Romosozumab API Manufacturers

General Description:

Romosozumab, identified by CAS number 909395-70-6, is a notable compound with significant therapeutic applications. Romosozumab is a humanized monoclonal antibody indicated for the treatment of osteoperosis in postmenopausal women at high risk of fracture and patients who have failed in other treatments or are intolerant to other osteoperosis therapies. Romosozumab prevents bone resorption and induces the formation of bone though it is associated with an increased risk of cardiac death, heart attack, and stroke in one study. In a comparison study of post menopausal women with osteoporosis and a past fracture, romosozumab for 12 months followed by alendronic acid for 12 months was superior to alendronic acid alone for 24 months. Romosozumab also demonstrates a faster and larger increase in bone density than teriparatide. Romosozumab is marketed in the United States by Amgen under the brand name Evinity. Romosozumab was granted FDA approval on April 9,2019.

Indications:

This drug is primarily indicated for: Romosozumab is indicated for the treatment of osteoporosis in post menopausal women at high risk of fractures and also in patients with osteoperosis who are intolerant to other treatments or who have failed in other treatments. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Romosozumab undergoes metabolic processing primarily in: The metabolism of romosozumab has not been clarified, however it is expected to be degraded into small peptides and amino acids like other protein drugs. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Romosozumab are crucial for its therapeutic efficacy: Romosozumab reaches peak concentration within 2 to 7 days with a median time of 5 days. Subcutaneous bioavailability is 50 to 70%. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Romosozumab is an important consideration for its dosing schedule: 12.8 days. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Romosozumab exhibits a strong affinity for binding with plasma proteins: Monoclonal antibodies are generally not protein bound. In about 10% to 18.1% of cases patients develop antibodies against romosozumab. 4.7% of the patients developed neutralizing antibodies. The presence of antibodies against romosozumab can reduce the availability of romosozumab by 22%, and 63% in the case of neutralizing antibodies. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Romosozumab from the body primarily occurs through: Monoclonal antibodies are eventually phagocytosed and broken down to smaller peptides and amino acids which are eliminated in a similar fashion to other proteins. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Romosozumab is distributed throughout the body with a volume of distribution of: 3.92L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Romosozumab is a critical factor in determining its safe and effective dosage: 0.38mL/hr/kg. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Romosozumab exerts its therapeutic effects through: Romosozumab is a subcutaneously injected humanized monoclonal antibody that inhibits the secreted protein sclerostin. Inhibition of this protein allows Wnt signalling in osteoblasts to promote bone formation and allows for the inhibition of receptor activator of nuclear factor kappa-beta-ligand (RANKL) mediated bone resorption by osteoclasts. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Romosozumab functions by: Osteocytes secrete sclerostin which inhibits bone formation by binding to low-density lipoprotein (LDL) receptor-related proteins 5 and 6 of osteoblasts, inhibiting the Wnt signal pathway. Romosozumab targets and inhibits the protein sclerostin, thereby preventing inhibition of bone formation by allowing Wnt to bind to LDL receptor-related proteins 5 and 6. Activation of the Wnt pathways leads to downstream signalling, translocation of beta catenin to the osteoblast nucleus where it promotes survival and proliferation of osteoblasts. Sclerostin also promotes bone resorption through increasing production of receptor activator of nuclear factor kappa-beta-ligand (RANKL). Romosozumab's inhibition of sclerostin also inhibits the increase in RANKL dependant increases in osteoclast activity and bone resorption. Both effects from the same therapy have not been seen in other osteoporosis treatments to date. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Romosozumab 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:

Romosozumab is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Antibodies, Antibodies, Monoclonal, Antibodies, Monoclonal, Humanized, Blood Proteins, Bone Anabolic Agents, Drugs Affecting Bone Structure and Mineralization, Drugs for Treatment of Bone Diseases, Globulins, Immunoglobulins, Immunoproteins, Musculo-Skeletal System, Proteins, Sclerostin Inhibitors, 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 Romosozumab include:

• Molecular Weight: 145805.0