Pharmacokinetics of the combination raltegravir/atazanavir in HIV-1-infected patients

A Jansen; radboud Colbers; A J A M van der Ven; C Richter; J K Rockstroh; J C Wasmuth; M van Luin; D M Burger

doi:10.1111/hiv.12029

Pharmacokinetics of the combination raltegravir/atazanavir in HIV-1-infected patients

A Jansen
, radboud Colbers
, A J A M van der Ven
, C Richter
, J K Rockstroh
, J C Wasmuth
, M van Luin
, D M Burger

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

OBJECTIVES: To evaluate the use of raltegravir with unboosted atazanavir in combination with one nucleoside reverse transcriptase inhibitor (NRTI) (lamivudine or emtricitabine) as a potentially well-tolerated once-daily (qd) maintenance regimen.

METHODS: We compared the pharmacokinetics of raltegravir 400 mg twice daily (bid) with raltegravir 800 mg qd in HIV-infected patients (n=17) on unboosted atazanavir (600 mg qd) in combination with lamivudine or emtricitabine.

RESULTS: The area under the plasma concentration vs. time curve for a dose interval t (AUC0 -t ) of 800 mg qd divided by 2 was not significantly different from the AUC0 -t of 400 mg bid (P=0.664) but the minimum concentration (C min ) was 72% lower with the qd regimen (P=0.002). The regimen was well tolerated and the viral load remained undetectable in all patients during the 6 weeks of the study follow-up.

CONCLUSIONS: A qd regimen of raltegravir 800 mg, atazanavir 600 mg and lamivudine or emtricitabine resulted in favourable pharmacokinetic profiles and good short-term safety and efficacy data. Larger phase IIb studies are needed to explore this novel regimen.

Original language	English
Pages (from-to)	449-52
Number of pages	4
Journal	HIV Medicine
Volume	14
Issue number	7
DOIs	https://doi.org/10.1111/hiv.12029
Publication status	Published - Aug 2013
Externally published	Yes

Keywords

Adolescent
Adult
Aged
Aged, 80 and over
Anti-HIV Agents/administration & dosage
Atazanavir Sulfate
Drug Administration Schedule
Drug Therapy, Combination
Female
HIV Infections/drug therapy
HIV-1/physiology
Humans
Male
Middle Aged
Oligopeptides/administration & dosage
Pyridines/administration & dosage
Pyrrolidinones/administration & dosage
Raltegravir Potassium
Reverse Transcriptase Inhibitors/pharmacokinetics
Viral Load
Young Adult

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10.1111/hiv.12029

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title = "Pharmacokinetics of the combination raltegravir/atazanavir in HIV-1-infected patients",

abstract = "OBJECTIVES: To evaluate the use of raltegravir with unboosted atazanavir in combination with one nucleoside reverse transcriptase inhibitor (NRTI) (lamivudine or emtricitabine) as a potentially well-tolerated once-daily (qd) maintenance regimen.METHODS: We compared the pharmacokinetics of raltegravir 400 mg twice daily (bid) with raltegravir 800 mg qd in HIV-infected patients (n=17) on unboosted atazanavir (600 mg qd) in combination with lamivudine or emtricitabine.RESULTS: The area under the plasma concentration vs. time curve for a dose interval t (AUC0 -t ) of 800 mg qd divided by 2 was not significantly different from the AUC0 -t of 400 mg bid (P=0.664) but the minimum concentration (C min ) was 72\% lower with the qd regimen (P=0.002). The regimen was well tolerated and the viral load remained undetectable in all patients during the 6 weeks of the study follow-up.CONCLUSIONS: A qd regimen of raltegravir 800 mg, atazanavir 600 mg and lamivudine or emtricitabine resulted in favourable pharmacokinetic profiles and good short-term safety and efficacy data. Larger phase IIb studies are needed to explore this novel regimen.",

keywords = "Adolescent, Adult, Aged, Aged, 80 and over, Anti-HIV Agents/administration \& dosage, Atazanavir Sulfate, Drug Administration Schedule, Drug Therapy, Combination, Female, HIV Infections/drug therapy, HIV-1/physiology, Humans, Male, Middle Aged, Oligopeptides/administration \& dosage, Pyridines/administration \& dosage, Pyrrolidinones/administration \& dosage, Raltegravir Potassium, Reverse Transcriptase Inhibitors/pharmacokinetics, Viral Load, Young Adult",

author = "A Jansen and radboud Colbers and \{van der Ven\}, \{A J A M\} and C Richter and Rockstroh, \{J K\} and Wasmuth, \{J C\} and \{van Luin\}, M and Burger, \{D M\}",

note = "{\textcopyright} 2013 British HIV Association.",

year = "2013",

month = aug,

doi = "10.1111/hiv.12029",

language = "English",

volume = "14",

pages = "449--52",

journal = "HIV Medicine",

issn = "1464-2662",

publisher = "Wiley-Blackwell Publishing Ltd",

number = "7",

}

TY - JOUR

T1 - Pharmacokinetics of the combination raltegravir/atazanavir in HIV-1-infected patients

AU - Jansen, A

AU - Colbers, radboud

AU - van der Ven, A J A M

AU - Richter, C

AU - Rockstroh, J K

AU - Wasmuth, J C

AU - van Luin, M

AU - Burger, D M

PY - 2013/8

Y1 - 2013/8

N2 - OBJECTIVES: To evaluate the use of raltegravir with unboosted atazanavir in combination with one nucleoside reverse transcriptase inhibitor (NRTI) (lamivudine or emtricitabine) as a potentially well-tolerated once-daily (qd) maintenance regimen.METHODS: We compared the pharmacokinetics of raltegravir 400 mg twice daily (bid) with raltegravir 800 mg qd in HIV-infected patients (n=17) on unboosted atazanavir (600 mg qd) in combination with lamivudine or emtricitabine.RESULTS: The area under the plasma concentration vs. time curve for a dose interval t (AUC0 -t ) of 800 mg qd divided by 2 was not significantly different from the AUC0 -t of 400 mg bid (P=0.664) but the minimum concentration (C min ) was 72% lower with the qd regimen (P=0.002). The regimen was well tolerated and the viral load remained undetectable in all patients during the 6 weeks of the study follow-up.CONCLUSIONS: A qd regimen of raltegravir 800 mg, atazanavir 600 mg and lamivudine or emtricitabine resulted in favourable pharmacokinetic profiles and good short-term safety and efficacy data. Larger phase IIb studies are needed to explore this novel regimen.

AB - OBJECTIVES: To evaluate the use of raltegravir with unboosted atazanavir in combination with one nucleoside reverse transcriptase inhibitor (NRTI) (lamivudine or emtricitabine) as a potentially well-tolerated once-daily (qd) maintenance regimen.METHODS: We compared the pharmacokinetics of raltegravir 400 mg twice daily (bid) with raltegravir 800 mg qd in HIV-infected patients (n=17) on unboosted atazanavir (600 mg qd) in combination with lamivudine or emtricitabine.RESULTS: The area under the plasma concentration vs. time curve for a dose interval t (AUC0 -t ) of 800 mg qd divided by 2 was not significantly different from the AUC0 -t of 400 mg bid (P=0.664) but the minimum concentration (C min ) was 72% lower with the qd regimen (P=0.002). The regimen was well tolerated and the viral load remained undetectable in all patients during the 6 weeks of the study follow-up.CONCLUSIONS: A qd regimen of raltegravir 800 mg, atazanavir 600 mg and lamivudine or emtricitabine resulted in favourable pharmacokinetic profiles and good short-term safety and efficacy data. Larger phase IIb studies are needed to explore this novel regimen.

KW - Adolescent

KW - Adult

KW - Aged

KW - Aged, 80 and over

KW - Anti-HIV Agents/administration & dosage

KW - Atazanavir Sulfate

KW - Drug Administration Schedule

KW - Drug Therapy, Combination

KW - Female

KW - HIV Infections/drug therapy

KW - HIV-1/physiology

KW - Humans

KW - Male

KW - Middle Aged

KW - Oligopeptides/administration & dosage

KW - Pyridines/administration & dosage

KW - Pyrrolidinones/administration & dosage

KW - Raltegravir Potassium

KW - Reverse Transcriptase Inhibitors/pharmacokinetics

KW - Viral Load

KW - Young Adult

U2 - 10.1111/hiv.12029

DO - 10.1111/hiv.12029

M3 - Article

C2 - 23506243

SN - 1464-2662

VL - 14

SP - 449

EP - 452

JO - HIV Medicine

JF - HIV Medicine

IS - 7

ER -

Pharmacokinetics of the combination raltegravir/atazanavir in HIV-1-infected patients

Abstract

Keywords

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