BackgroundAntiretrovirals, including tenofovir, can suppress human immunodeficiency virus (HIV) infection but cannot completely eradicate it. Patients with HIV infection are administered antiretroviral drugs over a long term; thus, managing consequent adverse drug reactions, such as renal dysfunction and bone mineral loss, is important. Currently, highly sensitive biomarkers that can detect adverse drug reactions early have not been well studied. MethodsThis single-center, prospective, observational study explored changes in the biomarkers of renal function, bone metabolism, and lipid profile before and after switching from tenofovir disoproxil fumarate (TDF) to tenofovir alafenamide (TAF) in patients with HIV infection. ResultsAll 31 enrolled patients had been treated with antiretrovirals for more than 5 years. The urinary liver-type fatty acid binding protein (L-FABP)/creatinine ratio was significantly decreased at 3 and 6 months after switching to TAF compared with that before switching to TAF (-0.5μg/g・Cr at 3 months, and -0.8μg/g・Cr at 6 months; p <005 for both at 3 and 6 months) . The urinary N-terminal telopeptide (NTx)/creatinine ratio decreased over the study period, and the ratios were significantly different between 3 months and 6 months (-11 nmol/mmol Cr at 3 months, -15.2 nmol/mmol Cr at 6 months; p =0.0069 at 3 months, p<.0001 at 6 months) . Low density lipoprotein-cholesterol level significantly increased at 3 (+26 mg/dL) and 6 months (+13 mg/dL) compared with that at the baseline (p < 0.0001).ConclusionsSwitching from TDF to TAF decreased the levels of renal and bone biomarkers, such as urinary L-FABP and NTx, but increased low density lipoprotein-cholesterol levels. Highly sensitive markers, such as urinary L-FABP and NTx, might be useful tools to predict adverse drug reaction early.