Avatrombopag Maleate- Thrombocytopenia, CAS No.: 677007-74-8

Avatrombopag Maleate - Thrombocytopenia: A Revolutionary Treatment for Low Blood Platelet Counts

Thrombocytopenia is a condition where the body has a low blood platelet count. These small cells, also known as thrombocytes, are necessary for the blood clotting process. If there are not enough platelets in the blood, it can lead to internal bleeding, which can be fatal.

Thrombocytopenia can be caused by several factors, such as chemotherapy, pregnancy, autoimmune diseases, or liver damage. Treatment for low blood platelet counts can be challenging, and current options include blood transfusions or immunoglobulin therapy. However, these treatments are not always practical, affordable, or effective.

Enter Avatrombopag Maleate, the first oral thrombopoietin receptor agonist approved by the FDA to treat thrombocytopenia. Avatrombopag Maleate raises platelet counts and can reduce the need for other treatments.

What is Avatrombopag Maleate?

Avatrombopag Maleate is a prodrug of avatrombopag, which is a small molecule that mimics thrombopoietin, a hormone that regulates platelet production. Avatrombopag targets and activates the thrombopoietin receptor, stimulating the bone marrow to produce more platelets.

The maleate salt form of avatrombopag enhances solubility and stability, allowing for oral administration. The tablet can be taken once a day for up to six months, depending on the patient's condition.

Clinical Trials Results

The FDA approved Avatrombopag Maleate based on two randomized, double-blind, placebo-controlled trials involving 435 patients with chronic liver disease and thrombocytopenia. The trials showed that Avatrombopag Maleate was effective in raising platelet counts to a safe level and maintaining them for at least six months.

In the first trial, published in The New England Journal of Medicine, the proportion of patients who achieved a platelet count of at least 50,000 per cubic millimeter without rescue therapy on day eight of treatment was significantly higher in the Avatrombopag group (88 percent) than in the placebo group (37 percent). The adverse events observed were mild or moderate and mainly consisted of headache, nausea, and fatigue.

In the second trial, published in Hepatology, patients with chronic liver disease and thrombocytopenia who received Avatrombopag Maleate had a 30-percent reduction in bleeding events compared to placebo. Patients also experienced a significant improvement in the quality of life, which is often compromised by thrombocytopenia.

Advantages of Avatrombopag Maleate

Avatrombopag Maleate offers several advantages over other treatments for thrombocytopenia, such as:

1. Oral administration: Avatrombopag Maleate can be taken at home, reducing the need for hospital visits and transfusions.

2. Convenience: Avatrombopag Maleate is a once-daily tablet, making it easier for patients to adhere to treatment.

3. Safety: Avatrombopag Maleate has a favorable safety profile, with adverse events mainly consisting of mild or moderate side effects.

4. Efficacy: Avatrombopag Maleate has been shown to raise platelet counts to a safe level and maintain them for at least six months.

5. Affordability: Avatrombopag Maleate is priced competitively compared to other thrombopoietin receptor agonists.

Conclusion

Avatrombopag Maleate is a breakthrough treatment for thrombocytopenia that offers several advantages, including oral administration, convenience, safety, efficacy, and affordability. If you are a merchant outside of China looking to provide your customers with a revolutionary product that can improve their quality of life, consider Avatrombopag Maleate. As a manufacturer, we can provide you with high-quality Avatrombopag Maleate at competitive prices. Contact us today to learn more about our product and how we can help you meet your customers' needs.

DESCRIPTION

The active ingredient in AVATROMBOPAG MALEATE is avatrombopag maleate, a thrombopoietin receptor agonist. The chemical name of avatrombopag maleate is

4 piperidinecarboxylic acid, 1-[3-chloro-5-[[[4-(4-chloro-2 thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-, (2Z)-2-butenedioate (1:1). It has the molecular formula C29H34Cl2N6O3S2 · C4H4O4. The molecular weight is 765.73.

The structural formula is:

The aqueous solubility of avatrombopag maleate at various pH levels indicates that the drug substance is practically insoluble at pH 1 to 11.

AVATROMBOPAG MALEATE is provided as an immediate-release tablet. Each AVATROMBOPAG MALEATE tablet contains 20 mg avatrombopag (equivalent to 23.6 mg of avatrombopag maleate) and the following inactive ingredients: lactose monohydrate, colloidal silicon dioxide, crospovidone, magnesium stearate and microcrystalline cellulose. Coating film:

polyvinyl alcohol, talc, polyethylene glycol, titanium dioxide and ferric oxide yellow.

Mechanism of Action

Avatrombopag is an orally bioavailable, small molecule TPO receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, resulting in an increased production of platelets. Avatrombopag does not compete with TPO for binding to the TPO receptor and has an additive effect

with TPO on platelet production.

Pharmacodynamics

Platelet Response

AVATROMBOPAG MALEATE administered to adult patients resulted in dose- and exposure-dependent elevations in platelet counts. The onset of the platelet count increase was observed within 3 to 5 days of the start of treatment, with peak effect after 10 to 13 days. Post treatment, platelet counts decreased gradually, returning to near baseline

values.

Name: Avatrombopag maleate

Avatrombopag maleate is a prescription medicine used to treat the symptoms of Thrombocytopenia (lack of platelets in the blood).

Indications

Treatment Of Thrombocytopenia In Patients With Chronic Liver Disease (CLD)

Avatrombopag maleate is indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure.

Treatment Of Thrombocytopenia In Patients With Chronic Immune Thrombocytopenia (ITP)

Avatrombopag maleate is indicated for the treatment of thrombocytopenia in adult patients with chronic immune thrombocytopenia who have had an insufficient response to a previous treatment.

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Company Honor

National New High-tech Enterprise

Key New High-tech Enterprise of National Torch Plan

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Provincial New High-tech Research & Development Center

Zhejiang Provincial Enterprise Technology Center

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Zhejiang Jiuyuan Gene Engineering Biopharmaceutical Research Institute

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