Corticorelin ovine triflutate API Manufacturers

General Description:

Corticorelin ovine triflutate, identified by CAS number 121249-14-7, is a notable compound with significant therapeutic applications. Corticorelin, available commercially as corticorelin ovine triflutate (tradename Acthrel), is a synthetic form of the peptide human corticotropin-releasing hormone (hCRH), a potent stimulator of adrenocorticotropic hormone (ACTH) release from the anterior pituitary. Endogenous forms hCRH are involved in the stress response and its main function is stimulation of the pituitary to release ACTH. It is used as a diagnostic agent to evaluate the status of the pituitary-adrenal axis in the differentiation of a pituitary source from an ectopic source of excessive ACTH secretion. It provides a differential diagnosis for Cushing's disease (a pituitary source of ACTH excess) or of ectopic ACTH syndrome (an ectopic source of ACTH excess). If corticorelin injection results in an increase of plasma ACTH and cortisol, the patient is diagnosed with Cushing's disease. However, if corticorelin injection does not result in an increase of plasma ACTH and cortisol, the patient is diagnosed with ectopic ACTH syndrome.

Indications:

This drug is primarily indicated for: Corticorelin is indicated for use in differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Absorption:

The absorption characteristics of Corticorelin ovine triflutate are crucial for its therapeutic efficacy: Plasma ACTH levels in normal subjects increased 2 minutes after injection of corticorelin doses of ≥0.3 mcg/kg and reached peak levels after 10-15 minutes. Plasma cortisol levels increased within 10 minutes and reached peak levels at 30 to 60 minutes. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Corticorelin ovine triflutate is an important consideration for its dosing schedule: Plasma half-lives for IR-corticorelin are 11.6 ± 1.5 minutes (mean ± SE) for the fast component and 73 ± 8 minutes for the slow component. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Corticorelin ovine triflutate exhibits a strong affinity for binding with plasma proteins: Corticorelin does not appear to be bound specifically by a circulating plasma protein. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Volume of Distribution:

Corticorelin ovine triflutate is distributed throughout the body with a volume of distribution of: The mean volume of distribution for IR-corticorelin is 6.2 ± 0.5 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Corticorelin ovine triflutate is a critical factor in determining its safe and effective dosage: 95 ± 11 L/m2/day. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Corticorelin ovine triflutate exerts its therapeutic effects through: In normal subjects, intravenous administration of corticorelin results in a rapid and sustained increase of plasma ACTH levels and a near parallel increase of plasma cortisol. In addition, intravenous administration of corticorelin to normal subjects causes a concomitant and prolonged release of the related proopiomelanocortin peptides β- and γ-lipotropins (β -and γ-LPH) and β-endorphin (β -END). The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Corticorelin ovine triflutate functions by: Corticorelin is a potent stimulator of adrenocorticotropic hormone (ACTH) release from the anterior pituitary. It is used as a diagnostic agent to evaluate the status of the pituitary-adrenal axis in the differentiation of a pituitary source from an ectopic source of excessive ACTH secretion. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Corticorelin ovine triflutate 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:

Corticorelin ovine triflutate is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Diagnostic Agents, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Hypothalamic Hormones, Nerve Tissue Proteins, Neuropeptides, Peptide Hormones, Peptides, Pituitary Hormone-Releasing Hormones, Proteins, Tests for Pituitary Function. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.