This review provides a brief assessment of the methodological field of trifluoromethylation and its possible impact on the development of new CF3-containing pharmaceuticals. Structural aspects of five new drug-candidates, [tafenoquine (aromatic CF3), roniciclib (heteroaromatic CF3), BAY-38-7271 (aliphatic CF3), sonidegib (OCF3) and navitoclax (S-CF3)] currently under the development in phase II and III clinical studies, and their biological properties, therapeutic area and synthesis are critically discussed.

Recent advances in the trifluoromethylation methodology and new CF3-containing drugs