Imatinib Krka D.D. (Imatinib)

Imatinib acts on malignant cells driven by BCR‑ABL, c‑KIT or PDGFR signaling pathways, providing targeted therapy for specific hematologic and solid tumours.

• Chronic myeloid leukemia (CML): achieves disease control by inhibiting BCR‑ABL‑driven proliferation.
• Philadelphia chromosome‑positive acute lymphoblastic leukemia (Ph+ ALL): facilitates remission through BCR‑ABL blockade.
• Gastrointestinal stromal tumour (GIST): induces tumour shrinkage by targeting c‑KIT and PDGFR signaling.

• Imatinib selectively inhibits the tyrosine kinase activity of BCR‑ABL, c‑KIT and platelet‑derived growth factor receptors (PDGFR). By binding to the ATP‑binding site of these kinases, it prevents downstream phosphorylation events that drive uncontrolled cell division, thereby halting the proliferation of malignant clones and promoting apoptosis in affected tissues.

Adverse reactions may vary in frequency and severity. Patients should be monitored regularly for any new or worsening symptoms.

Common Side Effects

• Nausea and vomiting: mild to moderate gastrointestinal upset.
• Edema: peripheral swelling, often in the lower extremities.
• Fatigue: generalized tiredness affecting daily activities.
• Diarrhea: loose stools that may require supportive care.

Serious or Rare Side Effects

• Hepatotoxicity: elevated liver enzymes or liver injury.
• Cardiac dysfunction: reduced left‑ventricular ejection fraction.
• Severe neutropenia or thrombocytopenia: increased risk of infection or bleeding.

Before initiating therapy, clinicians should assess baseline organ function and comorbid conditions.

• Baseline labs: obtain complete blood count, liver and renal function tests.
• Cardiac monitoring: evaluate ejection fraction in patients with pre‑existing heart disease.
• Drug interactions: review concomitant medications for CYP3A4 inhibitors or inducers.
• Pregnancy and lactation: avoid use unless benefits clearly outweigh potential risks.
• Store at ambient temperature: keep below 25 °C in the original container, protect from moisture and direct sunlight.

Imatinib may interact with several medicines that alter its metabolism or increase toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may raise imatinib plasma levels.
• Potent CYP3A4 inducers (e.g., rifampicin, carbamazepine): may reduce therapeutic exposure.

Moderate Interactions (Monitor Closely)

• Acid‑reducing agents (e.g., proton pump inhibitors): can modestly decrease absorption.
• Anticoagulants (e.g., warfarin): may enhance bleeding risk.
• Vaccines containing live attenuated virus: consider timing to avoid reduced efficacy.