Cyclophilin A(CypA) is a member of cyclophilins,a family of the highly homologous peptidyl prolyl cis-trans isomerases(PPIases),which can bind to cyclosporin A(CsA).CypA plays critical roles in various biological processes,including protein folding,assembly,transportation,regulation of neuron growth and HIV replication.In the article,the whole development of natural product leads,peptide analogue inhibitors and organic synthesized compounds of CypA inhibitors was summarized and the research progress of CypA was reviewed.