Thrombopoietin receptor agonist (TPO-R)
Brand names: Revolade, Promacta, Eltrombopag Cipla
Updated · Methodology
Second line
Second-line for chronic immune thrombocytopenia in adults and children over 1 year after steroid and splenectomy failure or splenectomy contraindication per ASH 2019 and the Spanish SEHH 2023. Adult starting dose 50 mg once daily, titrated to 75 mg daily. RAISE and the EXTEND long-term extension maintained platelets above 50×10⁹/L in 60–80% of patients.
Sources
ICD-10: D69.3 · ICD-11: 3B64.10
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Eltrombopag is a thrombopoietin receptor agonist. It is prescribed for chronic immune thrombocytopenia, aplastic anemia, and thrombocytopenia associated with chronic hepatitis C (AEMPS Ficha Técnica). In alt-anti-aging circles, eltrombopag is occasionally promoted for general platelet boost and immunity in healthy people. In healthy adults, no clinical studies of such use exist. The drug has serious risks: hepatotoxicity (requires regular liver enzyme monitoring), thromboembolic events (paradoxically, with excessive platelet elevation), cataract, and myelodysplastic changes in some patients. If eltrombopag was recommended to a healthy person, seek a second opinion immediately.
A small-molecule non-peptide thrombopoietin receptor (TPO-R) agonist – binds the receptor transmembrane domain, unlike endogenous thrombopoietin (extracellular domain). Activates JAK/STAT signaling in bone marrow megakaryocytes, stimulating proliferation and differentiation into platelets. Compared with peptide TPO agonists (romiplostim, injections), available orally – daily administration.
Boxed warning
FDA boxed warning: hepatotoxicity, sometimes fatal. Monitor liver enzymes and bilirubin before start, every 2 weeks for the first month, then monthly.
Contraindicated. Reliable contraception is required in women of reproductive age.
Contraindicated during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Verbatim lines from the interaction sections, in the language of the label
«Polyvalent Cations (Chelation): Eltrombopag chelates polyvalent cations (such as iron, calcium, aluminum, magnesium, selenium, and zinc) in foods, mineral supplements, and antacids. Take eltrombopag…»FDA, section 7 · Open on DailyMed
«Complicaciones trombóticas/AEMPS, section 4.4 · Open on CIMA
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Ciclosporina: Cuando se administró de forma concomitante con 200 mg y 600 mg de ciclosporina (un inhibidor de BCRP) se observó una disminución de eltrombopag. La administración concomitante con 200…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Sustratos de OATP1B1 y BCRP: La administración conjunta de eltrombopag y de los sustratos OATP1B1 (por ej. metotrexato) y BCRP (por ej. topotecán y metotrexato) debe realizarse con precaución (ver…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Lopinavir/AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Inhibidores de la HMG CoA reductasa: La administración de 75 mg de eltrombopag una vez al día, durante 5 días, con una dosis única de 10 mg de rosuvastatina, sustrato de OATP1B1 y BCRP, a 39 sujetos…»AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Cationes polivalentes (quelación): Eltrombopag forma quelatos con cationes polivalentes como el hierro, calcio, magnesio, aluminio, selenio y zinc. La administración de una dosis única de 75 mg de…»AEMPS, section 4.5 · Open on CIMA
«Medicamentos para el tratamiento de PTI: Los medicamentos utilizados en los ensayos clínicos en el tratamiento de PTI en combinación con eltrombopag incluyeron corticosteroides , danazol y/AEMPS, section 4.5 · Open on CIMA
«Sustratos del citocromo P450: La administración de 75 mg de eltrombopag una vez al día, durante 7 días, a 24 varones sanos, no inhibió o indujo el metabolismo de los sustratos de investigación para…»AEMPS, section 4.5 · Open on CIMA
«Medicamentos para el tratamiento de PTI: Los medicamentos utilizados en los ensayos clínicos en el tratamiento de PTI en combinación con eltrombopag incluyeron corticosteroides , danazol y/AEMPS, section 4.5 · Open on CIMA
«Sustratos del citocromo P450: En los estudios que utilizaron microsomas hepáticos humanos, eltrombopag (hasta 100 ? M) mostró no inhibir in vitro las enzimas CYP450, 1A2, 2A6, 2C19, 2D6, 2E1, 3A4/AEMPS, section 4.5 · Open on CIMA
«Sustratos del citocromo P450: La administración de 75 mg de eltrombopag una vez al día, durante 7 días, a 24 varones sanos, no inhibió o indujo el metabolismo de los sustratos de investigación para…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores e inductores de CYP1A2 y CYP2C8: Eltrombopag se metaboliza a través de múltiples vías, incluyendo CYP1A2, CYP2C8, UGT1A1, y UGT1A3 (ver sección 5.2). Es poco probable que los medicamentos…»AEMPS, section 4.5 · Open on CIMA
«Sustratos del citocromo P450: La administración de 75 mg de eltrombopag una vez al día, durante 7 días, a 24 varones sanos, no inhibió o indujo el metabolismo de los sustratos de investigación para…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores e inductores de CYP1A2 y CYP2C8: Eltrombopag se metaboliza a través de múltiples vías, incluyendo CYP1A2, CYP2C8, UGT1A1, y UGT1A3 (ver sección 5.2). Es poco probable que los medicamentos…»AEMPS, section 4.5 · Open on CIMA
«Protease Inhibitors: HIV Protease Inhibitors: No dose adjustment is recommended when eltrombopag is coadministered with lopinavir/FDA, section 7 · Open on DailyMed
«Interacciones que disminuyen los niveles de otros fármacos: La administración conjunta de una dosis única de ciclosporina (200 mg o 600 mg) con una dosis única de eltrombopag (50 mg) disminuye el AUC…»AEMPS, section 4.5 · Open on CIMA
«Variación del AUC de rosuvastatina*: Eltrombopag 75 mg 1 vez al día, 5 días»AEMPS, section 4.5 · Open on CIMA
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Eltrombopag is evaluated for the following indications with varying evidence strength: Immune thrombocytopenia (evidence tier A), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Eltrombopag (≥ 1 in 100): Headache, Nausea, Diarrhea, Fatigue, Elevated ALT and bilirubin. See the Safety section for uncommon and serious reactions.
Contraindicated. Reliable contraception is required in women of reproductive age.
Contraindicated during lactation.
Eltrombopag is contraindicated in: Eltrombopag hypersensitivity; Severe hepatic impairment; Pregnancy and lactation; Age under 1. Full list in the Safety section.
FDA boxed warning: hepatotoxicity, sometimes fatal. Monitor liver enzymes and bilirubin before start, every 2 weeks for the first month, then monthly.
Direct links to regulator labels. Open in a new tab.
Menaquinone (vitamin K2), Menaquinone-7, Phytomenadione, Tranexamic acid