Pageltra (Eltrombopag)

Eltrombopag acts on the thrombopoietin pathway to increase platelet production in several hematologic disorders.

• Chronic immune thrombocytopenia (ITP): Improves platelet counts in adults with persistent or chronic ITP.
• Severe aplastic anemia: Supports platelet recovery when used with immunosuppressive therapy.
• Hepatitis C‑related thrombocytopenia: Helps raise platelet numbers in patients undergoing antiviral therapy.
• Myelodysplastic syndromes (MDS) with severe thrombocytopenia: Used experimentally; clinical benefit may include higher platelet counts.

• Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor (c-Mpl) on megakaryocyte precursors, mimicking the natural ligand. This activation triggers intracellular signaling cascades (JAK/STAT, MAPK, and PI3K pathways) that promote proliferation and differentiation of megakaryocytes, leading to increased platelet production in the bone marrow.

Eltrombopag may cause a range of adverse reactions, most of which are dose‑dependent and reversible upon discontinuation.

Common Side Effects

• Nausea: Mild to moderate gastrointestinal upset.
• Diarrhea: Loose stools, often transient.
• Headache: Tension‑type or mild migraine‑like pain.
• Fatigue: Generalised tiredness without clear cause.
• Elevated liver enzymes: Mild increases in ALT/AST.

Serious or Rare Side Effects

• Hepatotoxicity: Significant liver injury requiring monitoring.
• Thromboembolic events: Deep‑vein thrombosis or pulmonary embolism.
• Bone marrow fibrosis: Rare progression of marrow scarring.
• Severe allergic reaction: Anaphylaxis or angioedema.
• Vision changes: Rare retinal pigment epithelium alterations.

When prescribing Eltrombopag, clinicians should consider several safety measures and patient‑specific factors.

• Liver function monitoring: Check ALT/AST before starting and periodically during therapy.
• Pregnancy and lactation: Use only if the potential benefit outweighs risk; data are limited.
• Concomitant anticoagulants: Assess bleeding risk and adjust therapy as needed.
• Iron deficiency: Correct before initiating therapy to optimise response.
• Renal impairment: Dose may need adjustment in severe renal dysfunction.
• Store at below 25°C: Keep in the original container, protect from moisture and direct sunlight.

Eltrombopag interacts with several medicines that can alter its absorption or increase toxicity.

Major Interactions (Avoid)

• Antacids containing aluminum or magnesium: Reduce oral absorption of Eltrombopag.
• Ciprofloxacin and other fluoroquinolones: May increase serum concentrations.
• Cyclosporine: Elevates risk of hepatotoxicity.

Moderate Interactions (Monitor Closely)

• Warfarin: May affect INR values; monitor coagulation parameters.
• Oral contraceptives: Potentially reduced efficacy; consider alternative contraception.
• Statins (especially simvastatin): May increase risk of liver enzyme elevation.