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General Description:

Burosumab, identified by CAS number 1610833-03-8, is a notable compound with significant therapeutic applications. Burosumab (KRN23) is an entirely human monoclonal IgG1 antibody that binds excess fibroblast growth factor 23 (FGF23) and has been successfully tested in clinical trials in children with X-linked hypophosphatemic rickets . The U.S. Food and Drug Administration approved Crysvita (burosumab) in April 2018. This is the first drug approved to treat adults and children ages 1 year and older with X-linked hypophosphatemia (XLH), which is a rare, inherited form of rickets. X-linked hypophosphatemia causes low circulating levels of phosphorus in the blood. It causes impaired bone growth and development in children and adolescents and issues with bone mineralization throughout a patient’s life . XLH is a serious disease which affects about 3,000 children and 12,000 adults in the United States. Most children with XLH suffer from bowed or bent legs, short stature, bone pain and severe dental pain. Some adults with this condition suffer from persistent, unrelenting discomfort and complications, such as joint pain, impaired mobility, tooth abscesses and hearing loss .

Indications:

This drug is primarily indicated for: This drug is indicated for the treatment of X-linked hypophosphatemia with radiological evidence of bone disease in children of 1 year of age and older and adolescents with growing skeletons . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Burosumab undergoes metabolic processing primarily in: Burosumab is composed solely of amino acids and carbohydrates as a native immunoglobulin and is unlikely to be eliminated via hepatic metabolic mechanisms. Its metabolism and elimination are expected to follow the immunoglobulin clearance pathways, resulting in degradation to small peptides and individual amino acids . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Burosumab are crucial for its therapeutic efficacy: Burosumab absorption after subcutaneous injection sites into to the blood circulation is nearly complete. Following the subcutaneous route of administration, the time to reach maximum serum concentrations (Tmax) of burosumab is estimated at 5-10 days. The peak serum concentration (Cmax) and area under the concentration-time curve (AUC) of serum burosumab is proportional to the dose, over the dose range of 0.1-2.0 mg/kg . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Burosumab is an important consideration for its dosing schedule: About 19 days . This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Burosumab from the body primarily occurs through: Because of its molecular size, burosumab is not likely to be directly excreted . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Burosumab is distributed throughout the body with a volume of distribution of: Burosumab is comprised solely of amino acids and carbohydrates as a native immunoglobulin and is not likeluy to be eliminated by hepatic metabolic mechanisms. The metabolism of burosumab and elimination are expected to follow the immunoglobulin clearance pathways, which results in its degradation to smaller peptides and amino acids . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Burosumab is a critical factor in determining its safe and effective dosage: The clearance of burosumab depends on weight and is estimated to be 0.290 L/day and 0.136 L/day in a typical adult (70 kg) and pediatric (30 kg) XLH patient, respectively . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Burosumab exerts its therapeutic effects through: This drug has the ability to reduce the loss of phosphate, to improve pathologically low serum phosphate concentrations and other metabolic changes, as well as to reduce the severity of rickets as seen radiographically . In summary, this drug works to support of bone mineralization . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Burosumab functions by: Burosumab is a recombinant human monoclonal antibody (IgG1) that both binds to and inhibits the actions of fibroblast growth factor 23 (FGF23). By inhibiting this growth factor, burosumab increases the tubular reabsorption of phosphate from the kidney and thus increases serum concentration of 1, 25 dihydroxy-Vitamin D . This form of vitamin D enhances intestinal absorption of phosphate and calcium, supporting bone mineralization . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Burosumab 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:

Burosumab is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Antibodies, Antibodies, Monoclonal, Blood Proteins, Drugs Affecting Bone Structure and Mineralization, Drugs for Treatment of Bone Diseases, Fibroblast Growth Factor-23 Blocking Antibodies, Globulins, Immunoglobulins, Immunoproteins, Musculo-Skeletal System, Proteins, Serum Globulins. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Burosumab include:

• Molecular Weight: 144100.0
• Molecular Formula: C6388H9904N1700O2006S46