The main objective of biomass pretreatment is to separate biomass components and provide easier access with ultimate aim for lignin removal, hemicellulose protection and cellulose crystallinity reduction. Effective bioconversion with least inhibitory compound production would play a considerable role in economic practicability of the process in order to achieve economic sustainability. In this regard, detoxification is an important condition to make biomass hydrolysate acquiescent to bioconversion; also, understanding of inhibitors effect on growth and fermentation are necessary requirements for system detoxification. A number of physical, chemical and biological methods like feedstock selection, membrane selection, neutralization, use of activated charcoal etc have been recommended and developed for removal or minimizing the inhibitory compounds effect. This work reviews various inhibitory compounds produced during pretreatment methods and their removal by various processes.