Eltrombopag

What is Eltrombopag?

• Eltrombopag (PROMACTA) is a thrombopoietin receptor agonist used to treat thrombocytopenia (abnormally low platelet counts) and severe aplastic anemia.

Eltrombopag

What are the uses of this medicine?

PROMACTA is a prescription medicine used to treat adults and children 1 year of age and older with low blood platelet counts due to persistent or chronic immune thrombocytopenia (ITP), when other medicines to treat ITP or surgery to remove the spleen have not worked well enough.

PROMACTA is also used to treat people with:

• low blood platelet counts due to chronic hepatitis C virus (HCV) infection before and during treatment with interferon.
• severe aplastic anemia (SAA) in combination with other medicines to treat SAA, as the first treatment for adults and children 2 years of age and older.
• severe aplastic anemia (SAA) when other medicines to treat SAA have not worked well enough.
• PROMACTA is used to try to raise platelet counts in order to lower your risk for bleeding.
• PROMACTA is not used to make platelet counts normal.

How does this medicine work?

• Eltrombopag is an orally bioavailable, small-molecule TPO-receptor agonist that interacts with the transmembrane domain of the human TPO-receptor and initiates signaling cascades that induce proliferation and differentiation from bone marrow progenitor cells.

Who Should Not Use this medicine ?

Limitations of Use:

• PROMACTA is not for use in people with a pre-cancerous condition called myelodysplastic syndrome (MDS), or in people with low platelet counts caused by certain other medical conditions or diseases.
• It is not known if PROMACTA is safe and effective when used with other antiviral medicines to treat chronic hepatitis C.

It is not known if PROMACTA is safe and effective in children:

• younger than 1 year with ITP
• with low blood platelet counts due to chronic hepatitis C
• whose severe aplastic anemia (SAA) has not improved after previous treatments.
• younger than 2 years when used in combination with other medicines to treat SAA as the first treatment for SAA.

What drug interactions can this medicine cause?

• Take PROMACTA at least 2 hours before or 4 hours after any medications or products containing polyvalent cations, such as antacids, dairy products, and mineral supplements to avoid significant reduction in absorption of PROMACTA due to chelation.
• Use caution when concomitantly administering PROMACTA and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan, pitavastatin, pravastatin, rosuvastatin, repaglinide, rifampin, simvastatin acid, SN-38 [active metabolite of irinotecan], valsartan) or breast cancer resistance protein (BCRP) (e.g., imatinib, irinotecan, lapatinib, methotrexate, mitoxantrone, rosuvastatin, sulfasalazine, topotecan).

Is this medicine FDA approved?

• Eltrombopag received breakthrough therapy designation from the U.S. Food and Drug Administration (FDA) in February 2014, for people with aplastic anemia for which immunosuppression has not been successful.

How should this medicine be used?

Recommended dosage: Persistent or Chronic ITP:

• Initiate PROMACTA at 50 mg once daily for most adult and pediatric patients 6 years and older, and at 25 mg once daily for pediatric patients aged 1 to 5 years.
• Dose reductions are needed for patients with hepatic impairment and some patients of East-/Southeast-Asian ancestry.
• Adjust to maintain platelet count greater than or equal to 50 x 109/L.
• Do not exceed 75 mg per day.

Chronic Hepatitis C-associated Thrombocytopenia:

• Initiate PROMACTA at 25 mg once daily for all patients.
• Adjust to achieve target platelet count required to initiate antiviral therapy.
• Do not exceed a daily dose of 100 mg.

First-line Severe Aplastic Anemia:

• Initiate PROMACTA once daily at 2.5 mg/kg (in pediatric patients aged 2 to 5 years old), 75 mg (pediatric patients aged 6 to 11 years old), or 150 mg for patients aged 12 years and older concurrently with standard immunosuppressive therapy.
• Reduce initial dose in patients of East-/Southeast-Asian ancestry.
• Modify dosage for toxicity or elevated platelet counts.

Refractory Severe Aplastic Anemia:

• Initiate PROMACTA at 50 mg once daily.
• Reduce initial dose in patients with hepatic impairment or patients of East-/Southeast-Asian ancestry.
• Adjust to maintain platelet count greater than 50 x 109/L. Do not exceed 150 mg per day.

Administration:

• Your healthcare provider will prescribe the dose of PROMACTA tablets or PROMACTA for oral suspension that is right for you.
• If your healthcare provider prescribes PROMACTA tablets, take PROMACTA tablets whole. Do not split, chew, or crush PROMACTA tablets and do not mix with food or liquids.
• If your healthcare provider prescribes PROMACTA for oral suspension, see the “Instructions for Use” that comes with your medicine for instructions on how to correctly mix and take a dose of PROMACTA.
• Use a new single-use oral dosing syringe to prepare each dose of PROMACTA for oral suspension. Do not re-use the oral dosing syringe.
• Do not stop taking PROMACTA without talking with your healthcare provider first. Do not change your dose or schedule for taking PROMACTA unless your healthcare provider tells you to change it.
• Take PROMACTA without a meal or with a meal low in calcium (50 mg or less) and at least 2 hours before or 4 hours after eating calcium-rich foods, such as dairy products, calcium-fortified juices, and certain fruits and vegetables.
• If you miss a dose of PROMACTA, wait and take your next scheduled dose. Do not take more than 1 dose of PROMACTA in 1 day.
• If you take too much PROMACTA, you may have a higher risk of serious side effects. Call your healthcare provider right away.
• Your healthcare provider will check your platelet count during your treatment with PROMACTA and change your dose of PROMACTA as needed.
• Tell your healthcare provider about any bruising or bleeding that happens while you take and after you stop taking PROMACTA.
• If you have SAA, your healthcare provider may do tests to monitor your bone marrow during treatment with PROMACTA.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 12.5 mg, 25 mg, 50 mg, and 75 mg
• oral suspension: 12.5 mg and 25 mg

This medicine is available in fallowing brand namesː

• PROMACTA

What side effects can this medication cause?

The most common side effects of this medicine include:

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

PROMACTA may cause serious side effects, including:

• Liver problems
• myelodysplastic syndrome (MDS) to acute myelogenous leukemia (AML)
• High platelet counts and higher risk for blood clots
• New or worsened cataracts (a clouding of the lens in the eye)

What special precautions should I follow?

• In patients with chronic hepatitis C, PROMACTA in combination with interferon and ribavirin may increase the risk of hepatic decompensation. Monitor liver function before and during therapy.
• PROMACTA may increase the risk of severe and potentially life-threatening hepatotoxicity. Monitor hepatic function and discontinue dosing as recommended.
• Increased Risk of Death and Progression of Myelodysplastic Syndromes to Acute Myeloid Leukemia.
• Portal vein thrombosis has been reported in patients with chronic liver disease receiving PROMACTA. Monitor platelet counts regularly.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• platelet counts may increase excessively and result in thrombotic/thromboembolic complications
• rash
• bradycardia
• ALT/AST elevations
• fatigue

Treatment of overdosage:

• The patient was treated with gastric lavage, oral lactulose, intravenous fluids, omeprazole, atropine, furosemide, calcium, dexamethasone, and plasmapheresis.
• In case of an overdose, consider oral administration of a metal cation-containing preparation, such as calcium, aluminum, or magnesium preparations to chelate eltrombopag and thus limit absorption.

Can this medicine be used in pregnancy?

• Available data from a small number of published case reports and postmarketing experience with PROMACTA use in pregnant women are insufficient to assess any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Can this medicine be used in children?

It is not known if PROMACTA is safe and effective in children:

• younger than 1 year with ITP
• with low blood platelet counts due to chronic hepatitis C
• whose severe aplastic anemia (SAA) has not improved after previous treatments.
• younger than 2 years when used in combination with other medicines to treat SAA as the first treatment for SAA.

What are the active and inactive ingredients in this medicine?

Tablets:

• Active ingredient: eltrombopag olamine
• Inactive ingredients:
• Tablet Core: magnesium stearate, mannitol, microcrystalline cellulose, povidone, and sodium starch glycolate.
• Coating: FD&C Blue No. 2 aluminum lake (50-mg tablet), FD&C Yellow No. 6 aluminum lake (25-mg tablet), hypromellose, Iron Oxide Black and Iron Oxide Red (75-mg tablet), polyethylene glycol 400, polysorbate 80 (12.5-mg tablet), or titanium dioxide.

For oral suspension:

• Active ingredient: eltrombopag olamine
• Inactive ingredients: mannitol, sucralose, and xanthan gum

Who manufactures and distributes this medicine?

• Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey

What should I know about storage and disposal of this medication?

Tablets:

• Store PROMACTA tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep PROMACTA in the bottle given to you.

For oral suspension:

• Store PROMACTA for oral suspension at room temperature between 68°F to 77°F (20°C to 25°C).
• After mixing, PROMACTA should be taken right away but may be stored for no more than 30 minutes between 68°F to 77°F (20°C to 25°C). Throw away (discard) the mixture if not used within 30 minutes.

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Thrombopoietin receptor agonists and Thrombopoiesis Stimulators

• • Avatrombopag, Eltrombopag, Fostamatinib, Lusutrombopag, Romiplostim, Oprelvekin (IL-11)

• Dailymed label info on Eltrombopag
• FDA Eltrombopag

Eltrombopag Resources
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