Glucosyl-attached Ospemifene

Korea University Background
The existing ospemifene requires a high recommended daily dose:
The existing ospemifene is a hydrophobic compound that provides excellent tolerability, but there are problems with low solubility and remarkably low bioavailability. Due to this, the recommended daily dose of ospemifene is provided with 60mg or more.
Technology Overview
Providing new compounds or pharmaceutically acceptable salts:

New compounds are provided by introducing glycosyltransferase to ospemifene ().
Glycosyltransferase has a sequence of amino acids marked with sequence number 1 (5’- GGCATATGATCCACGCGCACGACTTCCGGATG-3’).
Conversion into glycosyl-attached ospemifene derivative by chain enzyme reaction of MrGT2:
Separation(MrGT2) of GT-encoding gene from micromonospora rhodorangea gene.
Obtaining glycosyl-attached ospemifene derivative by sequential enzyme reaction of human-derived recombinant CYP and MrGT2.

Comparison of bioavailability with existing ospemifene:

Control group: ospemifene (OSPEM)(2.1 ng/ml)
Glycosyl-attached derivative (4-OSPEM-G: 8.4 ng/ml, 4-OSPEM- DG: 9.3 ng/ml)
It is confirmed that the blood concentration of 4-OH-OSPEM is more than four times compared with control group ().
The persistence of medicinal effect is presented while low bioavailability of existing ospemifene is improved.

New ospemifene derivative compound with improved bioavailability:
The blood concentration of 4-OH-OSPEM has been improved over four times than that of the existing ospemifene.
Potential for use as drugs with improved persistence of medicinal effect:
It implies that the new ospemifene derivative may remain for a relatively long period of time in a blood circulatory system through processes of absorption, distribution, metabolism and excretion after oral inoculation.
It can be used as medicines and functional foods for a treatment of diseases of menopausal women.
The global women’s health-related market reached$36.5 billion in 2016 and an annual average growth rate of 3.9% is expected.
– Built in laboratory environment.

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