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Guselkumab API Manufacturers & Suppliers

General Description:

Guselkumab, identified by CAS number 1350289-85-8, is a notable compound with significant therapeutic applications. Guselkumab is a human immunoglobulin G1 lambda (IgG1λ) monoclonal antibody that selectively blocks interleukin-23. IL-23 is an inflammatory cytokine that activates the CD4+ T-helper (Th17) cell pathway to mediate the inflammatory cascade that induces psoriatic plaque formation . In clinical trials, guselkumab demonstrated improved skin clearance and symptomatic improvements in dermatological manifestations of psoriasis. Developed by Janssen, the subcutenous injection form of guselkumab was approved in July 2017 under the market name Tremfya for the treatment of adult patients with moderate-to-severe plaque psoriasis.

Indications:

This drug is primarily indicated for: Indicated for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Guselkumab undergoes metabolic processing primarily in: Like other human IgG monoclonal antibodies, guselkumab is expected to be degraded into small peptides and amino acids via catabolic pathways . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Guselkumab are crucial for its therapeutic efficacy: Following a 100mg subcutaneous administration, the peak plasma concentration (Cmax) of guselkumab is 8.09 ± 3.68 mcg/mL which is reached after approximately 5.5 days . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Guselkumab is an important consideration for its dosing schedule: Mean half-life of guselkumab is approximately 15 to 18 days in subjects with plaque psoriasis . This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Guselkumab from the body primarily occurs through: Like other human IgG monoclonal antibodies, guselkumab is expected to be both renally and fecally excreted as smaller peptide units. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Guselkumab is distributed throughout the body with a volume of distribution of: The apparent volume of distribution is 13.5 L . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Guselkumab is a critical factor in determining its safe and effective dosage: Apparent clearance in subjects with plaque psoriasis is 0.516 L/day . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Guselkumab exerts its therapeutic effects through: Guselkumab is shown to reduce serum levels of IL-17A, IL-17F and IL-22 . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Guselkumab functions by: Guselkumab targets the p19 alpha subunit of IL-23. While IL-23 promotes the normal inflammatory and immune responses, the p19 and p40 subunits of IL-23 are found to be over-expressed in the condition of psoriasis and other autoimmune inflammatory skin diseases . Guselkumab selectively binds to the p19 subunit of IL-23 in dendritic cells and keratinocytes and blocks its interaction with IL-23 receptor, which further prevents the release of other pro-inflammatory cytokines and chemokines via stimulation of immune cells such as Th17 cells . Thus, guselkumab blocks the abnormally-heightened signalling of inflammatory cascades that promote epidermal abnormalities including keratinocyte hyperproliferation and psoriatic plaque formation . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Guselkumab 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:

Guselkumab is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Antibodies, Antibodies, Monoclonal, Antineoplastic and Immunomodulating Agents, Blood Proteins, Globulins, Immunoglobulins, Immunoproteins, Immunosuppressive Agents, Interleukin Inhibitors, Interleukin-23 Antagonist, Interleukin-23 Subunit p19, Misc. Skin and Mucous Membrane Agents, 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 Guselkumab include:

• Molecular Weight: 143.6
• Molecular Formula: C6402H9864N1676O1994S42