This article presents an integrated overview of Guanxin II (II) regarding its quality control, pharmacokinetics, pharmacology, clinical studies, adverse events, dosage and administration, and its pharmacoeconomic assessment. It has been demonstrated that Guanxin II has beneficial effects on coronary heart disease (CHD). The underlying mechanism was proved to be its anti-ischemic, anti-apoptotic, antioxidative, antiplatelet and anti-inflammatory effects, and so on. Tanshinol, hydroxysafflor yellow A and ferulic acid might be responsible for the cardioprotective effect of Guanxin II. In terms of acquisition cost, Guanxin II is cheaper than other drugs currently available for CHD. Guanxin II is safe, cheap, and effective in the management of CHD. However, the mechanism of its cardioprotective effects has not been completely understood because of limitations in the research methodologies of Chinese medicine. Further work should be carried out with single components such as tanshinol, hydroxysafflor yellow A and ferulic acid, using modern biochemical and molecular methods.