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Method of Biocatalytic Synthesis of 25-hydroxy-vitamine D3 (calcifediol)
Jerzy Haber Institute of Catalysis and Surface Chemistry Poland flag Poland
Abstract ID:
Calcifediol in an activated form of vitamin D3 and it\'s a main blood circulating metabolite responsible for maintaining calcium and phosphate homeostasis. The method allows 100% selective enzymatic hydroxylation of vit. D3 (cholecalciferol) to calcifedio...
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Calcifediol as a drug

Calcifediol (25-OH-D3) is an activated form of vitamin D3, it is also an important hormone formed in skin tissue from 7-dehydrocholesterol under sunlight UV irradiation or can be introduced into the organism from dietary sources. 25-OH-D3 is a main blood circulating metabolite of vitamin D3 responsible for maintaining calcium and phosphate homeostasis. As a drug, it is also much more potent than vitamin D3, therefore it is used in treatment of rickets or other calcium disorders. Recently, its oral supplementation has been proposed to increase its plasma level, especially in patients unable to activate vitamin D3 due to decline of hepatic function. Such treatment is proposed for patients with e.g. D3 deficiency, liver or kidney disorders, organ transplantation, asymptomatic primary hyperparathyroidism and many others conditions.

Enzymatic hydroxylation

The invention delivers enzymatic preparation that is able to act as catalyst in direct hydroxylation of cholecalciferol to calcifediol, in other words its pharmacological activation. The enzyme can be deployed either as homogenous catalyst or as an immobilized enzyme (both in form of powder or porous monolithic cylinder). The reaction does not require any cofactors (such as NAD+ or FAD) beside cheap oxidants (e.g. K3[Fe(CN)6]). In proper reactor conditions the catalyst is active up to 30 days. Moreover, due to mild oxidation potential of the enzyme side products do not occur, i.e. the process is 100% selective toward Calcifediol and is 100% regioselective (only C25 carbon atom is hydroxylated). Estimated production costs of Calcifediol obtained with this method range in between 3-5 Euro per mg at a 1g scale.



Benefits:

1. Green technology operating mainly in aqueous medium at ambient conditions (room temperature)

2. Cheap reoxidation of the catalysts, possibility of employing electrochemical methods

3. Straightforward downstream processing due to an easy extraction procedure and 100% selectivity of the process

4. 100% regioselectivity of the process (no other products)

5. Custom formulation of the biocatalyst tailor made for the customer technological needs (homogenous, heterogenous in form of solid powder or supported on porous monolith)

6. Different modes of the process available (batch, fed-batch or continuous processes)

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Type of Business Relationship Sought
ICSC is looking for a business partner interested in further development of the method for production of the calcifediol and joint-patenting the method for European market. Furthermore, out-licensing and know-how transfer is envisaged as a strategy for implementation of the technology in pharmaceutical production.
FEATURED
Last Updated Jun 2016
Technology Type PLATFORM
Phase of Development CLINICAL TRIALS
PRIVATE INSTITUTE