Supramolecular medicinal chemistry field has been a quite rapidly developing,increasingly active and newly rising interdiscipline which is the new expansion of supramolecular chemistry in pharmaceu-tical sciences,and is gradually becoming a relatively independent scientific area. Supramolecular drugs could be defined as medicinal supermolecules formed by two or more molecules through non-covalent bonds. So far a lot of supermolecules as chemical drugs have been widely used in clinics. Supermolecules as chemical drugs,i.e. supramolecular chemical drugs or supramolecular drugs,which might have the excellences of lower cost,shorter period,higher potential as clinical drugs for their successful research and development,may possess higher bioavailability,better biocompatibility and drug-targeting,fewer multidrug-resistances,lower toxicity,less adverse effect,and better curative effects as well as safety,and therefore exhibit wide potential application. These overwhelming advan-tages have drawn enormous special attention. This paper gives the definition of supramolecular drugs,proposes the concept of supramolecular chemical drugs,and systematically reviews the recent ad-vances in the research and development of supermolecules,including organic and inorganic complex ones as chemical drugs in the area of antitumor,anti-inflammatory,analgesic,antimalarial,antibacterial,antifungal,antivirus,anti-epileptic,cardiovascular agents and magnetic resonance imaging agents and so on. The perspectives of the foreseeable future and potential application of supramolecules as chemical drugs are also presented. Supramolecular medicinal chemistry has has a quite rapid developing, increasingly active and newly rising interdiscipline which is the new expansion of supramolecular chemistry in pharmaceu-tical sciences, and is gradually becoming a relatively independent scientific area. Supramolecular drugs could be defined as medicinal supermolecules formed So far a lot of supermolecules as chemical drugs have been widely used in clinics. Supermolecules as chemical drugs, ie supramolecular chemical drugs or supramolecular drugs, which might have the excellences of lower cost, shorter period, higher potential as clinical drugs for their successful research and development, may possess higher bioavailability, better biocompatibility and drug-targeting, fewer multidrug-resistances, lower toxicity, less adverse effect, and better curative effects as well as safety, and due exhibit wide potential application. These overwhelming advan-tages have dr This paper gives the definition of supramolecular drugs, Vihe the concept of supramolecular chemical drugs, and systematically reviews the recent ad-vances in the research and development of supermolecules, including organic and inorganic complex ones as chemical drugs in the area of antitumor, anti-inflammatory, analgesic, antimalarial, antibacterial, antifungal, antivirus, anti-epileptic, cardiovascular agents and magnetic resonance imaging agents and so on. The perspectives of the foreseeable future and potential application of supramolecules as chemical drugs are also presented.