Cholesterol gallbladder stones can be dissolved with chenodeoxycholic acid (CDCA) or ursodeoxycholic acid (UDCA). Response rate is 60-90%, dissolution rate 60% in stones not exceeding 1.5 cm in diameter. Mean treatment time amounts to 18 months. To improve oral litholysis: 1) UDCA was combined with the amino acid taurine, 2) CDCA and UDCA were administered in a single bedtime dose, 3) they were combined, each bile acid in half dosage, and 4) they were mixed with terpenes. Although there was some improvement with the combination therapy, final outcome is still suboptimal. Many investigations have been performed concerning gallbladder function, mucus production and nucleating factors, showing both that cholesterol supersaturation of bile is the conditio sine qua non for gallstone formation and that other factors play an additional, important role for the development of the first nidus. These factors have to be considered when therapy shall be improved. As yet oral litholysis has shown neither drug-related side effects nor lethality. It is not more expensive than surgery. Direct contact litholysis with methyl tert-butyl ether could reduce the indication for oral treatment to floating stones or patients who refuse gallbladder puncture. But although oral litholysis does not provide us with optimal results and needs further improvements, it will always keep its place in gallstone therapy.