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Desoxycorticosterone pivalate | CAS No: 808-48-0 | GMP-certified suppliers
A medication that supports mineralocorticoid replacement for managing adrenal insufficiency and Addison’s disease primarily in veterinary applications.
Therapeutic categories
Primary indications
- Examined for treatment of adrenocortical insufficiency especially in multiple sclerosis, congenital cerebral palsy, polyarteritis nodosa, and rheumatoid arthritis
- Currently only approved in treating cats and dogs for the treatment of Addison's disease
Product Snapshot
- Desoxycorticosterone pivalate is formulated as an injectable peptide
- It is primarily used for managing adrenocortical insufficiency and related autoimmune conditions in veterinary medicine
- The product holds veterinary approval for treating Addison's disease in cats and dogs, with experimental status in human applications
Clinical Overview
Clinically, desoxycorticosterone pivalate is approved for veterinary use in managing Addison’s disease in dogs and cats, where mineralocorticoid replacement is essential. Historically, it has been examined experimentally for treatment of adrenocortical insufficiency in human conditions including multiple sclerosis, congenital cerebral palsy, polyarteritis nodosa, and rheumatoid arthritis, though such applications remain outside current approved indications.
Pharmacologically, the compound acts by mimicking endogenous mineralocorticoids, primarily influencing sodium, potassium, and water metabolism. Administration results in decreased renal sodium excretion accompanied by increased potassium excretion. These effects lead to elevated plasma sodium concentrations, reduced potassium levels, expansion of blood and extracellular fluid volumes, and a reduction in hematocrit. The increased renal tubular reabsorption of sodium underpins these physiological responses.
The mechanism of action involves binding to the mineralocorticoid receptor, a nuclear receptor that regulates gene transcription related to electrolyte and fluid balance. Upon ligand binding, the steroid-receptor complex translocates to the cell nucleus, binding chromatin to activate transcription of target genes. This genomic action promotes synthesis of proteins responsible for the mineralocorticoid's physiological effects.
Metabolic considerations include activity as a substrate of cytochrome P-450 enzymes, specifically CYP3A4, implicating possible drug-drug interaction potential through this pathway. Safety and toxicity data in veterinary use emphasize proper dosing to avoid mineralocorticoid excess, which can result in hypertension, electrolyte disturbances, and fluid retention.
From a sourcing perspective, quality control must ensure chemical purity and stability consistent with pharmaceutical-grade standards. Given the compound’s poor aqueous solubility and sensitivity to air, appropriate handling and formulation strategies are critical. API procurement should include verification of compliance with relevant regulatory guidelines and confirmation of material traceability to support veterinary pharmaceutical manufacturing.
Identification & chemistry
| Generic name | Desoxycorticosterone pivalate |
|---|---|
| Molecule type | Small molecule |
| CAS | 808-48-0 |
| UNII | 16665T4A2X |
| DrugBank ID | DB01134 |
Pharmacology
| Summary | Desoxycorticosterone pivalate is a mineralocorticoid receptor agonist that modulates electrolyte and fluid balance by promoting renal sodium reabsorption and potassium excretion. Its mechanism involves nuclear receptor activation leading to transcriptional regulation of proteins involved in electrolyte metabolism. Therapeutically, it is used to manage adrenocortical insufficiency by restoring mineralocorticoid activity. |
|---|---|
| Mechanism of action | Desoxycorticosterone Pivalate binds to the mineralocorticoid receptor. Mineralocorticoids are a family of steroids, secreted by the adrenal cortex, necessary for the regulation of a number of metabolic processes including electrolyte regulation. Desoxycorticosterone pivalate exerts its effect through its interaction with the mineralocorticoid receptor (MR), whereby it reacts with the receptor proteins to form a steroid-receptor complex. This complex moves into the nucleus, where it binds to chromatin which results in genetic transcription of cellular DNA to messenger RNA. The steroid hormones appear to induce transcription and synthesis of specific proteins, which produce the physiological effects seen after administration. |
| Pharmacodynamics | Used to treat adrenocortical insufficiency, desoxycorticosterone pivalate is a mineralocorticoid hormone and an analogue of desoxycorticosterone. It primarily acts on the metabolism of sodium, potassium and water. When the drug is given, there is decreased excretion of sodium accompanied by increased excretion of potassium; the concentration of sodium in the blood is thereby increased whereas that of potassium is decreased. There is a concomitant increase in the volume of blood and extracellular fluids, with a fall in hematocrit. It increases the rate of renal tubular absorption of sodium. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mineralocorticoid receptor | Humans | agonist |
ADME / PK
| Protein binding | 90% |
|---|
Formulation & handling
- Desoxycorticosterone pivalate is a small molecule steroid with low aqueous solubility, indicating formulation challenges for oral bioavailability. Its high LogP suggests lipophilicity, favoring lipid-based or depot formulations for sustained release. Stability considerations include protection from hydrolysis and oxidation given its steroid structure.
Regulatory status
Supply Chain
| Supply chain summary | Desoxycorticosterone pivalate is primarily supplied by originator companies involved in its packaging and distribution. Branded products for this API have a global presence, including markets in the US, EU, and other regions. Patent expirations have led to, or are expected to lead to, increased availability of generic alternatives in relevant markets. |
|---|
Safety
| Toxicity | Symptoms of overdose include polyuria, polydipsia, increased blood volume, edema, and cardiac enlargement. |
|---|
- Overdose may result in fluid retention symptoms including polyuria, polydipsia, edema, and cardiac enlargement
- Monitor for signs of increased blood volume to mitigate potential cardiovascular stress
- Handle with appropriate protective measures to avoid exposure, considering systemic effects from absorption
Desoxycorticosterone Pivalate is a type of Adrenocorticotropic hormones
Adrenocorticotropic hormones (ACTH) belong to the pharmaceutical API (Active Pharmaceutical Ingredient) subcategory, playing a vital role in the endocrine system. ACTH, also known as corticotropin, is a hormone synthesized and secreted by the anterior pituitary gland.
ACTH acts as a key regulator of the body's response to stress, controlling the production and release of cortisol, a hormone essential for various physiological processes. Its primary function is to stimulate the adrenal cortex to produce and secrete cortisol, which is crucial for maintaining normal metabolism, immune response, and stress adaptation.
Pharmaceutical companies produce synthetic ACTH as an API, which can be utilized for therapeutic purposes. It is commonly used in medical treatments involving adrenal insufficiency, such as Addison's disease. Synthetic ACTH helps to diagnose and manage these conditions by stimulating the adrenal glands to produce cortisol, aiding in the restoration of hormonal balance.
Moreover, ACTH is also used in diagnostic procedures to assess the functionality of the adrenal glands. By administering synthetic ACTH, healthcare professionals can evaluate the response of the adrenal glands and diagnose conditions like adrenal gland disorders or pituitary gland abnormalities.
In conclusion, ACTH is an important pharmaceutical API subcategory that encompasses synthetic corticotropin hormone. Its clinical applications include treatment of adrenal insufficiency and diagnosis of adrenal gland disorders. Pharmaceutical companies manufacture synthetic ACTH to ensure the availability of this crucial hormone for medical interventions.
Desoxycorticosterone Pivalate (Adrenocorticotropic hormones), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
Desoxycorticosterone Pivalate API manufacturers & distributors
Compare qualified Desoxycorticosterone Pivalate API suppliers worldwide. We currently have 1 companies offering Desoxycorticosterone Pivalate API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
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