Romiplostim
Romiplostim Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Romiplostim |
| Availability | Prescription only |
| Generic | Romiplostim |
| Romiplostim Other Names | Romiplostim |
| Related Drugs | Nplate, Promacta, prednisone, dexamethasone, triamcinolone, Decadron |
| Weight | 125mcg, 250mcg, 500mcg, |
| Type | Subcutaneous Powder For Injection, Subcutaneous |
| Formula | C2634H4086N722O790S18 |
| Weight | 59000.0 Da |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
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).
Treatment of chronic immune thrombocytopenic purpura.
Romiplostim is also used to associated treatment for these conditions: Chronic immune thrombocytopenia, Refractory immune thrombocytopenia
How Romiplostim works
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.
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.
Food Interaction
No interactions found.Romiplostim Disease Interaction
Major: leukemiaModerate: hepatic impairment, renal impairment
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
Elimination Route
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.
Half Life
Immune thrombocytopenia patients, subQ = 3.5 days (median) (range 1-34 days)
Elimination Route
Renal clearance (more dominant mode of clearance as dose increases) and
binding to c-Mpl receptors (dominant mode of clearance at low doses)
Innovators Monograph
You find simplified version here Romiplostim
