Romiplostim

Specification

• Cat#: THP-0207
• Product Name: Romiplostim
• Description: The product is a thrombopoiesis stimulating dimer Fc-peptide fusion protein (peptibody) to increase platelet production through activation of the thrombopoietin receptor. The peptibody molecule has two identical single-chain subunits, each one is made up of 269 amino acid residues. Each subunit consists of an IgG1 Fc carrier domain that is covalently attached to a polypeptide sequence that contains two binding domains to interact with thrombopoietin receptor c-Mpl. Each domain consists of 14 amino acids.
• Sequences: Thrombopoietin receptor binding domain amino acid sequence: IEGPTLRQWLAARA Amino acid sequence for Fc fusion compound: MDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGGIEGPTLRQWLAARAGGGGGGGGIEGPTLRQWLAARA
• Species: Human
• Molecular Weight: 59000.0 Da
• Purity: >99% by SDS-Page and HPLC analysis
• Cas No: 267639-76-9
• Formula: C2634H4086N722O790S18
• Endotoxin Level: <0.001 EU per 1 μg of the peptide by the LAL method
• Biological Activity: 125ug/250ug/500ug

Pharmaceutical Information

• Pharmaceutical Application: Romiplostim
• Applications: Treatment of chronic immune thrombocytopenic purpura.
• Examples of Clinical Use: Chronic immune thrombocytopenic purpura
• Pharmacodynamics: Responses to platelet increase varies between patients thus indicating a need for individualization of dose. However, a dose dependent-increase in platelet counts have been observed in clinical trials. Does not affect platelet destruction.
• Mechanism of action: Romiplostim is a thrombopoietin receptor agonist that activates intracellular transcriptional pathways via c-Mpl to increase production of platelets. It also works similarly to thrombopoietin (TPO), an endogenous glycoprotein hormone that regulates the production of platelets in the bone marrow.
• Affected organisms: Humans and other mammals
• Targets: Target 1. Thrombopoietin receptor

Related Reading

Romiplostim is an artificially synthesized thrombopoietin that serves as a biological analogue and can be used to treat specific types of thrombocytopenia.

Background of Romiplostim

Human thrombopoietin (TPO) is an important cytokine that mediates the maturation and release of platelets. Romiplostim is a recombinant fusion protein formed by the fusion of human thrombopoietin and human IgG1 Fc region. The unique feature of Romiplostim is that it targets the TPO receptor (c-MPL), which promotes platelet production.

Structure of Romiplostim

Romiplostim is a fusion protein composed of 533 amino acid residues, with a molecular weight of approximately 60kDa. Due to its fusion protein in the human IgG1 Fc region, Romiplostim interacts with Fc γ Receptor binding stimulates the body's immune response.

Research and development history of Romiplostim

Romiplostim was developed by American biotechnology company Amgen and obtained FDA approval in 2008. It is approved for the treatment of adult patients with chronic immune thrombocytopenia (ITP). Afterwards, Romiplostim was widely used globally for the treatment of ITP.

The function of Romiplostim

Romiplostim activates hematopoietic stem cells and precursor cell by binding to TPO receptors, promotes the maturation of existing platelets and increases the number of platelets. This treatment can significantly increase the patient's platelet count and reduce the risk of bleeding associated with thrombocytopenia.

The mechanism of action of Romiplostim

Romiplostim combines with TPO receptor to stimulate hematopoietic stem cells/Precursor cell to proliferate and differentiate into mature platelets. Romiplostim can enhance the differentiation of platelet mother cells in bone marrow and stimulate the release of more platelets into the bloodstream.

Romiplostim related drugs

Prior to Romiplostim, there were several other thrombopoietin analogues used for the treatment of ITP, including Elthrombopag and Avatrombopag. These drugs differ from Romiplostim in that they primarily maintain the proliferation and differentiation of hematopoietic stem cells, rather than directly acting on mature platelets. In addition, the common IgG1 Fc region contained in Romiplostim may have adverse effects on the patient's immune response, resulting in some missing fusion proteins in the Fc region targeting TPO (such as Eltrombopag oral tablets and Avatrombopag oral tablets).