Pharmacokinetics of Emtricitabine, Tenofovir, and GS-9137 Following Coadministration of Emtricitabine/Tenofovir Disoproxil Fumarate and Ritonavir-Boosted GS-9137

@article{Ramanathan2007PharmacokineticsOE,
  title={Pharmacokinetics of Emtricitabine, Tenofovir, and GS-9137 Following Coadministration of Emtricitabine/Tenofovir Disoproxil Fumarate and Ritonavir-Boosted GS-9137},
  author={Srini Ramanathan and Gong Shen and Andrew K. Cheng and Brian P. Kearney},
  journal={JAIDS Journal of Acquired Immune Deficiency Syndromes},
  year={2007},
  volume={45},
  pages={274-279}
}
Objectives:To evaluate the potential for clinically relevant drug-drug interaction between emtricitabine/tenofovir disoproxil fumarate (FTC/TDF) and the ritonavir-boosted HIV integrase inhibitor GS-9137 (GS-9137/r). Methods:Healthy adults were administered FTC/TDF (200/300 mg once daily) for 7 days, followed by randomization to the order of receiving GS-9137/r (50/100 mg once daily) and GS-9137/r plus FTC/TDF in a crossover fashion under fed conditions for 10 days. Pharmacokinetic (PK) blood… Expand
Concomitant administration of BILR 355/r with emtricitabine/tenofovir disoproxil fumarate increases exposure to emtricitabine and tenofovir: a randomized, open-label, prospective study.
TLDR
There was no evidence of increased risk of TFV or FTC toxicity upon co-administration of FTC/TDF with BILR 355/r and the pharmacokinetic interaction of ritonavir-boosted B ILR 355 was well tolerated. Expand
Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial
TLDR
If regulatory approval is given, EVG/COBI/FTC/TDF would be the first integrase-inhibitor-based regimen given once daily and the only one formulated as a single tablet for initial HIV treatment. Expand
Pharmacokinetics of Coadministered Ritonavir-Boosted Elvitegravir and Zidovudine, Didanosine, Stavudine, or Abacavir
TLDR
There are no clinically relevant drug interactions between EVG/r and the NRTIs zidovudine, didanosine, stavUDine, or abacavir and these agents can be coadministered without dose adjustment. Expand
Steady-State Amprenavir, Tenofovir, and Emtricitabine Pharmacokinetics Before and After Reducing Ritonavir Boosting of a Fosamprenavir/Tenofovir/Emtricitabine Regimen from 200 mg to 100 mg Once Daily (TELEX II)
TLDR
Reducing RTV boosting from 200 to 100 mg QD of FPV/TDF/FTC QD conferred no detrimental effect on APV, tenofovir, FTC, or RTV pharmacokinetics and maintained virologic suppression. Expand
Model Linking Plasma and Intracellular Tenofovir/Emtricitabine with Deoxynucleoside Triphosphates
TLDR
Model simulations of analog:dNTP molar ratios using IPERGAY dosing suggested that FTC significantly contributes to the protective effect of preexposure prophylaxis (PrEP). Expand
Pharmacokinetics and Bioavailability of an Integrase and Novel Pharmacoenhancer-Containing Single-Tablet Fixed-Dose Combination Regimen for the Treatment of HIV
TLDR
Fixed-dose combination tablet containing COBI 150 mg resulted in desired high EVG Ctau concentrations and clinically equivalent tenofovir and FTC exposures relative to currently approved individual agents and was thus selected for subsequent evaluation. Expand
Very High Concentrations of Active Intracellular Phosphorylated Emtricitabine in Neonates (ANRS 12109 Trial, Step 2)
TLDR
The exposure to the active form of FTC was high in neonates despite plasma drug concentrations equivalent to those in adults, and high FTC-TP concentrations were observed in the four children who had serious adverse events (SAEs). Expand
Pharmacokinetics and Safety of Single-Dose Tenofovir Disoproxil Fumarate and Emtricitabine in HIV-1-Infected Pregnant Women and Their Infants
TLDR
Rapidly decreasing TFV levels in infants suggest that multiple or higher doses of TDF will be necessary to maintain concentrations that are effective for viral suppression in HIV-infected pregnant women and their infants. Expand
Plasma and Intracellular Tenofovir Pharmacokinetics in the Neonate (ANRS 12109 Trial, Step 2)
TLDR
Tenofovir (TFV) pharmacokinetics in plasma and peripheral blood mononuclear cells (PBMCs) of the neonate of HIV-1-infected pregnant women was investigated for the first time, suggesting a lag in appearance of TFV-DP. Expand
Lack of Interaction Between the HIV Integrase Inhibitor S/GSK1349572 and Tenofovir in Healthy Subjects
TLDR
Pharmacokinetic parameters of S/GSK1349572 and tenofovir during combination therapy were similar to those when given alone, demonstrating no significant drug interaction. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 28 REFERENCES
Pharmacokinetics and Safety of Tenofovir Disoproxil Fumarate on Coadministration With Lopinavir/Ritonavir
TLDR
Coadministration of TDF with LPV/r resulted in increased tenofovir exposures at steady state, possibly through increased absorption, and this increase is not believed to be clinically relevant based on the safety and efficacy of Lopinavir/ritonavir-containing regimens in HIV-infected patients in long-term controlled clinical trials. Expand
Tenofovir disoproxil fumarate–emtricitabine coformulation for once-daily dual NRTI backbone
Truvada® is the coformulation of tenofovir disoproxil fumarate (TDF; 300 mg) and emtricitabine (FTC; 200 mg) in a single tablet, providing the nucleotide backbone for once-daily dosing, as aExpand
Tenofovir disoproxil fumarate–emtricitabine coformulation for once-daily dual NRTI backbone
Truvada® is the coformulation of tenofovir disoproxil fumarate (TDF; 300 mg) and emtricitabine (FTC; 200 mg) in a single tablet, providing the nucleotide backbone for once-daily dosing, as aExpand
Pharmacokinetics of Tenofovir Disoproxil Fumarate and Ritonavir-Boosted Saquinavir Mesylate Administered Alone or in Combination at Steady State
TLDR
No clinically relevant interactions between TDF and RTV-boosted SQV were observed under conditions simulating clinical practice, and modestly increased SQV exposures are not clinically meaningful given its clinical use with RTV already results in >10-fold-higher SQV levels. Expand
Tenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV.
TLDR
The combination of tenofovir DF and emtricitabineplus efavirenz fulfilled the criteria for noninferiority to a fixed dose of zidovudine and lamivudine plus efvirenz and proved superior in terms of virologic suppression, CD4 response, and adverse events resulting in discontinuation of the study drugs. Expand
Antiviral Activity, Pharmacokinetics, and Dose Response of the HIV-1 Integrase Inhibitor GS-9137 (JTK-303) in Treatment-Naive and Treatment-Experienced Patients
TLDR
GS-9137 demonstrated substantial short-term antiviral activity and was well tolerated as monotherapy, thus warranting further study. Expand
Systemic and Renal Pharmacokinetics of Adefovir and Tenofovir Upon Coadministration
TLDR
It is demonstrated that coadministration of tenofovir disoproxil fumarate and adefovir dipivoxil does not result in substantial changes to their individual pharmacokinetic profiles. Expand
Lack of Pharmacokinetic Drug Interaction between Tenofovir Disoproxil Fumarate and Nelfinavir Mesylate
ABSTRACT A study explored the pharmacokinetics of tenofovir (300 mg administered once daily) and nelfinavir (1,250 mg twice daily) when coadministered in 29 healthy volunteers. Tenofovir, nelfinavir,Expand
Effect of Tenofovir Disoproxil Fumarate on the Pharmacokinetics and Pharmacodynamics of Total, R‐, and S‐Methadone
TLDR
To evaluate the potential effect of tenofovir disoproxil fumarate (DF) on the pharmacokinetics of methadone, a drug used for the treatment of heroin addiction with high abuse potential. Expand
Current concepts in antiretroviral therapy failure.
  • C. del Rio
  • Medicine
  • Topics in HIV medicine : a publication of the International AIDS Society, USA
  • 2006
TLDR
When designing a regimen for a patient for whom antiretroviral therapy has failed, the regimen should contain at least 3 active drugs, and regimens are best selected with assistance from genotypic and phenotypic drug resistance testing. Expand
...
1
2
3
...