Mecasermin rinfabate API Manufacturers

General Description:

Mecasermin rinfabate, identified by CAS number 478166-15-3, is a notable compound with significant therapeutic applications. Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH). Mecasermin rinfabate is similar to in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3). The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwide. Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines Agency.

Indications:

This drug is primarily indicated for: Mecasermin rinfabate was approved for treatment of severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH). Severe primary IGF-1 deficiency is defined by: A) height standard deviation (SD) score less than or equal to 3 SD below normal B) basal IGF-1 SD score less than or equal to 3 SD below normal C) normal or above normal levels of growth hormone In 2007, Insmed (Mecasermin rinfabate's manufacturer) made an agreement with Tercica (Mecasermin's manufacturer) that Mecasermin would no longer be available for this indication but could be developed for non short stature conditions such as severe insulin resistance, myotonic muscular dystrophy, and HIV associated adipose redistribution syndrome. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Mecasermin rinfabate undergoes metabolic processing primarily in: There is little published data on the pharmacokinetics of Mecasermin rinfabate. Mecasermin rinfabate is expected to degrade into small peptides and amino acids. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteases. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Mecasermin rinfabate are crucial for its therapeutic efficacy: There is little published data on the pharmacokinetics of Mecasermin rinfabate. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissue. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Mecasermin rinfabate is an important consideration for its dosing schedule: Half life ranges from 10 to 16 hours with a mean of 13 hours. Mecasermin rinfabate is said to have a longer half life than . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Mecasermin rinfabate exhibits a strong affinity for binding with plasma proteins: Mecasermin rinfabate is formulated as two proteins (IGF-1 and IGFBP-3) already bound together in the same way they are naturally found in the human body. This increases the serum half life of . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Mecasermin rinfabate from the body primarily occurs through: An excretion study in monkeys showed elimination in the urine 72 hours after administration. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Mecasermin rinfabate is distributed throughout the body with a volume of distribution of: Approximately 1000mL/kg. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Mecasermin rinfabate is a critical factor in determining its safe and effective dosage: Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg. Mecasermin rinfabate is said to have lower clearance than. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Mecasermin rinfabate exerts its therapeutic effects through: Mecasermin rinfabate promotes vertical growth in pediatric patients in a similar fashion to . 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. The structure of IGFBP-3 remains unsolved. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Mecasermin rinfabate functions by: Mecasermin rinfabate supplies recombinant-DNA-origin IGF-1 (rhIGF-1) bound to recombinant-DNA-origin IGFBP-3. 80% of IGF-1 is naturally bound to IGFBP-3 so the binding of rhIGF-1 to rhIGFBP-3 increases the half life of rhIGF-1 compared to . rhIGF-1 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Mecasermin rinfabate belongs to the None, classified under the direct parent group Peptides. This compound is a part of the Organic Compounds, falling under the Organic Acids superclass, and categorized within the Carboxylic Acids and Derivatives class, specifically within the Amino Acids, Peptides, and Analogues subclass.

Categories:

Mecasermin rinfabate is categorized under the following therapeutic classes: Anterior Pituitary Lobe Hormones and Analogues, Pituitary and Hypothalamic Hormones and Analogues, Somatropin and Somatropin Agonists, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Mecasermin rinfabate include:

• Water Solubility: Soluble