Objective: To investigate the pharmacokinetics, safety/tolerability and antiviral activity of enfuvirtide administered once-daily (QD) versus twice-daily (BID).
Design: An open-label, randomized, multiple dose, two-period crossover study comparing 180 mg enfuvirtide, two injections QD versus 90 mg enfuvirtide, two injections, BID.
Methods: Steady-state intensive pharmacokinetic samples were obtained on days 7 and 14.
Results: Thirty-seven subjects received at least one dose of enfuvirtide. Thirty-three subjects completed both dosing periods. The regimens were bioequivalent based on the ratio of geometric mean area under the curve (AUC)0-tau [112 +/- 6.2 microg x h/ml QD; 115 +/- 6.4 microg x h/ml 2 x BID; QD/BID 0.98; 90% confidence interval (CI) 0.89,1.07]. The maximum observed plasma concentration within a dosing interval (Cmax) was 49% higher for QD (9.5 +/- 2.7 microg/ml) versus BID (6.3 +/- 1.7 microg/ml) and the pre-dose plasma concentration (Ctrough) was 57% lower for QD (1.6 +/- 1.1 microg/ml) versus BID (3.8 +/- 1.3 microg/ml). The LSM decrease in viral load from baseline to day 7 was 1.0 +/- 0.14 log10 (n = 18) for QD and 1.4 +/- 0.2 log10 (n = 17) for BID (LSM difference 0.385; P = 0.07). Linear regression analysis suggested that decline in viral load up to day 7 was associated with Ctrough but not Cmax or AUC. There were no significant differences in adverse events between the two dosing regimens.
Conclusions: Administration of enfuvirtide 180 mg QD results in bioequivalence compared with 90 mg BID based on AUC with a similar short-term safety profile, but a trend towards a weaker antiretroviral effect. Larger and longer-term studies are needed to determine if 180 mg once daily is an effective dosing alternative for enfuvirtide.
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http://dx.doi.org/10.1097/01.aids.0000200534.94608.7d | DOI Listing |
Indian J Clin Biochem
January 2025
Department of Orthopedics, All India Institute of Medical Sciences, Jodhpur, India.
Many studies showed Vitamin D deficiency is highly prevalent in healthy individuals. We planned to study the normal levels of Vitamin D in healthy individuals and make recommendation for defining deficiency of 25(OH)D in Indian population. ormal healthy subjects 18 to 60 years of age were included.
View Article and Find Full Text PDFPhysiol Res
March 2023
Faculty of Biotechnology and Food Sciences, Institute of Applied Biology, Slovak University of Agriculture in Nitra, Nitra, Slovak Republic.
The aim of the study was to examine the potential impacts of bisphenol A (BPA) and its analogues BPB, BPF, and BPS on mice TM3 Leydig cells, with respect to basal cell viability parameters such as metabolic activity, cell membrane integrity, and lysosomal activity after 48-h exposure. In addition, monitoring of potential bisphenol´s actions included evaluation of ROS production and gap junctional intercellular communication (GJIC) complemented by determination of testosterone secretion. Obtained results revealed significant inhibition in mitochondrial activity started at 10 microg/ml of bisphenols after 48-h exposure.
View Article and Find Full Text PDFPhysiol Res
November 2021
AgroBioTech Research Centre, Slovak University of Agriculture in Nitra, Nitra, Slovak Republic. Department of Animal Physiology, Faculty of Biotechnology and Food Sciences, Slovak University of Agriculture in Nitra, Nitra, Slovak Republic.
Beneficial effects of Sambucus nigra L. (black elder) as a traditional medicine have been associated with the phytoconstituents including polyphenols, terpenes and lectins. Various antioxidant rich natural products have also been implicated with improvement of reproductive health and fertility, however, the effect of Sambucus nigra on the ovarian cell functions has not been investigated yet.
View Article and Find Full Text PDFPhysiol Res
November 2021
Department of Animal Physiology, Faculty of Biotechnology and Food Sciences, Slovak University of Agriculture in Nitra, Nitra, Slovak Republic.
This study aimed to examine the effect of dietary flavonoid isoquercitrin on ovarian granulosa cells using the immortalized human cell line HGL5. Cell viability, survival, apoptosis, release of steroid hormones 17beta-estradiol and progesterone, and human transforming growth factor-beta2 (TGF-beta2) and TGF-beta2 receptor as well as intracellular reactive oxygen species (ROS) generation were investigated after isoquercitrin treatment at the concentration range of 5-100 microg.ml-1.
View Article and Find Full Text PDFAntibiotics (Basel)
March 2021
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia.
Marine natural products (MNPs) have been an important and rich source for antimicrobial drug discovery and an effective alternative to control drug resistant infections. Herein, we report bioassay guided fractionation of marine extracts from sponges , and that led us to identify novel compounds with antimicrobial properties. Tertiary amines or quaternary amine salts: aniline , benzylamine , tertiary amine and , and quaternary amine salt , along with three known compounds () were isolated from a crude extract and MeOH eluent marine extracts.
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