Avatrombopag Maleate is a thrombopoietin receptor agonist (TPO-RA) that is administered orally to boost platelet production in patients with thrombocytopenia under the brand name Doptelet. This small-molecule drug specifically binds and activates the thrombopoietin receptor (c-Mpl), promoting megakaryocyte development and proliferation while increasing platelet numbers.

Doptelet is primarily indicated for two conditions:

1. In adults with chronic liver disease (CLD), thrombocytopenia is used to lessen the requirement for platelet transfusions prior to planned medical procedures.
2. Adults with chronic immune thrombocytopenia (ITP) are treated when corticosteroids and immunoglobulins have not produced enough of a response.

Composition and Formulation

Each Doptelet tablet contains 20 mg of Avatrombopag (as Avatrombopag Maleate) as the active ingredient. The formulation includes various inactive excipients such as:

• Microcrystalline cellulose
• Lactose monohydrate
• Magnesium stearate
• Povidone
• Colloidal silicon dioxide
• Croscarmellose sodium

The tablets are film-coated, typically round, and colored to help distinguish them from other medications.

Pharmacology

Mechanism of Action (MOA)

The natural function of thrombopoietin (TPO) in the bone marrow is mimicked by the thrombopoietin receptor agonist (TPO-RA) avatrombopag. When it attaches itself to the c-Mpl receptor, it causes:

increased megakaryocyte (platelet precursor) synthesis

Increased synthesis of platelets in a dose-dependent fashion

Avatrombopag lowers the risk of immune response-related problems because it does not cause the production of neutralizing antibodies, in contrast to recombinant TPO or peptide-based TPO-R agonists.

Pharmacokinetics

• Absorption: Rapidly absorbed after oral administration, with peak plasma concentration reached within 3–6 hours.
• Distribution: Extensively protein-bound (>96%) in plasma.
• Metabolism: Primarily metabolized by the CYP2C9 and CYP3A4 enzyme pathways.
• Elimination: Half-life of approximately 19–26 hours, excreted mainly in feces (~88%) and urine (~6%).

Indications and Usage

1. Thrombocytopenia in Chronic Liver Disease (CLD)

• Used to reduce the need for platelet transfusion before a scheduled medical or surgical procedure.
• Typically administered 10–13 days before the procedure, with dosing adjusted based on baseline platelet count.

2. Chronic Immune Thrombocytopenia (ITP)

• Indicated for adults with primary chronic ITP who have had an inadequate response to corticosteroids, immunoglobulins, or splenectomy.
• Used as a long-term treatment to maintain sufficient platelet levels and prevent bleeding episodes.

Dosage and Administration

Thrombocytopenia in Chronic Liver Disease (CLD)

• Platelet count <40,000/µL: 60 mg (three 20 mg tablets) once daily for 5 days
• Platelet count 40,000–50,000/µL: 40 mg (two 20 mg tablets) once daily for 5 days

Chronic Immune Thrombocytopenia (ITP)

• Starting dose: 20 mg once daily
• Dose adjustments may be required based on platelet response, with periodic monitoring.
• Administration Tips:
  • Take with food for optimal absorption.
  • Do not crush or chew the tablets.

Contraindications

Avatrombopag is contraindicated in patients with:

• Hypersensitivity to Avatrombopag or any excipient in the formulation
• Severe hepatic impairment (Child-Pugh Class C), unless benefits outweigh the risks

Warnings and Precautions

• **Increased platelet counts with Avatrombopag may raise the risk of thromboembolic events such pulmonary embolism (PE) or deep vein thrombosis (DVT). **Hepatic Considerations: Because chronic liver illness alters medication metabolism, patients should be closely watched.

  Long-term use may result in bone marrow fibrosis, which calls for routine blood tests.

  Drug Interactions:

  • Strong CYP3A4 or CYP2C9 inhibitors (e.g., ketoconazole) may increase Avatrombopag exposure.
  • CYP3A4 inducers (e.g., rifampin) may reduce its effectiveness.

Adverse Effects

Common Side Effects:

• Headache
• Nausea
• Fatigue
• Fever
• Abdominal pain

Serious Side Effects:

• Thromboembolic events (stroke, DVT, PE)
• Hepatic toxicity
• Severe hypersensitivity reactions

Clinical Studies

Several phase III clinical trials have demonstrated the efficacy and safety of Avatrombopag:

A 5-day protocol dramatically raises platelet counts for CLD, according to studies, which lowers the requirement for transfusions.

Avatrombopag efficiently regulates platelet counts in ITP, avoiding bleeding issues.

Conclusion

Avatrombopag Maleate (Doptelet) is a very effective and well-tolerated TPO receptor agonist for the treatment of thrombocytopenia in chronic liver disease and chronic ITP. Because of its oral administration, favorable pharmacokinetics, and lower risk of immunological reactions, it is an excellent alternative to more conventional thrombopoietic drugs like eltrombopag and romiplostim. However, its use must be carefully monitored due to the potential thrombotic risks.

Order Now At Mdx Pharma bd….

To order from MDX Pharma BD, visit their website at https://mdxpharmabd.com, where you can browse products and place orders online. For inquiries or orders via email, contact emedicarepharma@gmail.com. Alternatively, call (+88) 01929123476. Their address is 29, Abdullahpur, Uttara, Dhaka-1230, Bangladesh.

Q. Are avatrombopag and eltrombopag superior?
AVA-treated patients had a higher platelet level in the second month (p = 0.041) and a quicker median time to response (p = 0.012) than ELT-treated patients. Compared to ELT, AVA experienced fewer adverse events (p = 0.046).

Q. What is the price of avatrombopag?
Doptelet (avatrombopag), a medication that belongs to the class of platelet-stimulating medicines, is frequently used to treat thrombocytopenia and immune thrombocytopenia. Depending on the drugstore you visit, a supply of 30 Doptelet 20 mg oral tablets costs approximately $13,223.