Chirality is an important concept in pharmaceutical chemistry for drug development; it influences the pharmacokinetics, pharmacodynamics, and efficacy of drugs. Chirality changes the shape of drug molecules and the stereochemistry of molecules because of the presence of their chiral centres, which determine any molecule’s interactions with biological systems, and this interaction results in significant differences in therapeutic outcomes of different enantiomers of a single drug molecule. Chirality also has an impact on drug delivery systems and drug design; we discussed the role and importance of chirality enhancing drug efficacy, safety, and targeted delivery. Advancements in nanotechnology and stereochemical organic synthesis have further enhanced targeted therapies by refining drug design and development processes.