SCIENCE

Cyclodextrin

Cyclodextrin is a ring-structured molecule, composed of five to seven glucoses linked together in a cyclic shape. The cavity of the ring structure exhibits hydrophobicity, whereas the surface exhibits hydrophilicity. Such a ring structure allows it to host hydrophobic molecules such as cholesterol inside the cavity and solubilize them.

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Cyclodextrin regulates cholesterol homeostasis

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Increased cholesterol influx or decreased cholesterol efflux can induce accumulation of excessive cholesterol within cells, which hampers proper cellular functions and leads to various cholesterol-associated diseases. Cyclodextrin helps maintenance of cholesterol homeostasis by promoting cholesterol metabolism pathways. 

Cyclodextrin functions in various organs

The ability of cyclodextrins to regulate cholesterol homeostasis has shown to help treat cholesterol-associated diseases in various organs throughout our body including brain, heart, aorta, kidney, and others.

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Cyclodextrin in clinical trials

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Hydroxypropyl-beta-cyclodextrin (HPβCD) is a derivative of beta-cyclodextrin. HPβCD is more soluble and less cytotoxic than natural beta-cyclodextrin. HPβCD is being investigated in clinical trials for diseases including Niemann-Pick type C, Alzheimer's disease, and focal segmental glomerulosclerosis.

Ototoxicity

Despite the promising effects of cyclodextrin on regulating cholesterol homeostasis, ototoxicity can occur following peripheral or central nervous system-directed delivery of HPβCD. It has been experimentally shown in various animal species that both routes can result in the preferential loss of outer hair cells (OHCs) in the cochlea. Ototoxicity caused by loss of OHCs can cause permanent hearing loss, which should be managed with hearing aids.

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Next-generation cyclodextrin 

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RENATUS is dedicated to creating a next-generation cyclodextrin to bring new, safe medicines for patients with cholesterol-associated diseases. With its independent technology, RENATUS has generated a potent cyclodextrin with superb safety and efficacy.