Plant-derived medicines constitute a significant component of today’s human healthcare systems in industrialized as well as developing countries. Plants are capable of synthesizing a huge variety of small organic molecules, called secondary metabolites, usually composed of very complex and unique carbon skeleton structures. The abundance and diversity of secondary metabolites are coupled with wide pharmaceutical, therapeutic and medicinal values. Most of the plant derived biomedicines are widely used for recreation and stimulation (the alkaloids nicotine and cocaine; the terpene cannabinol) purposes. Considerable progress has been made in the technology of large-scale plant cell culture for the industrial production of plant-derived fine chemicals. Keeping in view of the huge world market for plant secondary metabolites, it is a challenge for biotechnologists to find techniques to produce these compounds in sufficient quantity and quality. Biotechnological intervention through micropropagation, biotransformation, and metabolic engineering can make the process quite profitable to exploit the productive potential of living cells for the production of bioactive compounds. Therefore, the increasing global demand for biomedicines can only be achieved by application of biotechnological approaches.