Mecasermin
Mecasermin Uses, Dosage, Side Effects, Food Interaction and all others data.
Mecasermin contains recombinant-DNA-engineered human insulin-like growth factor-1 (rhIGF-1). IGF-1 consists of 70 amino acids in a single chain with three intramolecular disulfide bridges and a molecular weight of 7649 daltons. The amino acid sequence of the product is identical to that of endogenous human IGF-1. The rhIGF-1 protein is synthesized in bacteria (E. coli) that have been modified by the addition of the gene for human IGF-1.
Mecasermin is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth . Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects).
| Trade Name | Mecasermin |
| Availability | Prescription only |
| Generic | Mecasermin |
| Mecasermin Other Names | Mecasermin, Mecasermin recombinant, Mecasermina |
| Related Drugs | Increlex, iPlex |
| Weight | 10mg/ml, |
| Type | Subcutaneous Solution, Subcutaneous |
| Formula | C331H518N94O101S7 |
| Weight | 7649.0 Da |
| Protein binding | In blood, IGF-1 is bound to six IGF binding proteins, with > 80% bound as a complex with IGFBP-3 and an acid-labile subunit . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Mecasermin is a recombinant insulin-like growth factor-1 used for the long-term treatment of growth failure in pediatric patients with primary IGF-1 deficiency or with growth hormone gene deletion due to the development of neutralizing antibodies to GH.
For the long-term treatment of growth failure in pediatric patients with Primary IGFD or with GH gene deletion who have developed neutralizing antibodies to GH . It is not indicated to treat Secondary IGFD resulting from GH deficiency, malnutrition, hypothyroidism or other causes; it is not a substitute for GH therapy.
Mecasermin is also used to associated treatment for these conditions: Primary Insulin-like Growth Factor-1 Deficiency
How Mecasermin works
Mecasermin supplies recombinant-DNA-origin IGF-1, which binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth.
Toxicity
Overdosage of Mecasermin leads to hypoglycemia. One case of acute overdose was treated with IV glucose. Long-term overdosage may result in signs and symptoms of acromegaly. The effects of Mecasermin in human pregnancy has not been studied, however effects on fetal development in animal studies were only seen at doses higher than the maximum recommended human dose based on body surface area. Studies on excretion of the drug in human milk, use in patients under 2 years, use in patients over 65 years, or use in patients with renal or hepatic impairment have not been performed.
Food Interaction
- Take with food. Mecasermin should be administered shortly before or after a meal due to its hypoglycemic effects.
Mecasermin Drug Interaction
Unknown: charcoal, charcoal, multivitamin with minerals, multivitamin with minerals, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, ubiquinone, ubiquinone, copper gluconate, copper gluconate, glucose, glucose, diltiazem, diltiazem, metoprolol, metoprolol, metoprolol, metoprolol, cholecalciferol, cholecalciferol
Mecasermin Disease Interaction
Moderate: diabetics, lymphoid tissue hypertrophy, scoliosis, visual complications
Volume of Distribution
- 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] at a dose of 0.045mg/kg
Elimination Route
While the bioavailability of rhIGF-1 after subcutaneous administration in healthy subjects has been reported to be close to 100%, the absolute bioavailability of mecasermin given subcutaneously to subjects with primary insulin-like growth factor-1 deficiency (Primary IGFD) has not been determined.
Half Life
Mean half life of 5.8 hours
Clearance
Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) * Clearance is estimated to be 0.04L/hr/kg at 0.5 micrograms/mL of IGFBP-3 * Clearance is estimated to be 0.01L/hr/kg at 3 micrograms/mL of IGFBP-3 (the median level of IGFBP-3 for patients with normal IGF-1 levels)
Elimination Route
Information on the elimination of Mecasermin is not readily available, however it is likely to be metabolized by the liver and kidney like other injectable peptide drugs.
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