Real-life safety of Emtricitabine/Tenofovir Alafenamide/Bictegravir

• Published in: PloS one 2023-08, Vol.18 (8), p.e0289132-e0289132
• Main Authors: Squillace, Nicola, Ricci, Elena, Maggi, Paolo, Taramasso, Lucia, Menzaghi, Barbara, De Socio, Giuseppe Vittorio, Piconi, Stefania, Maurizio Celesia, Benedetto, Orofino, Giancarlo, Sarchi, Eleonora, Pellicanò, Giovanni Francesco, Simeone, Filomena, Valsecchi, Laura, Bandera, Alessandra, Cenderello, Giovanni, Attala, Letizia, Angioni, Goffredo, Falasca, Katia, Cascio, Antonio, Bargiacchi, Olivia, Di Biagio, Antonio, Bonfanti, Paolo
• Format: Article
• Language: English
• Subjects: Adipocytes; Alanine; Alanine transaminase; Analysis; Antiretroviral agents; Antiretroviral drugs; Antiretroviral therapy; Antiviral agents; Biological products industry; Biology and Life Sciences; Blood; Blood lipids; Blood sugar; Care and treatment; Central nervous system; Cholesterol; Clinical trials; Complications and side effects; Drug therapy; Drug therapy, Combination; Drugs; Emtricitabine; Glucose; Health aspects; Hepatitis; Hepatitis B; High density lipoprotein; Highly active antiretroviral therapy; HIV; HIV (Viruses); HIV infection; Human immunodeficiency virus; Infection; Infectious diseases; Insomnia; Integrase; Lipids; Liver; Medical research; Medicine and Health Sciences; Medicine, Experimental; Metabolism; Patient outcomes; Pharmaceutical industry; Prescribing; Research and Analysis Methods; Safety; Safety and security measures; Sleep disorders; Switching; Tenofovir; Triglycerides; Variance analysis
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0289132

Integrase strand transfer inhibitors (INSTI) are one of the most prescribed drug classes for the treatment of HIV infection worldwide. Emtricitabine/Tenofovir Alafenamide/ Bictegravir (FTC/TAF/BIC) has been evaluated in randomized clinical trials; few studies have verified tolerability and safety in clinical practice. Our aim was to investigate the metabolic and hepatic safety in a real-life setting of FTC/TAF/BIC. Consecutive people living with HIV infection (PLWH) enrolled in the SCOLTA project, switching to or initiating their first antiretroviral treatment with FTC/TAF/BIC were included. PLWH with HBV co-infection were excluded. Metabolic and hepatic variables were collected at T0 and T1, were defined as baseline and 6-month follow-up respectively, and their modifications were analysed using the paired t-test and the analysis of variance. Five hundred and thirty-nine PLWH with at least one follow-up visit were included in the analysis. Mean age was 48 years (±12.1), 74% were male, 16.1% were naïve to antiretrovirals (ART). At T1, ART-experienced PLWH showed a significant reduction of total cholesterol (TC) and triglycerides, and a slight increase in blood glucose (BG) and ALT. On the contrary, in ART-naïve PLWH blood lipids significantly increased, although with an unaffected TC/high density lipoprotein (HDL)-c ratio, while alanine aminotransferase (ALT) decreased significantly, mainly in those with altered baseline level. The treatment interruptions were 45 (8.4%) over the whole observation period, 13 (2.4%) due to AEs. The most frequent AEs were related to the central nervous system (6 events of depression, insomnia, headache, agitation) and 3 PLWH discontinued the regimen because of grade 1-2 weight gain. In ART-experienced PLWH switching to FTC/TAF/BIC a significant improvement of lipid profile occurred but with significant BG and ALT variation without clinical relevance. In ART-naïve PLWH, blood lipids increased even though lipid profile did not worsen, and a trend towards normalization of liver enzymes was suggested. FTC/TAF/BIC is well tolerated in the real life setting.