Besides prevention of caries and periodontitis, an increasing number of oral care products focus on teeth whitening. The aim of this review is to summarize and discuss frequently used whitening agents and their efficacy from a chemical viewpoint. Therefore, a comprehensive literature survey on teeth whitening agents and products was conducted. The current whitening methods are analyzed and discussed from a chemist’s viewpoint. Frequently used whitening agents are abrasives (mechanical removal of stains), antiredeposition agents (prevention of deposition of chromophores), colorants (intended to lead to a white color), proteases (degradation of proteins), peroxides (oxidation of organic chromophores), and surfactants (removal of hydrophobic compounds from tooth surface). In-office bleaching using peroxides is effective, but side effects like tooth sensitivity or a damage of the natural organic matrix of enamel and dentin may occur. The applicability of abrasives in teeth whitening is limited due to potential tooth wear, especially when toothpastes with high RDA values are used. The effect of other whitening agents in vivo is often unclear because of a shortage of placebo-controlled clinical trials.