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Calcifediol | CAS No: 19356-17-3 | GMP-certified suppliers
A medication that treats vitamin D deficiency, refractory rickets, hypoparathyroidism, and manages hypocalcemia and osteoporosis in patients with renal failure or corticosteroid use.
Therapeutic categories
Primary indications
- Used to treat vitamin D deficiency or insufficiency, refractory rickets (vitamin D resistant rickets), familial hypophosphatemia and hypoparathyroidism, and in the management of hypocalcemia and renal osteodystrophy in patients with chronic renal failure undergoing dialysis
- Also used in conjunction with calcium in the management and prevention of primary or corticosteroid-induced osteoporosis
Product Snapshot
- Calcifediol is available as oral capsules and solutions, as well as intravenous injectable formulations
- It is primarily used for managing vitamin D deficiency and related conditions, including hypophosphatemia, hypoparathyroidism, renal osteodystrophy, and osteoporosis
- Calcifediol holds approved regulatory status in the US and Canada, with availability as both an approved pharmaceutical and a nutraceutical product
Clinical Overview
Pharmacologically, calcifediol functions as a prohormone that requires further activation via renal 1-alpha hydroxylation to calcitriol, the biologically active hormone. Calcitriol modulates calcium and phosphorus homeostasis by binding to the vitamin D receptor (VDR), a nuclear receptor that forms a heterodimer with the retinoid-X receptor (RXR). This complex regulates gene transcription, leading to increased intestinal absorption of calcium and phosphorus, enhanced renal tubular calcium reabsorption, and promotion of bone mineralization. Deficiency of vitamin D metabolites results in impaired mineralization of bone matrix, manifesting as rickets in children and osteomalacia in adults.
Key ADME parameters include hepatic conversion of cholecalciferol to calcifediol, followed by renal hydroxylation to calcitriol. Factors affecting liver or kidney function can alter serum levels and bioavailability. The metabolism of calcifediol involves classical steroid hormone pathways, with a secosteroid backbone characteristic of vitamin D derivatives.
Safety considerations include monitoring for hypercalcemia and hyperphosphatemia, especially in patients with compromised renal function or those receiving concurrent calcium supplementation. Long-term or excessive dosing requires vigilance to prevent calcification-related toxicities.
Notable pharmaceutical products may include calcifediol formulations approved for clinical use and nutraceutical preparations with variable regulatory status. In the context of API procurement, quality control should focus on identity confirmation, assay of potency, purity profiling, and compliance with pharmacopeial standards. Sourcing from reputable manufacturers with validated synthetic processes and thorough characterization is essential to ensure batch consistency and regulatory compliance.
Identification & chemistry
| Generic name | Calcifediol |
|---|---|
| Molecule type | Small molecule |
| CAS | 19356-17-3 |
| UNII | T0WXW8F54E |
| DrugBank ID | DB00146 |
Pharmacology
| Summary | Calcidiol is metabolized to calcitriol, the active form of vitamin D3, which binds to vitamin D receptors forming heterodimers with retinoid-X receptors to regulate gene transcription. This activity modulates calcium and phosphorus homeostasis by enhancing intestinal absorption, renal reabsorption, and bone resorption of these minerals. The pharmacological effects support mineralization of bone and maintenance of serum calcium levels, addressing conditions related to vitamin D deficiency and impaired mineral metabolism. |
|---|---|
| Mechanism of action | Calcidiol is transformed in the kidney by 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to calcitriol, the active form of vitamin D3. Calcitriol binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. Calcitriol increases the serum calcium concentrations by: increasing GI absorption of phosphorus and calcium, increasing osteoclastic resorption, and increasing distal renal tubular reabsorption of calcium. Calcitriol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein. |
| Pharmacodynamics | Calcidiol is the precursor of vitamin D3. Vitamin D3 is a steroid hormone that has long been known for its important role in regulating body levels of calcium and phosphorus, in mineralization of bone, and for the assimilation of vitamin A. The classical manifestations of vitamin D deficiency is rickets, which is seen in children and results in bony deformaties including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix, and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease, and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium and phosphorus mobilization from bone to plasma. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Vitamin D3 receptor | Humans | agonist |
ADME / PK
| Absorption | Readily absorbed. |
|---|---|
| Half-life | 288 hours |
| Metabolism | Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25- dihydroxycholecalciferol), the active form of vitamin D3. |
Formulation & handling
- Calcifediol is a small molecule secosteroid used in oral and intravenous formulations, including solutions and capsules.
- Due to its lipophilic nature (LogP 5.65) and low water solubility, formulations may require solubilization strategies for consistent bioavailability.
- Food intake, especially high-fat meals, significantly increases systemic exposure, which should be considered during formulation and clinical use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is in a mid-to-late stage of its lifecycle, with key patents expiring between 2020 and 2028 in the United States, and products marketed primarily in the US and Canada. Market maturity is increasing as patent protections near expiration. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Calcifediol is currently manufactured and packaged by a single originator company, Organon Pharmaceuticals, primarily serving the US and Canadian markets with branded products such as Rayaldee. The patent landscape indicates multiple patents protecting the product in the United States, with the earliest expired in 2020 and others extending protection until 2027 and 2028. This suggests the presence of existing generic competition for some indications, while additional patent protections may limit broader generic entry until later dates. |
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Safety
| Toxicity | Bone pain, constipation (especially in children or adolescents), diarrhea, drowsiness, dryness of mouth; headache (continuing), increased thirst, increase in frequency of urination, especially at night, or in amount of urine, irregular heartbeat, itching skin, loss of appetite, metallic taste, muscle pain, nausea or vomiting (especially in children or adolescents), unusual tiredness or weakness. |
|---|
- Handle with appropriate protective equipment to minimize exposure, as the compound may cause drowsiness, headache, and mucosal dryness upon contact or inhalation
- Monitor for signs of systemic toxicity such as bone pain, gastrointestinal disturbances, and muscle pain during manufacturing or formulation processes
- Avoid contamination and ensure proper ventilation to prevent respiratory or dermal irritation potentially leading to irregular heartbeat or skin itching
Calcifediol is a type of Vitamins
Vitamins are an essential subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a crucial role in maintaining optimal health and well-being. These organic compounds are required in small quantities by the human body to support various metabolic processes and ensure proper functioning of bodily systems. Vitamins can be broadly classified into two groups: fat-soluble vitamins (such as vitamins A, D, E, and K) and water-soluble vitamins (including vitamin C and B-complex vitamins). Each vitamin has a specific role and function within the body.
Pharmaceutical APIs in the vitamin subcategory are carefully synthesized or extracted to meet stringent quality standards and ensure purity, efficacy, and safety. They are used as active ingredients in the formulation of various pharmaceutical products, including dietary supplements, fortified foods, and pharmaceutical formulations.
Vitamin APIs are commonly utilized in the pharmaceutical industry for their therapeutic benefits. For instance, vitamin D API is widely prescribed to treat deficiencies and maintain optimal bone health, while vitamin C API is utilized for its antioxidant properties and immune-boosting effects. B-complex vitamins, such as vitamin B12 API, are essential for energy production and nerve function.
Overall, vitamins are integral to maintaining good health, and pharmaceutical APIs in this subcategory play a vital role in providing these essential nutrients to individuals through various pharmaceutical and dietary applications.
Calcifediol (Vitamins), classified under Therapeutic Nutrients/Minerals/Electrolyte
Therapeutic Nutrients/Minerals/Electrolytes: A Comprehensive Technical DescriptionTherapeutic nutrients, minerals, and electrolytes are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used to support and enhance overall health and well-being. These compounds play a crucial role in maintaining the body's physiological balance, aiding in various metabolic processes, and addressing specific deficiencies.
Therapeutic nutrients encompass a broad range of substances, including vitamins, minerals, and electrolytes. Vitamins are organic compounds required in small quantities for proper bodily functions and are essential for growth, development, and disease prevention. Minerals, on the other hand, are inorganic substances that support numerous physiological processes, such as bone formation, nerve function, and energy production.
Electrolytes are minerals that carry an electric charge when dissolved in bodily fluids, including sodium, potassium, calcium, magnesium, and chloride. They play a crucial role in maintaining proper hydration, nerve impulses, muscle contractions, and pH balance.
Pharmaceutical APIs in the Therapeutic Nutrients/Minerals/Electrolyte category are designed to address specific deficiencies or imbalances in the body. These APIs are often used in the formulation of dietary supplements, nutritional products, and therapeutic treatments. They are manufactured under stringent quality control guidelines to ensure purity, potency, and bioavailability.
Therapeutic nutrients/minerals/electrolytes APIs are available in various forms, including tablets, capsules, powders, and liquid formulations. They are formulated to meet specific dosage requirements and can be combined with other ingredients for targeted health benefits.
Overall, therapeutic nutrients, minerals, and electrolytes APIs are essential components in maintaining optimal health. Their use helps address deficiencies, support bodily functions, and promote overall well-being. Pharmaceutical companies and healthcare professionals rely on these high-quality APIs to develop effective and safe products that contribute to a healthier population.
Calcifediol API manufacturers & distributors
Compare qualified Calcifediol API suppliers worldwide. We currently have 3 companies offering Calcifediol API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| CARBOGEN AMCIS | Producer | Netherlands | Netherlands | BSE/TSE, CEP, CoA, FDA, GMP, ISO14001, ISO9001, MSDS, USDMF | 15 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
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