The role of dolutegravir in the management of HIV infection
Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naïve and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized...
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| Published in: | Infection and drug resistance Vol. 8; pp. 19 - 29 |
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| Main Authors: | , , , |
| Format: | Journal Article |
| Language: | English |
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Dove Medical Press Limited
01-01-2015
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| Abstract | Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naïve and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized by uridine diphosphate glucuronosyl transferase 1A1; no inhibition or induction of cytochrome P450 enzymes is noted. As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. Other adverse effects are minimal but include diarrhea, headache, and nausea. Clinical trials in treatment-naïve and experienced patients are ongoing and will be presented in this text. |
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| AbstractList | Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naive and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized by uridine diphosphate glucuronosyl transferase 1A1; no inhibition or induction of cytochrome P450 enzymes is noted. As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. Other adverse effects are minimal but include diarrhea, headache, and nausea. Clinical trials in treatment-naive and experienced patients are ongoing and will be presented in this text. Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naïve and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized by uridine diphosphate glucuronosyl transferase 1A1; no inhibition or induction of cytochrome P450 enzymes is noted. As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. Other adverse effects are minimal but include diarrhea, headache, and nausea. Clinical trials in treatment-naïve and experienced patients are ongoing and will be presented in this text. Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naive and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized by uridine diphosphate glucuronosyl transferase 1A1; no inhibition or induction of cytochrome P450 enzymes is noted. As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. Other adverse effects are minimal but include diarrhea, headache, and nausea. Clinical trials in treatment-naive and experienced patients are ongoing and will be presented in this text. Keywords: antiretroviral, integrase inhibitor, Tivicay®, treatment-naive studies, treatment-experienced studies |
| Audience | Academic |
| Author | Lockhart, Staci M Miller, Misty M Rathbun, R Chris Liedtke, Michelle D |
| AuthorAffiliation | 2 AbbVie Inc., Oklahoma City, OK, USA 1 Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA |
| AuthorAffiliation_xml | – name: 1 Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA – name: 2 AbbVie Inc., Oklahoma City, OK, USA |
| Author_xml | – sequence: 1 givenname: Misty M surname: Miller fullname: Miller, Misty M organization: Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA – sequence: 2 givenname: Michelle D surname: Liedtke fullname: Liedtke, Michelle D organization: Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA – sequence: 3 givenname: Staci M surname: Lockhart fullname: Lockhart, Staci M organization: AbbVie Inc., Oklahoma City, OK, USA – sequence: 4 givenname: R Chris surname: Rathbun fullname: Rathbun, R Chris organization: Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA |
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| Copyright | COPYRIGHT 2015 Dove Medical Press Limited 2015 Miller et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License 2015 |
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| Keywords | antiretroviral Tivicay treatment-experienced studies treatment-naïve studies integrase inhibitor |
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| Snippet | Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naïve and experienced patients. As a... Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naive and experienced patients. As a... |
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| Title | The role of dolutegravir in the management of HIV infection |
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