A review is given of the background to and results of the succesful pharmacological testing of [AuX2(damp)] (X = Cl, OAc; damp = 2 − Me2NCH2C6H4) against a range of microbes, fungi and tumouts, culminating in in vivo xenografts of ZR‐1‐75. These are the first fully evaluated gold(III) complexes. The activity and reactions of the diacetato‐complex bear a resemblance to cisplatin, and some of the relevant chemistry is discussed. Preliminary screening data for C,P‐chelated tertiary phosphine derivatives of gold(III) are presented.