Calcitriol

Calcitriol is a form of Vitamin D3 with three alcohol groups. It increases gastrointestinal calcium absorption, stimulates osteoclastic calcium resorption from bone, facilitates the effect parathyroid hormone (PTH) has on bone resorption, and increases renal tubular absorption of calcium. Production of calcitriol by the cells of the proximal tubule of the nephron in the kidney is stimulated by hypocalcemia and hypophosphatemia as well as parathyroid hormone.

Synonyms

1a,25-Dihydroxyvitamin D3
1a,25-Dihydroxycholecalciferol
(1a,3ß,5Z,7E)-9,10-Seco-cholesta-5,7,10(19)-triene-1,3,25-triol

Background and use

Vitamin D3 is a prohormone produced in skin through ultraviolet irradiation of 7-dehydrocholesterol. It is biologically inert and must be metabolised to 25-hydroxyvitamin D3 in the liver and then to 1,25-dihydroxyvitamin D3 (Calcitriol) in the kidney in order to exert its function. The hormonal form of vitamin D3, i.e. Calcitriol, acts through a nuclear receptor to carry out its many functions: calcium absorptions, phosphate absorption in the intestine, calcium mobilisation in bone and calcium re-absorption in the kidney. Therefore classical pharmacological uses of Calcitriol include: treatment of calcium malabsorption, ricket, osteoporosis, renal osteodistrophy and osteomalacia.

One important finding during the 90s was the discovery that Vitamin D metabolites and Calcitriol exert other functions in the body beside the classical calcium mobilising activity, i.e. they show cell differentiating and immunomodulating activity. Therefore it is possible to use  Calcitriol for treating hyperparatyroidism, psoriasis, some autoimmune diseases and certain types of cancer. However because of the danger of hypercalcemia, the dosage has to be strictly controlled.

Regulatory compliance

Cerbios-Pharma’s calcitriol complies to the European and the US Pharmacopoeia. EDMF and US-DMF are available, active and updated. An application for the Certificate of Suitability of the European Pharmacopoeia at the European Directorate for the Quality of Medicines (EDQM) was filed recently.

Intellectual property

A process for the production of Calcitriol is patent protected (EP 735 510; US 5 698 714; AU 676 982; IL 118 837)

Packaging information

The API is packed in 2mL, 20mL, 50mL or 100mL brown, type 1 glass bottles with rubber closure and aluminium crimp cap.

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