A medication called Imatinib 400 mg contains the antitumor drug imatinib, which is categorized as a tyrosine kinase inhibitor. It is mainly used to treat certain cancers, particularly gastrointestinal stromal tumors (GIST) and chronic myeloid leukemia (CML). Imatinib is only available with a prescription, and it should only be taken under a doctor’s supervision.

Active Ingredient and Strength

400 mg of imatinib mesylate, or 400 mg of imatinib base, is contained in each Imatinib pill. Imatinib functions by targeting specific proteins that are necessary for the growth and metastasis of cancer cells.

Mechanism of Action

Imatinib selectively inhibits several tyrosine kinases, including PDGFR (platelet-derived growth factor receptor), c-KIT, and BCR-ABL. These enzymes are essential to the pathophysiology of several types of cancer. The constitutive tyrosine kinase-active BCR-ABL fusion protein is a product of the Philadelphia chromosome defect in chronic myeloid leukemia (CML). By attaching itself to the BCR-ABL protein’s ATP-binding site, imatinib stops the protein’s function and stops subsequent signaling cascades that encourage the growth of cancer cells.

Imatinib inhibits the c-KIT and PDGFRα tyrosine kinases, which are frequently mutated and active in gastrointestinal stromal tumors (GISTs). In tumor cells, this inhibition causes apoptosis (programmed cell death) to rise and cell proliferation to decrease.

Indications

The following conditions can be treated with Imatinib 400 mg:

Patients in the chronic, rapid, or blast phases of chronic myeloid leukemia (CML) might be adults or children.

Adults with Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL) are specifically affected.

Adults with malignant gastrointestinal stromal tumors (GIST) that are either incurable or have spread.

MDS/MPD: Myelodysplastic/Myeloproliferative Diseases: Linked to PDGFR gene mutations.

FIP1L1-PDGFRα fusion kinase is linked to both Hypereosinophilic Syndrome (HES) and Chronic Eosinophilic Leukemia (CEL).

Systemic Mastocytosis (SM), particularly when PDGFR mutations are present.

The condition known as Dermatofibrosarcoma Protuberans (DFSP) is incurable, recurring, and/or metastatic.

Dosage and Administration

Imatinib dosage recommendations vary depending on the patient’s condition and the indication. To lessen gastrointestinal irritation, it is usually taken once or twice a day with a meal and a large glass of water. Depending on the side effect profile or therapeutic response, dosage changes can be required.

400 mg per day for CML in the chronic phase

600 mg once daily for Blast Crisis or Accelerated CML

400–600 mg per day for GIST

Every day, 600 mg of Ph+ ALL

Additional signs: As instructed by a medical expert

It is recommended that Imatinib tablets be swallowed whole rather than broken up or chewed.

Side Effects

Imatinib may have minor to severe adverse effects, as is the case with all drugs. Typical adverse effects consist of:

Vomiting and feeling queasy

Having diarrhea

Joint pain or cramping in the muscles

Edema, particularly peripheral and periorbital

Weariness

A headache

Rash

Discomfort in the abdomen

The following are serious but uncommon side effects:

Myelosuppression (thrombocytopenia, neutropenia, and anemia)

Hepatotoxicity

Cardiotoxicity

Pleural effusion and fluid retention

Bleeding in the stomach

Rare Stevens-Johnson syndrome

Throughout treatment, it is advised to regularly check blood counts, liver function, and renal function.

Contraindications and Precautions

Patients who have a history of known hypersensitivity to imatinib or any of the formulation’s excipients should not use Imatinib. People who have heart illness, renal impairment, or liver impairment should use it carefully.

Imatinib should not be used by women who are pregnant or nursing unless the advantages exceed the dangers. Imatinib may be detrimental to the fetus and has the potential to cause teratogenic effects.

Drug Interactions

Drugs that interfere with cytochrome P450 enzymes, especially CYP3A4, may interact with Imatinib. Imatinib levels may rise when used concurrently with potent CYP3A4 inhibitors (such as clarithromycin or ketoconazole), while its efficacy may be diminished by inducers (such as phenytoin or rifampin).

To prevent any interactions, it’s critical to let your healthcare provider know about all of the drugs, vitamins, and herbal products you’re using.

Storage

Imatinib 400 mg tablets should be kept at room temperature (15°C to 30°C) in a dry location away from moisture and light. Keep out of children’s reach.

Conclusion

A targeted treatment called Imatinib 400 mg (Imatinib INN) has shown notable improvements in the treatment of a number of solid cancers and hematologic malignancies. It functions by selectively blocking important molecular factors that contribute to the development of cancer. It provides a controllable safety profile and an effective therapy alternative when administered under appropriate medical supervision.

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1. What is Imatinib used for?
It is frequently given to treat cancers such as gastrointestinal stromal tumors (GIST), acute lymphoblastic leukemia (ALL), and chronic myeloid leukemia (CML).

2. What is the mechanism of action of imatinib?
Tyrosine kinase inhibitor imatinib helps prevent or reduce the progression of cancer by blocking the activity of aberrant proteins that tell cancer cells to proliferate.

3. How should 400 mg of Imatinib be taken?
To lower the risk of stomach discomfort, it is often taken once or twice a day with meals and a full glass of water.

4. What are Imatinib 400 mg’s typical adverse effects?
Nausea, vomiting, cramping in the muscles, rash, diarrhea, and exhaustion are a few typical adverse effects.

5. Are there any drug interactions with Imatinib 400 mg?
Indeed, imatinib may interact with medications such as warfarin, certain antibiotics, antifungals, and medications that are processed by the CYP3A4 enzyme in the liver. You should always let your doctor know about all of your prescriptions.

6. Is it safe to take 400 mg of Imatinib when pregnant or nursing?
Because it could harm the fetus or baby, it is not advised during pregnancy or breastfeeding unless necessary.