Even though combinatorial chemistry has been an essential part of early drug discovery for more than two decades, so far only one de novo combinatorial chemistry-synthesized chemical has been approved for clinical use by FDA (sorafenib, a multikinase inhibitor indicated for advanced renal cancer).
Mada je kombinatorna hemija bila esencijalni deo ranih istraživanja lekova tokom perioda koji premašuje dve dekade, do sada je samo jedna de novo kombinatorno hemijski sintetisana hemikalija odobrena za kliničku upotrebu od strane FDA (sorafenib, multikinazni inhibitor koji se koristi u tretmanu napredne faze raka bubrega).