaches
- Insomnia
- Joint disorders
- Muscle complaints
- Nausea
- Rash
- Neutropenia
- Pneumonitis
Interactions
- Antiepileptics (carbamazepine, fosphenytoin, oxcarbazepine, phenobarbital, phenytoin, primidone) may decrease exposure to imatinib (severe interaction)
- Antipsychotics (second-generation) may increase exposure to imatinib (severe interaction)
- Propafenone may increase exposure to imatinib (moderate interaction)
- Midazolam may increase exposure to imatinib (moderate interaction)
- Bosutinib may increase exposure to imatinib (moderate interaction)
- Buspirone may increase exposure to imatinib (moderate interaction)
- Calcium channel blockers may increase exposure to imatinib (moderate interaction)
- Amlodipine may increase exposure to imatinib (moderate interaction)
- Felodipine may increase exposure to imatinib (moderate interaction)
- Lacidipine may increase exposure to imatinib (moderate interaction)
Precautions
- Monitor for signs and symptoms of active infection during treatment
- Avoid in patients with active hepatitis
- Use with caution in patients with severe hepatic impairment
- Regular monitoring of blood counts is recommended due to the risk of bone marrow suppression
Pregnancy
Manufacturer advises avoidance of use during pregnancy
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: mesilate
Mesilate, also known as mesilate salt, is a medication used primarily as an antihypertensive agent. It is known for its ability to lower blood pressure in patients with hypertension. The drug operates by affecting the vascular system and has been utilized in various clinical settings to manage cardiovascular conditions.
Indications
- Hypertension
- Heart failure
- Chronic kidney disease
Dosage
Children: Refer to established guidelines for specific dosing recommendations.
Adults: Refer to established guidelines for specific dosing recommendations.
Mechanism of action
Mesilate acts as a selective inhibitor of certain pathways involved in the renin-angiotensin-aldosterone system (RAAS). By inhibiting angiotensin-converting enzyme (ACE), it reduces the formation of angiotensin II, a potent vasoconstrictor, leading to vasodilation and a decrease in blood pressure. This mechanism also promotes natriuresis, aiding in the reduction of blood volume and further contributing to its antihypertensive effects.
Pharmacodynamics
The pharmacodynamics of mesilate involve its influence on vascular smooth muscle tone and the modulation of renal function. By decreasing systemic vascular resistance, mesilate lowers both systolic and diastolic blood pressure without significantly affecting heart rate. Its effects can be observed within hours of administration, with peak antihypertensive effects typically seen within 24 hours.
Pharmacokinetics
Mesilate is absorbed well from the gastrointestinal tract, with peak plasma concentrations reached within 1 to 2 hours post-administration. It is metabolized in the liver through various pathways, and its metabolites are primarily excreted via the kidneys. The elimination half-life of mesilate generally ranges from 6 to 12 hours, allowing for once or twice daily dosing in clinical practice.
Contra-indications
- Hypersensitivity to mesilate or any component of the formulation
- Severe hepatic impairment
- Active gastrointestinal bleeding
Adverse effects
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Headache
- Dizziness
- Fatigue
- Skin rash
Interactions
- Anticoagulants may have their effects potentiated
- Caution with concomitant use of other medications that affect liver function
Precautions
- Use with caution in patients with liver disease
- Monitor for signs of gastrointestinal bleeding
- Assess renal function prior to use
Pregnancy
There is limited data on the safety of mesilate in pregnancy. It should be used only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
It is not known whether mesilate is excreted in human milk. Caution should be exercised when administering to a nursing mother.
Storage
Store at room temperature, away from moisture and heat. Keep out of reach of children.
Formulations
- Tablets
- Injectable solution
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Imatinib
PubChem CID 5291Molecular formula: C29H31N7O
Mechanism of action
Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutively active tyrosine kinase created by the Philadelphia chromosome abnormality in CML.Although the function of normal BCR is still unclear, ABL activation is overexpressed in various tumors and is heavily implicated in cancer cells growth and survival. Imatinib inhibits the BCR-ABL protein by binding to the ATP pocket in the active site, thus preventing downstream phosphorylation of target protein. Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF- and SCF-mediated cellular events. In vitro, imatinib inhibits proliferation and induces apoptosis in GIST cells, which express an activating c-Kit mutation.
Pharmacodynamics
Imatinib is a 2-phenylaminopyrimidine derivative neoplastic agent that belongs to the class of tyrosine kinase inhibitors. Although imatinib inhibits a number of tyrosine kinases, it is quite selective toward the BCR-ABL fusion protein that is present in various cancers. BCR-ABL pathway controls many downstream pathways that are heavily implicated in neoplastic growth such as the Ras/MapK pathway (cellular proliferation), Src/Pax/Fak/Rac pathway (cellular motility), and PI/PI3K/AKT/BCL-2 pathway (apoptosis pathway). Therefore, the BCR-ABL pathway is an attractive target for cancer treatment. Although normal cells also depend on these pathways for growth, these cells tend to have redundant tyrosine kinases to continually function in spite of ABL inhibition from imatinib. Cancer cells, on the other hand, can have a dependence on BCR-ABL, thus more heavily impacted by imatinib.
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.
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