Bilirubin is the yellow breakdown product of normal heme catabolism. Heme is found in haemoglobin, a principle component of red blood cells. In this book, the authors present a brief review of what has already been done in the field of bilirubin research and provide some new insights into the future of the molecular simulation of bilirubin transport and studies of its chemistry. Topic discussed include biophysical and technical aspects of phototherapy for neonatal hyperbilirubinemia; genetic variants in bilirubin metabolism pathway, serum bilirubin and cardiovascular disease; molecular simulation of bilirubin transport and its pKa values and drug-induced cholestatic liver injury.