Lipid profile changings after switching from rilpivirine/tenofovir disoproxil fumarate/emtricitabine to rilpivirine/tenofovir alafenamide/emtricitabine: Different effects in patients with or without baseline hypercholesterolemia

Abstract

Tenofovir alafenamide (TAF) has similar efficacy compared to tenofovir disoproxil fumarate (TDF), but a less favorable effect on lipids. Aim of this retrospective multicentre study was to evaluate the impact on lipids of switching from rilpivirine (RPV)/ emtricitabine (FTC)/TDF to RPV/FTC/TAF in a cohort of HIV-1 infected patients. Total cholesterol (TC), high density lipoproteins (HDL) and low density lipoproteins (LDL) were compared at the moment of the switch and at the first following evaluation, by using paired t-test. Overall, 573 patients were considered, 99% with HIV-RNA <50 copies/ml, with mean age of 49.7 (±0.4) years and median 13.4 (6.9–22.5) years of HIV infection. In the study population with available data (431/573, 75%), mean TC changed from 173 ±1.7 to 188 ±1.8 mg/dl; mean HDL from 46 ±0.7 to 51± 0.7 mg/dl; mean LDL from 111 ±1.5 to 120 ±1.8 mg/dl (p<0.0001 for all). Neither LDL/HDL nor TC/HDL ratio changed significantly, with LDL/HDL from 2.6 ±0.5 to 2.5 ±0.5 (p = 0.12) and TC/HDL from 4.0 ±0.6 to 3.9 ±0.6 (p = 0.11). In patients with baseline diagnosis of hypercholesterolemia (TC>200 mg/dl, N = 87), there was no significant change in TC (224 ±2.2 to 228 ±3.4 mg/dl, p = 0.286) or LDL (150±2.5 to 151±3.2 mg/dl, p = 0.751), while HDL increased from 51 ±1.6 to 55 ±1.7 mg/dl (p<0.0001) and both LDL/HDL and TC/HDL ratio decreased significantly, from 3.2±0.1 to 3.0 ±0.1 (p = 0.025) and from 4.7±0.1 to 4.4 ±0.1 (p = 0.004). In this real life study, a slight increase in lipids was found after switching from RPV/FTC/TDF to RPV/FTC/TAF, but these results were not confirmed in people with hypercholesterolemia, in which lipids did not change and LDL/HDL and TC/HDL ratio decreased.

Changing Trends in Lipid Profile and Biomarkers of Renal Function and Bone Metabolism Before and After Switching From Tenofovir Disoproxil Fumarate to Tenofovir Alafenamide: a Prospective Observational Study

“…Previous studies have also shown the elevation in the LDL-C and TG levels, but the range of elevation depended on the observational period, and the characteristics of the participants (17)(18)(19). One of the major risks for hyperlipidemia that was identi ed after switching to TAF was the elevation at beginning in TG or LDL-C levels (20) although opposite results also reported (21). In our study, LDL-C levels increased regardless of the hyperlipidemia at baseline.…”

Injectable Antiretroviral Drugs: Back to the Future

“…RPV should be taken with a normal caloric meal (533 Kcal) or high-fat high-caloric meal (928 Kcal) and need careful evaluation of possible drug interactions, in particular with proton pump inhibitors and antiepileptic drugs. In a trial on healthy volunteers that were exposed to intravenous nanosuspension, maximum concentration was achieved in three days and decreased to below 10 ng/mL after 12–26 weeks with a half-life of five weeks [ 19 , 20 , 21 ].…”

An expert review on the use of tenofovir alafenamide for the treatment of chronic hepatitis B virus infection in Asia

“…While switch-over from TDF to TAF may be associated with an improvement in bone and renal safety in HBV-infected patients, changes in lipid profile have also been noted with TDF to TAF switch-over in people living with HIV. A significant increase in total and low-density lipoprotein cholesterol and decrease in high-density lipoprotein cholesterol has been noted with switch-over from TDF- to TAF-based regimen in HIV-infected individuals [ 72 – 74 ]. However, these results have not been confirmed in HIV-infected individuals with baseline hypercholesterolemia [ 72 ].…”

“…A significant increase in total and low-density lipoprotein cholesterol and decrease in high-density lipoprotein cholesterol has been noted with switch-over from TDF- to TAF-based regimen in HIV-infected individuals [ 72 – 74 ]. However, these results have not been confirmed in HIV-infected individuals with baseline hypercholesterolemia [ 72 ]. The clinical relevance of these findings, if any to HBV-infected individuals, remains to be established.…”