Use of cyclodextrins in diseases and disorders involving phospholipid dysregulation

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A patent application by Knut M. Wittkowski (ASDERA LLC, US) entitled “Use of cyclodextrins in diseases and disorders involving phospholipid dysregulation” (WO 2019/067145 and WO 2019/067269) has recently been published by the EPO. The invention features methods for sequestering phospholipids (PLs) from circulation with a composition comprising alpha-cyclodextrins (aCDs) and a fatty acids. Current cyclodextrin (CD) drugs are based on beta-CDs, which carry the risk of cholesterol-related ototoxicity and need to be administered by overnight intravenous infusion. The genetic data reanalyzed by the inventor suggests reduction of phospholipids (PLs), rather than cholesterol, as the bCDs’ mode of action and, thus, use of the smaller aCDs, which are too small to fit cholesterol and to cause permanent hearing loss. As shown in the clinical studies conduced, aCDs are absorbed from the intestine when formulated as a clathrate with capric acid (C10) and, thus, can be administered orally. After absorption into the blood stream, aCDs sequester phospholipids (PLs) and are excreted into urine with the PLs. The inventor postulates that lowering PL levels reduces not only systemic inflammation, but also endocytosis (the uptake of substrates by cells) to levels seen with intermittent fasting. This synergy slows down (1) growth and metastasis of tumors, (2) accumulation of LDL in macrophages (atherosclerosis) and hepatocytes (diabetes), (3) interference of lysosomes with autophagy (cellular housekeeping clearing plaques and tangles) in neurodegenerative and lysosomal storage diseases, and (4) the ability of viruses to “hijack” endocytosis for their replication.

According to WHO data, cancer causes 10 million deaths per year, 55 million people worldwide live with dementia, and 500 million with diabetes. As the world’s population over 50 will nearly double over the next 30 years, the prevalence of age-related diseases is increasing [1]. More save and effective interventions to prevent and treat age-related diseases are urgently needed.


Featured picture credit: wikipedia

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