The attentiveness towards phytochemicals, which represents the group of biologically active compounds derived from plants, also referred to as phytocomponents, and has sprung up due to their therapeutics implications. This review article encourages researchers to appreciate the most recent innovations in analytical approaches to the determination and measurement of phytochemicals, methods such as spectroscopy, chromatography and mass spectrometry are some of the techniques examined here. Moreover, it covers the bioactivity and mechanisms of action of phytochemicals, the effect of which is their being directing to molecular targets and leading to a modulation of cellular signaling network. The way that the plant-derived compounds are absorbed, distributed, metabolized and excreted (pharmacokinetics) and the way that they act on the body (pharmacodynamics) are examined in details and they are found to be efficient for treating many diseases. Drug discovery and development also include a range of interdisciplinary fields such as chemistry, pharmacology, and other disciplines. In these areas, research includes also industry considerations and ethical practices. This overview covers the range of achievements based on phytochemical research in the current stage and the expectations on its prospective influence on health care. Keywords: Phytochemicals, Analytical Techniques, Bioactivity, Pharmacokinetics and Pharmacodynamics