Somapacitan API Manufacturers

General Description:

Somapacitan, identified by CAS number 1338578-34-9, is a notable compound with significant therapeutic applications. Somapacitan, also known as NNC0195-0092, is a growth hormone analog indicated to treat adults with growth hormone deficiency. This human growth hormone analog differs by the creation of an albumin binding site, and prolonging the effect so that it requires weekly dosing rather than daily. Somapacitan was granted FDA approval on 28 August 2020.

Indications:

This drug is primarily indicated for: Somapacitan is indicated as a replacement for growth hormone in adult patients with growth hormone deficiency. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Somapacitan undergoes metabolic processing primarily in: Studies in humans and rats show that somapacitan is metabolized through cleavage of the albumin-binding moiety and linker sidechain before further non-specific mechanisms. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Somapacitan are crucial for its therapeutic efficacy: A 0.02mg/kg single dose of somapacitan reaches a C_max of 14.4 ng/mL, with a T_max of 11.1 hours, and an AUC of 475 ng\*h/mL. A 0.04mg/kg single dose of somapacitan reaches a C_max of 19.8 ng/mL, with a T_max of 25.6 hours, and an AUC of 777 ng\*h/mL. A 0.08mg/kg single dose of somapacitan reaches a C_max of 64.2 ng/mL, with a T_max of 16.6 hours, and an AUC of 2753 ng\*h/mL. A 0.12mg/kg single dose of somapacitan reaches a C_max of 142.5 ng/mL, with a T_max of 22.5 hours, and an AUC of 6382 ng\*h/mL. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Somapacitan is an important consideration for its dosing schedule: The elimination half life of somapacitan is 2-3 days. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Somapacitan exhibits a strong affinity for binding with plasma proteins: Somapacitan is >99% bound to albumin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Somapacitan from the body primarily occurs through: Somapacitan is approximately 81% eliminated in the urine and 13% in the feces. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Somapacitan is distributed throughout the body with a volume of distribution of: The approximate volume of distribution of somapacitan is 14.6 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Somapacitan is a critical factor in determining its safe and effective dosage: The apparent maximum rate of saturable elimination is estimated to be 0.268 ± 0.03 mg/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Somapacitan exerts its therapeutic effects through: Somapacitan stimulates the growth hormone receptor. Somapacitan has a long duration of action as it is given once weekly. It has a moderately wide therapeutic window as an acute overdose may cause hypoglycemia followed by hyperglycemia. Patients should be counselled regarding the risk of increased mortality in patients with critical illness, risk of neoplasms, glucose intolerance in diabetes mellitus, intracranial hypertension, hypersensitivity, fluid retention, hypoadrenalism, hypothyroidism, pancreatitis, lipohypertrophy, and lipoatrophy. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Somapacitan functions by: Somapacitan binds to the growth hormone receptor and induces intracellular signalling to up-regulate insulin-like growth factor I (IGF-1). IGF-1 causes growth in bones and muscle tissue. Growth hormones more directly cause the fusion of myoblasts and myotubes to cause muscle fibre growth, activate neural stem cells, and induce chondrocyte proliferation. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Somapacitan 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:

Somapacitan is categorized under the following therapeutic classes: Alcohols, Amino Acids, Amino Acids, Cyclic, Amino Acids, Essential, Amino Acids, Peptides, and Proteins, Anterior Pituitary Lobe Hormones and Analogues, Benzene Derivatives, Carbohydrates, Cytochrome P-450 CYP1A2 Inducers, Cytochrome P-450 CYP1A2 Inducers (strength unknown), Cytochrome P-450 CYP2C19 Inhibitors, Cytochrome P-450 CYP2C19 inhibitors (strength unknown), Cytochrome P-450 Enzyme Inducers, Cytochrome P-450 Enzyme Inhibitors, Growth Hormone, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Human Growth Hormone Analogs, Lipids, Peptide Hormones, Peptides, Phenols, Pituitary and Hypothalamic Hormones and Analogues, Pituitary Hormones, Pituitary Hormones, Anterior, Somatropin and Somatropin Agonists, Sugar Alcohols, 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 Somapacitan include:

• Molecular Formula: C1038H1609N273O319S9