The concerns about the safety of human health are always the priority in any field of applications associated directly with the humans. Introducing new compounds to the world is a challenging task, requiring extensive research and rigorous testing to ensure their effectiveness and safety. This chapter has given all the necessary details to familiarize the reader with the regulatory status and clinical trials of chitosan and derivatives. Prior to the commercialization of chitosan-containing medicinal goods for human medical uses, a thorough safety examination of the chitosan material was required as practiced for any other compound. The creation of novel biomedical goods entails a number of factors, including biopolymer characteristics, manufacturing quality and quantity, and therapeutic impacts. The use of chitosan in human studies requires approval from national and international regulatory bodies, such as the FDA in the USA. Characterization and functionality, product specifications, and analysis using validated methods have all been important regulatory issues in the commercialization of chitosan for biomedical uses. Any chitosan products under consideration for premarketing approval or other uses should be thoroughly examined for biocompatibility. Chitosan can be used as an excipient or as a vehicle for delivering potential drugs and biologics like gene products. Chitosan has been studied as a potential drug for neuronal disorders, blood pressure control, and body weight loss. In addition, a number of animal studies and clinical trials of 166Ho-chitosan for various cancers are examined. Based on the literature review, it has been deduced that for the treatment of malignancies, several techniques of administering 166Ho-chitosan might be utilized.