Eltrombopag is an oral, small-molecule, non-peptide thrombopoietin receptor agonist (TPO-RA). It binds to the transmembrane domain of the human TPO receptor (c-Mpl) and stimulates the proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, leading to increased platelet production. It is a critical therapeutic agent for thrombocytopenic conditions in the Indian context.
Adult: Chronic ITP: Initial dose 50 mg once daily. For patients of East Asian ancestry or with moderate/severe hepatic impairment: Initial dose 25 mg once daily. Adjust in increments of 25 mg every 2 weeks to achieve platelet count ≥50,000/µL. Max dose 75 mg/day. SAA: 150 mg once daily (in combination with IST). HCV-thrombocytopenia: 25 mg once daily.
Note: Take on an empty stomach (1 hour before or 2 hours after a meal). Do not take within 4 hours of any food or product containing polyvalent cations (e.g., antacids, calcium, iron, mineral supplements, dairy products). Swallow tablet whole with water. Do not crush or chew.
Eltrombopag is an orally bioavailable, non-peptide agonist of the thrombopoietin (TPO) receptor (c-Mpl). Unlike endogenous TPO, which binds to the extracellular domain, eltrombopag binds to the transmembrane domain of the c-Mpl receptor on hematopoietic stem cells and megakaryocyte precursors. This binding activates intracellular signal transduction pathways (JAK-STAT and MAPK), leading to the proliferation and differentiation of megakaryocytes and subsequent increased production of platelets.
Pregnancy: Category C. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown reproductive toxicity. Thrombopoietin receptor agonists may cross the placenta.
Driving: Eltrombopag may cause dizziness and fatigue. Patients should be cautioned about operating machinery or driving until they know how the medication affects them.
| Antacids (Aluminum, Magnesium, Calcium) | Significantly reduces eltrombopag absorption. | Major |
| Iron Supplements (Ferrous sulfate) | Significantly reduces eltrombopag absorption. | Major |
| Dairy Products (Calcium) | Significantly reduces eltrombopag absorption. | Major |
| Fluvoxamine (strong CYP1A2 inhibitor) | Increases eltrombopag exposure (AUC). | Moderate |
| Rifampicin (CYP inducer) | Decreases eltrombopag exposure. | Moderate |
| Rosuvastatin, Atorvastatin | Eltrombopag may increase statin exposure via OATP1B1 inhibition. | Moderate |
| Repaglinide | Eltrombopag may increase repaglinide exposure. | Moderate |
Same composition (Eltrombopag (25mg)), different brands: