Provided herein are methods for reducing levels of blood cholesterol, low-density lipoprotein (LDL), and/or the treatment of diseases associated with high cholesterol, hyperlipidemia, dyslipidemia, or high levels of low-density lipoprotein (LDL), wherein the methods comprise administering a DRP1 inhibitor to a subject in need thereof. In certain embodiments, the subject is selected for treatment as described herein when the subject exhibits intolerance to conventional statin therapy. Also contemplated herein are the use of DRP1 inhibitors in the treatment of cancer and inflammatory disease.