This review is briefly to recall the history of research and development (R&D) of Chinese materia medica (CMM) and to discuss the challenges of Chinese traditional and herbal medicines (CTHM) facing the modern science and technology. The R&D of CTHM is thought to be an important pathway for new drug discovery. Since1949, about 140 approved new drugs have been developed, among which about 80 originated directly or indirectly from medicinal plants. CTHM has gained interest from the international medical, biomedical, and pharmaceutical institutions as a valuable source of potential medicines. For the modernization of CMM and innovative research of CTHM, there are following challenges to be faced: (1) to evaluate the efficacy, pharmacological properties, action mechanism, and active chemical constituents; (2) to develop new methodologies for the quality and safety of CTHM; (3) to apply new “-omics” techniques to accelerate drug discoveries developed from CTHM; and (4) to apply international practices including good agricultural practice, good manufacturing practice, good laboratory practice, and good clinical practice in the R&D of CTHM. This review is briefly recalling the history of research and development (R & D) of Chinese materia medica (CMM) and to discuss the challenges of Chinese traditional and herbal medicines (CTHM) facing the modern science and technology. The R & D of CTHM is thought to be an important pathway for new drug discovery. Since 1949, about 140 approved new drugs have been developed, among which about 80 originated directly or indirectly from medicinal plants. CTHM has gained interest from the international medical, biomedical, and pharmaceutical institutions as a valuable source For potential modernization of CMM and innovative research of CTHM, there are following challenges to be faced: (1) to evaluate the efficacy, pharmacological properties, action mechanism, and active chemical constituents; (2) to develop new methodologies for the quality and safety of CTHM; (3) to apply new “- omics ” techniques to accelerate drug discoveries developed from CTHM; and (4) to apply internatio nal practices including good agricultural practice, good manufacturing practice, good laboratory practice, and good clinical practice in the R & D of CTHM.