Eltrombopag

Eltrombopag is a prescription medication used for the treatment of chronic immune thrombocytopenia, chronic hepatitis C-associated thrombocytopenia, and severe aplastic anemia.

• Eltrombopag is available under the following different brand names: Promacta

Adult and pediatric dosage

Tablet

• 12.5mg
• 25mg
• 50mg
• 75mg

Chronic Immune Thrombocytopenia (ITP) 

Adult dosage

• Initial: 50 mg orally every day
• Maintenance: Adjust the dose to achieve and maintain platelet count (Plt) above 50 x 10^9/L to reduce risk of bleeding; not to exceed 75 mg/day

Pediatric dosage

• Children below 1 year: Safety and efficacy not established
• Children between 1-5 Years: Initiate at 25 mg every day
• Children above 6 years: Initiate at 50 mg orally every day
• Maintenance: Adjust dose to achieve and maintain platelet count (Plt) above 50 x 10^9/L to reduce risk of bleeding; not to exceed 75 mg/day

Chronic Hepatitis C-associated Thrombocytopenia 

Adult dosage

• Initial: 25 mg orally every day
• Adjust the dose in 25 mg increments every 2 weeks as needed to achieve target platelet count required to initiate/maintain antiviral therapy with pegylated interferon and ribavirin; not to exceed 100 mg/day

Severe Aplastic Anemia

Adult dosage

First-line therapy

• Initial dose: 150 mg orally every day for 6 months
• Do not exceed initial dose; total duration is 6 months
• Refractory SAA
• Initial dose: 50 mg orally every day
• Adjust dose in 50-mg increments every 2 weeks as needed to achieve target Plt above 50 x 10^9/L as necessary; not exceed 150 mg/day; may take up to 16 weeks for hematologic response

Pediatric dosage

First-line therapy

• Children below 2 years: Safety and efficacy not established
• Children between 2-5 years: 2.5 mg/kg every day for 6 months initially
• Children between 6-11 years: 75 mg orally every day for 6 months initially
• Children above 12 years: 150 mg orally every day for 6 months initially
• Do not exceed initial dose; total duration is 6 months

Dosage Considerations – Should be Given as Follows: 

• See "Dosages."

Common side effects of Eltrombopag include:

• low red blood cell count (anemia)
• nausea
• fever
• abnormal liver function tests
• cough
• tiredness
• headache
• diarrhea 

Serious side effects of Eltrombopag include:

• higher risk of blood clots,
• new or worsened cataract
• increased risk of worsening of precancerous blood condition

Rare side effects of Eltrombopag include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Eltrombopag has severe interactions with no other drugs.
• Eltrombopag has serious interactions with at least 37 other drugs.
• Eltrombopag has moderate interactions with at least 92 other drugs.
• Eltrombopag has minor interactions with the following drug:
  • cimetidine 

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Eltrombopag?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Eltrombopag?”

Cautions

•  If a patient with hepatic impairment (Child-Pugh Class A, B, C) initiates therapy for first-line treatment of severe aplastic anemia, reduce the initial dose
•  In aplastic anemia, use the lowest dose to achieve and maintain hematologic response; discontinue if no hematologic response observed after 16 weeks of therapy, excessive platelet count responses, or liver test abnormalities
• Chronic hepatitis C with cirrhosis may increase the risk of hepatic decompensation and death when treated with alfa interferons; no dosage adjustment is recommended in patients with chronic hepatitis C and hepatic impairment
• Not indicated for the treatment of patients with myelodysplastic syndromes (MDS); increased risk of death and progression of MDS to acute myeloid leukemia observed in a clinical trial showing an increased relative risk of progression to AML by 166%
• Thrombotic/thromboembolic complications reported; have included both venous and arterial events and were observed at low and at normal platelet counts.
• Portal vein thrombosis reported in patients with chronic liver disease receiving therapy
• Consider potential risk of thromboembolism when administering to patients with known risk factors for thromboembolism (e.g., Factor V Leiden, ATIII deficiency, antiphospholipid syndrome, chronic liver disease).
• Risk of thrombocytopenia and hemorrhage after discontinuation
• Not for normalizing platelet counts as it may increase thrombotic/thromboembolic complications; for use only when the degree of thrombocytopenia and clinical conditions increase the risk for bleeding in patients with chronic immune idiopathic thrombocytopenia
• May develop or worsen cataracts; screen before administering and during treatment
• Discontinue if platelet count does not respond to a level to avoid clinically important bleeding after 4 weeks at the maximum recommended dose
• In hepatitis C, use only when thrombocytopenia prevents initiation and maintenance of interferon-based therapy; discontinue if antiviral therapy discontinued
• Hepatotoxicity
  • May increase risk of severe and potentially life-threatening hepatotoxicity (see Black Box Warnings), monitor liver function before and during therapy
  • Treatment of ITP, chronic hepatitis C-associated thrombocytopenia, and refractory severe aplastic anemia
  • Measure serum ALT, AST, and bilirubin prior to initiation of therapy, every 2 weeks during the dose adjustment phase, and monthly following establishment of a stable dose. The drug inhibits UDP ­glucuronosyltransferase (UGT)1A1 and organic anion-transporting polypeptide (OATP)1B1, which may lead to indirect hyperbilirubinemia; if bilirubin is elevated, perform fractionation; evaluate abnormal serum liver tests with repeat testing within 3 to 5 days
  • If abnormalities are confirmed, monitor serum liver tests weekly until resolved or stabilized; discontinue treatment if ALT levels increase to greater than or equal to 3 x ULN in patients with normal liver function or greater than or equal to 3 x baseline (or greater than 5 x ULN, whichever is the lower) in patients with pre-treatment elevations in transaminases and are: progressively increasing, or persistent for greater than or equal to 4 weeks, or accompanied by increased direct bilirubin, or accompanied by clinical symptoms of liver injury or evidence for hepatic decompensation
  • If the potential benefit for reinitiating treatment is considered to outweigh the risk for hepatotoxicity, then consider cautiously reintroducing therapy and measure serum liver tests weekly during dose adjustment phase; hepatotoxicity may reoccur if therapy is reinitiated; if liver test abnormalities persist, worsen, or recur, then permanently discontinue therapy
• First-line treatment of severe aplastic anemia
  • Measure ALT, AST, and bilirubin prior to initiation of therapy, every other day while hospitalized for h-ATG therapy, and then every 2 weeks during treatment; during treatment, manage increases in ALT or AST levels as recommended 

Pregnancy and Lactation

• Available data from published case reports and postmarketing experience with use in pregnant women are insufficient to assess any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• Contraception
  • Based on animal reproduction studies, fetal harm may occur when administered to a pregnant woman
  • Use effective contraception in sexually active females of reproductive during treatment and for at least 7 days after stopping treatment
• Lactation
  • No data available regarding the presence of eltrombopag or metabolites in human milk, effects on the breastfed child, or on milk production
  • However, the drug was detected in pups of lactating rats 10 days postpartum suggesting potential for transfer during lactation; due to the potential for serious adverse reactions in a breastfed child from the drug, breastfeeding is not recommended during treatment