The targeted therapy medication Imatinib 100 mg (Imatinib INN) is mainly used to treat a variety of cancers, especially hematological malignancies and some solid tumors. It is a member of the pharmacological class known as tyrosine kinase inhibitors (TKIs), which function by preventing the growth and multiplication of cancer cells by blocking particular enzymes. The most prevalent illnesses for which Imatinib is given are Gastrointestinal Stromal Tumors (GISTs) and Chronic Myeloid Leukemia (CML).

Mechanism of Action

The Philadelphia chromosomal defect that is present in the majority of CML cases produces the BCR-ABL fusion protein, which is specifically inhibited by imatinib, a selective inhibitor of a class of tyrosine kinase enzymes. Imatinib 100 mg stops the phosphorylation of proteins involved in cellular signaling by attaching itself to the tyrosine kinase’s ATP-binding site. Cancerous cells’ aberrant growth and division are stopped by this inhibition, which eventually causes their apoptosis (programmed cell death).

Imatinib is useful in treating cancers like GIST that overexpress these receptors since it targets not just BCR-ABL but also c-KIT and PDGFR (platelet-derived growth factor receptor).

Indications

The following conditions can be effectively treated with Imatinib 100 mg:

Chronic myeloid leukemia (CML) has three stages: blast crisis, accelerated, and chronic.

Philadelphia chromosome-associated acute lymphoblastic leukemia (Ph+ ALL)

Unresectable and/or metastatic gastric stromal tumors (GISTs)

Myeloproliferative/Myelodysplastic Disorders (MDS/MPD)

Hypereosinophilic Syndrome (HES) and Chronic Eosinophilic Leukemia (CEL)

Mastocytosis of the System

Protuberans of Dermatofibrosarcoma (DFSP)

Dosage and Administration

The dosage of Imatinib is determined by the patient’s response to treatment, the disease’s stage, and the particular indication. To reduce gastrointestinal discomfort, it is advised to take the tablet with a meal and a full glass of water. It is often given once or twice daily.

Common dosages consist of:

400 mg per day for CML in the chronic phase

600–800 mg per day for CML (accelerated/blast phase)

GIST: 400 mg once daily; based on response, this amount may be raised to 600–800 mg.

Depending on efficacy and tolerance, dosages may be changed.

Side Effects

Although not everyone experiences them, Imatinib 100 mg may have adverse effects like any other medicine. Typical adverse effects consist of:

Diarrhea, nausea, and vomiting

Fluid retention, or edema, especially around the ankles and eyes

Joint discomfort and cramping in the muscles

Weakness and exhaustion

Rashes on the skin

A headache

Pain in the abdomen

The following are serious but uncommon adverse effects:

Myelosuppression (thrombocytopenia, neutropenia, and anemia)

Hepatotoxicity

Rare cardiovascular events

Extreme skin reactions

bleeding in the stomach (particularly in GIST sufferers)

Regular liver function tests and blood counts should be performed on patients.

Precautions and Warnings

Lactation and Pregnancy: Imatinib should not be used during pregnancy unless it is necessary. It could hurt the fetus. Additionally, breastfeeding is not advised when taking imatinib.

Use with caution if you have hepatic or renal impairment; you may need to alter your dosage.

Cardiovascular Conditions: Fluid retention and associated problems should be closely watched in patients with a history of heart disease.

Drug Interactions: Warfarin, certain antibiotics, antifungals, CYP3A4 inhibitors/inducers, and other medications may interact with Imatinib. A comprehensive drug history should be reviewed before starting treatment.

Storage Instructions

Keep below 30°C in a cool, dry location. Keep out of children’s reach. After the date of expiration shown on the container, do not use.

Conclusion

A significant development in cancer treatment is Imatinib 100 mg (Imatinib INN), which provides targeted therapy with a high level of efficacy and a controllable safety profile. Imatinib, a mainstay treatment for GIST and CML, keeps enhancing patient quality of life and survival. To control side effects and guarantee the best results, it should be administered under close medical supervision and with frequent monitoring.

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1. What is the purpose of Imatinib 100 mg?
Chronic Myeloid Leukemia (CML), Acute Lymphoblastic Leukemia (ALL) with the Philadelphia chromosome, Gastrointestinal Stromal Tumors (GISTs), and a few other uncommon disorders are the main cancers that Imatinib100 mg (Imatinib) is used to treat.

2. Imatinib (Imatinib): How does it work?
Tyrosine kinase, an enzyme that stimulates the proliferation of cancer cells, is inhibited in order for it to function. Imatinib slows or stops the growth of cancer by blocking this enzyme.

3. How should I take 100 mg of Imatinib?
To lower the chance of stomach distress, take the tablet with a meal and a full glass of water. As directed by your physician, avoid chewing or crushing the tablets.

4. Is it safe to use Imatinib when pregnant?
Imatinib may cause harm to the fetus. It is not recommended during pregnancy if it is strictly necessary. When taking this medication, use effective contraception.

5. Can I take Imatinib with other medications?
Since imatinib can interact with a variety of medications, including blood thinners, antibiotics, and antifungals, let your doctor know about all additional prescriptions, herbal remedies, and supplements.