Cardiovascular and cerebral arterial disease has become the number 1 killer of human being. The main pathology is atherosclerotic plaque, characterised by the build-up of cholesterol in the inner lining of the arteries, which blocks blood flow. 2-hydroxypropylβ-cyclodextrin (HPβCD) has been shown to encapsulate cholesterol to cause a regression of plaques in animals. However, there was no research on its effects in human subjects. This study is unique in that it was designed and performed by the first author (KH). He had severe coronary arterial atherosclerosis treated with classical statins and multiple stents but had been declared as having a life expectancy of 0.5-2.5 years in 2019. HPβCD was infused intravenously at different doses for a period of 36 days. Several significant results have been discovered. Firstly, the treatment led to a significant reduction of plaques in the right coronary artery revealed by coronary angiography before and after the treatment regimen. Secondly, the treatment reduced the level of cholesterol and triglyceride in the blood. Thirdly, the elevated urine albumin and albumin/creatinine ratio prior to the treatment was reduced to normal level. Lastly, no significant adverse effects were observed in liver function and hearing. This is the first clinical trial to show the efficacy of HPβCD in removing atherosclerotic plaques from coronary arteries.