Simvastatin is an inhibitor of HMG-CoA reductase that exhibits anti-hyperlipidemic, anticonvulsant/antiepileptic, anti-osteoporotic, neuroprotective, cognition enhancing, antithrombotic, and anticancer chemotherapeutic activities. Clinically, simvastatin decreases levels of LDL and total cholesterol and lowers cardiovascular morbidity and mortality rates. Simvastatin decreases insulin synthesis and secretion in vitro, potentially through increasing ATP-sensitive K+ currents and inhibiting L-type Ca2+ currents. In animal models of Parkinson’s disease, simvastatin upregulates expression of M1/4 muscarinic acetylcholine receptors (mAChRs), improving long-term memory. In other animal models, simvastatin increases bone mineral density, bone volume fraction, and bone microarchitecture. Additionally, simvastatin decreases platelet activation and inhibits thrombus formation in vitro and in vivo. This compound also increases expression of p27 and decreases expression of histone methyltransferase EZH2, inhibiting cellular proliferation and tumor growth in preclinical cancer models and increasing survival rates in clinical settings.
Note: This is the inactive form of the statin. To activate, add one equivalent of sodium hydroxide to convert it to the sodium form.