As we progress into the 21st century, cancer stands as one of the most dreaded diseases. With approximately one in every four individuals facing a lifetime risk of developing cancer, cancer remains one of the most serious health challenges worldwide. Its multifaceted nature makes it an arduous and tricky problem to diagnose and treat. Over the years, researchers have explored plenty of approaches and avenues to improve cancer management. One notable strategy includes the study of extracellular vesicles (EVs) as potential biomarkers and therapeutics. Among these EVs, exosomes have emerged as particularly promising candidates due to their unique characteristic properties and functions. They are small membrane-bound vesicles secreted by cells carrying a cargo of biomolecules such as proteins, nucleic acids, and lipids. These vesicles play crucial roles in intercellular communication, facilitating the transfer of biological information between cell-to-cell communication. Exosomes transport cargoes such as DNA, RNA, proteins, and lipids involved in cellular reprogramming and promoting cancer. In this review, we explore the molecular composition of exosomes, significance of exosomes chemistry in cancer development, and its theranostic application as well as exosomes research complications and solutions.