Once-daily treatment with saquinavir mesylate (2000 mg) and ritonavir (100 mg) together with a fixed-dose combination of abacavir/lamivudine (600/300 mg) or tenofovir/emtricitabine (245/200 mg) in HIV-1-infected patients

ABSTRACTA complete 2-drug regimen of dolutegravir at 50 mg and rilpivirine at 25 mg was approved to treat HIV-1 infection in virologically suppressed patients after demonstrating acceptable efficacy and tolerability. This study investigated the bioequivalence and pharmacokinetics of the fixed-dose combination tablet compared with those of separate tablets. Secondary endpoints were the tolerability and safety of the fixed-dose combination tablet. In this open-label, randomized-sequence, 2-way crossover trial, single doses of the fixed-dose combination tablet (the test treatment) and the combination of separate tablets (the reference treatment) were administered to healthy adults after a moderate-fat meal, with a 21-day washout between treatments. Pharmacokinetic samples were collected through 12 days after dosing. The primary endpoints were the area under the plasma concentration-time curve (AUC) and the maximum concentration of drug in plasma (Cmax). The study employed a prespecified sample size reestimation based on a blind midpoint review ofCmaxvariability to update the enrollment size to achieve statistical power. Of 118 participants enrolled, 113 received both treatments and underwent pharmacokinetic assessment. The 90% confidence intervals for the geometric least-squares mean ratios for the AUC from 0 h to infinity, the AUC from 0 h to the last quantifiable measurement, andCmax(test treatment versus reference treatment) were within the bioequivalence range of 0.80 to 1.25 for both drugs, indicating bioequivalence. In this study, a single dose of either treatment was well tolerated overall, with 4% (n= 5) and 3% (n= 3) of participants reporting adverse events considered related to the test and reference treatments, respectively. The dolutegravir-rilpivirine fixed-dose combination tablet is bioequivalent to a combination of separate tablets, and no new safety signals emerged. (This study has been registered at ClinicalTrials.gov under identifier NCT02741557.)

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Different daily glycemic profiles after switching from once-daily alogliptin plus twice-daily metformin to their once-daily fixed-dose combination in Japanese type 2 diabetic patients

Endocrine Journal ◽

10.1507/endocrj.ej18-0313 ◽

2019 ◽

Vol 66 (1) ◽

pp. 11-17

Author(s):

Mitsuyoshi Takahara ◽

Toshihiko Shiraiwa ◽

Naoto Katakami ◽

Yoshifumi Maeno ◽

Kaoru Yamamoto ◽

...

Keyword(s):

Fixed Dose Combination ◽

Fixed Dose ◽

Diabetic Patients ◽

Type 2 Diabetic Patients ◽

Once Daily ◽

Dose Combination ◽

Type 2 Diabetic

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Combination Therapy with Tenofovir Disoproxil Fumarate/Emtricitabine/Elvitegravir/Cobicistat Plus Darunavir Once Daily in Antiretroviral-Naive and Treatment-Experienced Patients: A Retrospective Review

Journal of the International Association of Providers of AIDS Care (JIAPAC) ◽

10.1177/2325957417752260 ◽

2018 ◽

Vol 17 ◽

pp. 232595741775226 ◽

Cited By ~ 3

Author(s):

Mark J. Naccarato ◽

Deborah M. Yoong ◽

Ignatius W. Fong ◽

Kevin A. Gough ◽

Marian A. Ostrowski ◽

...

Keyword(s):

Reverse Transcriptase ◽

Tenofovir Disoproxil Fumarate ◽

Retrospective Chart Review ◽

Transcriptase Inhibitor ◽

Primary Objective ◽

Fixed Dose ◽

Drug Resistant ◽

Once Daily ◽

Dose Combination ◽

Hiv 1

Background: Patients with drug-resistant HIV often require complex antiretroviral regimens. However, combining fixed-dose combination tablets such as tenofovir–disoproxil–fumarate, emtricitabine, and cobicistat-boosted elvitegravir (TDF/FTC/EVG/cobi) with darunavir (DRV) can provide a simple, once-daily (QD), 2-tablet regimen for patients with drug-resistant HIV. Primary objective was to determine the percentage of patients with HIV-1 RNA <40 copies/mL at 48 weeks. Methods: We performed a retrospective chart review of patients initiated on TDF/FTC/EVG/cobi plus DRV. Results: Among the 21 included patients, prior resistance showed a median of 2 nucleoside reverse transcriptase inhibitor mutations, 1 nonnucleoside reverse transcriptase mutation, and 1 protease inhibitor mutation. At week 48, 14 (67%) patients achieved HIV-1 RNA <40 copies/mL, 1 patient experienced viral rebound, and 6 (29%) had missing data or discontinued therapy. No patient discontinued for adverse events. Conclusion: According to this observational study, QD TDF/FTC/EVG/cobi plus DRV is considered safe, well tolerated, and generally effective in suppressing HIV drug-resistant virus.

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