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High Instantaneous Inhibitory Potential of Bictegravir and the New Spiro-β-Lact...

Bártolo, Inês; Moura, Ines; Gonçalves, Paloma; Diniz, Ana Rita; Borrego, Pedro; Martin, Francisco; Figueiredo, Inês; Gomes, Perpétua

Integrase inhibitors (INIs) are an important class of drugs for treating HIV-2 infection,given the limited number of drugs active against this virus. While the clinical efficacy of raltegravirand dolutegravir is well established, the clinical efficacy of bictegravir for treating HIV-2 infected patients has not been determined. Little information is available regarding the activity of bictegravir against HIV-2 i...


High Instantaneous Inhibitory Potential of Bictegravir and the New Spiro-ß-Lact...

Bártolo, Inês; Moranguinho, Inês; Gonçalves, Paloma; Ana Rita Diniz; Borrego, Pedro; Martin, Francisco; Figueiredo, Inês; Gomes, Perpetua

Integrase inhibitors (INIs) are an important class of drugs for treating HIV-2 infection, given the limited number of drugs active against this virus. While the clinical efficacy of raltegravir and dolutegravir is well established, the clinical efficacy of bictegravir for treating HIV-2 infected patients has not been determined. Little information is available regarding the activity of bictegravir against HIV-2...


High instantaneous inhibitory potential of Bictegravir and the new Spiro-β-Lact...

Bártolo, Inês; Moranguinho, Inês; Gonçalves, Paloma; Diniz, Ana Rita; Borrego, Pedro; Martin, Francisco; Figueiredo, Inês; Gomes, Perpétua

Integrase inhibitors (INIs) are an important class of drugs for treating HIV-2 infection, given the limited number of drugs active against this virus. While the clinical efficacy of raltegravir and dolutegravir is well established, the clinical efficacy of bictegravir for treating HIV-2 infected patients has not been determined. Little information is available regarding the activity of bictegravir against HIV-2...


The 2-hydroxy-nevirapine metabolite as a candidate for boosting apolipoprotein ...

Marinho, Aline T.; Batuca, Joana R.; Miranda, Joana P.; Caixas, Umbelina; Dias, Clara G.; Branco, Teresa; Soto, Karina; Pinheiro, Pedro

The antiretroviral nevirapine (NVP) is associated to a reduction of atherosclerotic lesions and increases in high-density lipoprotein (HDL)-cholesterol. Despite being a hepatotoxic drug, which forbids its re-purposing to other therapeutic areas, not all NVP metabolites have the same potential to induce toxicity. Our aim was to investigate the effects of NVP and its metabolites in an exploratory study, towards t...


In vitro evaluation of novel reverse transcriptase inhibitors TAF (tenofovir al...

Bártolo, Inês; Borrego, Pedro; Gomes, Perpétua; Gonçalves, Fátima; Caixas, Umbelina; Pinto, Inês V.; Taveira, Nuno

New antiretroviral drugs are needed to treat HIV-2 infected patients failing therapy. Herein, we evaluate the activity of novel reverse transcriptase inhibitors tenofovir alafenamide (TAF) and OBP-601(2,3-didehydro-3-deoxy-4-ethynylthymidine) against primary isolates from HIV-2 infected patients experiencing virologic failure. TAF and OBP-601 were tested against twelve primary isolates obtained from nine drug-e...


In vitro evaluation of novel reverse transcriptase inhibitors TAF (tenofovir al...

Bártolo, Inês; Borrego, Pedro; Gomes, Perpetua; Gonçalves, Maria Fátima; Caixas, Umbelina; Vaz-Pinto, Inês; Taveira, Nuno

New antiretroviral drugs are needed to treat HIV-2 infected patients failing therapy. Herein, we evaluate the activity of novel reverse transcriptase inhibitors tenofovir alafenamide (TAF) and OBP-601(2,3-didehydro-3-deoxy-4-ethynylthymidine) against primary isolates from HIV-2 infected patients experiencing virologic failure. TAF and OBP-601 were tested against twelve primary isolates obtained from nine drug-e...


Baseline susceptibility of primary HIV-2 to entry inhibitors

Borrego, Pedro; Calado, Rita; Marcelino, José M; Bártolo, Inês; Rocha, Cheila; Cavaco-Silva, Patrícia; Doroana, Manuela; Antunes, Francisco

Background: The baseline susceptibility of primary HIV-2 to maraviroc (MVC) and other entry inhibitors is currently unknown.


Baseline susceptibility of primary HIV-2 to entry inhibitors

Borrego, Pedro; Calado, Rita; Marcelino, José M.; Bártolo, Inês; Rocha, Cheila; Cavaco-Silva, Patricia; Doroana, Manuela; Antunes, Francisco

Background The baseline susceptibility of primary HIV-2 to maraviroc (MVC) and other entry inhibitors is currently unknown. Methods The susceptibility of 19 HIV-2 isolates obtained from asymptomatic and AIDS patients and seven HIV-1 clinical isolates to the fusion inhibitors enfuvirtide (ENF) and T-1249, and to the coreceptor antagonists AMD3100, TAK-779 and MVC, was measured using a TZM-bl cell-based assay. Th...


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