Abacavir/lamivudine combination in the treatment of HIV: a review

Sivasubramanian, Geetha; Frempong-Manso, Emmanuel; MacArthur, Rodger D.

doi:10.2147/tcrm.s1657

Cited by 7 publications

(2 citation statements)

References 62 publications

(69 reference statements)

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“…Abacavir and its derivates are widely used in human medicine, especially HIV type 1, in combination with other antiviral drugs to enhance efficacy against HIV [ 25 , 26 ]. Because of low solubility, high cytotoxicity, low bioavailability, and a lack of target specificity of many antiviral chemotherapeutics [ 27 ], phosphorylation was proposed to increase the bioavailability and decrease the cytotoxicity of the activated nucleoside analogs in virus-infected cells [ 28 ].…”

Section: Abacavir and Its Derivatesmentioning

confidence: 99%

Antiviral Chemotherapy in Avian Medicine—A Review

Szotowska,

Ledwoń

2024

Viruses

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This review article describes the current knowledge about the use of antiviral chemotherapeutics in avian species, such as farm poultry and companion birds. Specific therapeutics are described in alphabetical order including classic antiviral drugs, such as acyclovir, abacavir, adefovir, amantadine, didanosine, entecavir, ganciclovir, interferon, lamivudine, penciclovir, famciclovir, oseltamivir, ribavirin, and zidovudine, repurposed drugs, such as ivermectin and nitazoxanide, which were originally used as antiparasitic drugs, and some others substances showing antiviral activity, such as ampligen, azo derivates, docosanol, fluoroarabinosylpyrimidine nucleosides, and novel peptides. Most of them have only been used for research purposes and are not widely used in clinical practice because of a lack of essential pharmacokinetic and safety data. Suggested future research directions are also highlighted.

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Section: Abacavir and Its Derivatesmentioning

confidence: 99%

Antiviral Chemotherapy in Avian Medicine—A Review

Szotowska,

Ledwoń

2024

Viruses

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“…The antiviral efficacy of dolutegravir, abacavir, and lamivudine has been demonstrated for the constituent compounds alone and in various combinations. 5 , 6 , 7 , 8 , 9 , 10 Efficacy, including an ability to suppress viral replication, has been demonstrated for coadministration of dolutegravir 50 mg with abacavir 600 mg/lamivudine 300 mg. 8 , 9 , 10 This combination also exhibited improved safety and efficacy through 144 weeks of repeat dosing compared with fixed‐dose combination therapy of efavirenz/tenofovir disoproxil fumarate/emtricitabine and had fewer discontinuations due to adverse events (AEs). 8 , 9 In addition, switching to the single‐tablet regimen abacavir/dolutegravir/lamivudine was noninferior to continuing current antiretroviral therapy in a phase 3b study of adults infected with HIV‐1 and stable viral suppression.…”

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confidence: 99%

Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of Abacavir/Dolutegravir/Lamivudine Combination Tablets in Healthy Japanese Study Participants

Singh

Adkison²,

Wolstenholme

et al. 2021

Clinical Pharm in Drug Dev

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Pharmacokinetics, safety, and tolerability of abacavir 600 mg/dolutegravir 50 mg/lamivudine 300 mg were assessed in this phase 1, single-arm, open-label, single-dose study in fasted healthy male (n = 4) and female (n = 8) participants of Japanese heritage. Participants received a single dose of abacavir 600 mg/dolutegravir 50 mg/lamivudine 300 mg after an 8-hour fast, with safety assessments and blood samples for pharmacokinetic parameters collected through 72 hours after dosing. Geometric mean maximum plasma concentrations were 5.22 μg/mL (time to maximum concentration [t max ], 1.01 hours) for abacavir, 4.13 μg/mL (t max , 3.50 hours) for dolutegravir, and 3.35 μg/mL (t max , 2.98 hours) for lamivudine. Geometric mean area under the concentration-time curve values were 18.20, 71.60, and 16.60 μg • h/mL for abacavir, dolutegravir, and lamivudine, respectively. No adverse events were reported, and no clinically significant findings were observed in laboratory values, physical examinations, or 12-lead electrocardiographic parameters. Single-tablet administration of abacavir 600 mg/dolutegravir 50 mg/lamivudine 300 mg was well tolerated in Japanese participants. Exposure to abacavir and lamivudine was comparable with that seen in previous studies. A modest increase in exposure to dolutegravir vs previous clinical studies was observed but is not expected to impact the clinical management of HIV-1 or increase the risk for adverse events.

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