Romiplostim
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Identification
- Summary
Romiplostim is a fusion protein thrombopoietin (TPO) peptide analog that increases platelet counts by binding to and activating the human TPO receptor. Used to treat thrombocytopenia associated with chronic immune thrombocytopenia (ITP).
- Brand Names
- Nplate
- Generic Name
- Romiplostim
- DrugBank Accession Number
- DB05332
- Background
Romiplostim 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. Interestingly, romiplostim's amino acid sequence is not similar to that of endogenous thrombopoietin. Romiplostim is produced by recombinant DNA technology in Escherichia coli. FDA approved on August 22, 2008.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Haematopoietic growth factors - Protein Chemical Formula
- C2634H4086N722O790S18
- Protein Average Weight
- 59000.0 Da
- Sequences
>Thrombopoietin receptor binding domain amino acid sequence IEGPTLRQWLAARA
>Amino acid sequence for Fc fusion compound MDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYV DGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKA KGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLD SDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGGIEGPTLR QWLAARAGGGGGGGGIEGPTLRQWLAARA
Download FASTA Format- Synonyms
- Romiplostim
- External IDs
- AMG 531
- AMG-531
Pharmacology
- Indication
Treatment of chronic immune thrombocytopenic purpura.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Chronic immune thrombocytopenia •••••••••••• Management of Refractory immune thrombocytopenia •••••••••••• - Contraindications & Blackbox Warnings
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- 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.
Target Actions Organism AThrombopoietin receptor agonistHumans - Absorption
Cmax, healthy volunteers, subQ = 24-36 hours; Cmax, immune thrombocytopenia patients, subQ = 7-50 hours (median = 14 hours). Not affected by age, weight, or gender. Accumulation does not occur after six weekly doses of 3 mcg/kg romiplostim.
- Volume of distribution
In healthy volunteers, non-linear decrease in Vd with increase IV dose of romiplostim which indicates saturation of c-Mpl receptors. Vd, 0.3 μg/kg = 122 mL/kg Vd, 10 μg/kg = 48.2 mL/kg
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Renal clearance (more dominant mode of clearance as dose increases) and
binding to c-Mpl receptors (dominant mode of clearance at low doses)- Half-life
Immune thrombocytopenia patients, subQ = 3.5 days (median) (range 1-34 days)
- Clearance
Not Available
- Adverse Effects
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- Toxicity
The most common adverse reactions (≥ 5% higher patient incidence in Nplate versus placebo) are arthralgia, dizziness, insomnia, myalgia, pain in extremity, abdominal pain, shoulder pain, dyspepsia, and paresthesia. Headache was the most commonly reported adverse reaction that did not occur at ≥ 5% higher patient incidence in Nplate versus placebo. LD50 = 980 mg/kg.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareCyclophosphamide The risk or severity of pulmonary toxicity can be increased when Romiplostim is combined with Cyclophosphamide. Vinblastine The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vinblastine. Vincristine The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vincristine. Vindesine The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vindesine. Vinflunine The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vinflunine. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nplate Powder, for solution 250 mcg / vial Subcutaneous Amgen Europe B.V. 2009-04-15 Not applicable Canada Nplate Injection, powder, for solution 125 mcg Subcutaneous Amgen Europe B.V. 2020-12-16 Not applicable EU Nplate Injection, powder, for solution 500 mcg Subcutaneous Amgen Europe B.V. 2016-09-08 Not applicable EU Nplate Injection, powder, for solution 500 mcg Subcutaneous Amgen Europe B.V. 2016-09-08 Not applicable EU Nplate Injection, powder, for solution 250 mcg Subcutaneous Amgen Europe B.V. 2016-09-08 Not applicable EU
Categories
- ATC Codes
- B02BX04 — Romiplostim
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Biological Factors
- Blood and Blood Forming Organs
- Carbohydrates
- Colony-Stimulating Factors
- Cytokines
- Glycoconjugates
- Glycoproteins
- Hematopoietic Cell Growth Factors
- Hemostatics
- Increased Megakaryocyte Maturation
- Increased Platelet Production
- Intercellular Signaling Peptides and Proteins
- Membrane Proteins
- Peptides
- Proteins
- Receptors, Thrombopoietin, agonists
- Recombinant Proteins
- Thrombopoietin Receptor Agonist
- Thrombopoietin Receptor Agonists
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- GN5XU2DXKV
- CAS number
- 267639-76-9
References
- General References
- Kumagai Y, Fujita T, Ozaki M, Sahashi K, Ohkura M, Ohtsu T, Arai Y, Sonehara Y, Nichol JL: Pharmacodynamics and pharmacokinetics of AMG 531, a thrombopoiesis-stimulating peptibody, in healthy Japanese subjects: a randomized, placebo-controlled study. J Clin Pharmacol. 2007 Dec;47(12):1489-97. Epub 2007 Oct 9. [Article]
- Rice L: Drug evaluation: AMG-531 for the treatment of thrombocytopenias. Curr Opin Investig Drugs. 2006 Sep;7(9):834-41. [Article]
- Keating GM: Romiplostim: a review of its use in immune thrombocytopenia. Drugs. 2012 Feb 12;72(3):415-35. doi: 10.2165/11208260-000000000-00000. [Article]
- Link [Link]
- External Links
- KEGG Drug
- D08990
- PubChem Substance
- 347910087
- 805452
- ChEMBL
- CHEMBL1201832
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Romiplostim
- FDA label
- Download (232 KB)
- MSDS
- Download (479 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Immune Thrombocytopenia (ITP) 2 somestatus stop reason just information to hide Not Available Completed Not Available Thrombocytopenia 1 somestatus stop reason just information to hide Not Available Completed Not Available Wiskott-Aldrich Syndrome (WAS) 1 somestatus stop reason just information to hide Not Available Completed Treatment Hematology / Myelodysplastic Syndrome / Thrombocytopenia 1 somestatus stop reason just information to hide 4 Completed Treatment Immune Thrombocytopenia (ITP) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Subcutaneous 125 MCG Injection, powder, for solution Subcutaneous 250 MCG Injection, powder, for solution Subcutaneous 500 MCG Injection, powder, lyophilized, for solution Subcutaneous 125 ug/0.25mL Injection, powder, lyophilized, for solution Subcutaneous 250 ug/0.5mL Injection, powder, lyophilized, for solution Subcutaneous 500 ug/1mL Powder, for solution Subcutaneous 250 mcg / vial Powder, for solution Subcutaneous 500 mcg / vial Injection, powder, lyophilized, for solution Subcutaneous 625 mcg Injection, solution 250 mcg Injection, solution 500 mcg Injection, powder, lyophilized, for solution Subcutaneous 250 mcg Injection, powder, for solution Subcutaneous 250 mcg/1vial Injection, powder, for solution Subcutaneous Injection, powder, for solution Subcutaneous 250 mcg/0.5ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor for thrombopoietin that acts as a primary regulator of megakaryopoiesis and platelet production. May represent a regulatory molecule specific for TPO-R-dependent immune responses
- Specific Function
- thrombopoietin receptor activity
- Gene Name
- MPL
- Uniprot ID
- P40238
- Uniprot Name
- Thrombopoietin receptor
- Molecular Weight
- 71244.08 Da
References
- Krzyzanski W, Sutjandra L, Perez-Ruixo JJ, Sloey B, Chow AT, Wang YM: Pharmacokinetic and pharmacodynamic modeling of romiplostim in animals. Pharm Res. 2013 Mar;30(3):655-69. doi: 10.1007/s11095-012-0894-2. Epub 2012 Dec 19. [Article]
Drug created at November 18, 2007 18:23 / Updated at June 03, 2022 07:24