Nelfinavir

Jarvis, Blair; Faulds, Diana

doi:10.2165/00003495-199856010-00013

Cited by 81 publications

(16 citation statements)

References 29 publications

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“…Nelfinavir is a selective inhibitor of HIV protease, which is responsible for posttranslational processing of HIV propeptides. 106 Yamamoto et al 107 had found that nelfinavir could strongly inhibit the replication of SARS-CoV. Therefore, nelfinavir could also be an option for the treatment of COVID-19.…”

Section: Nelfinavirmentioning

confidence: 99%

Potential interventions for novel coronavirus in China: A systematic review

Zhang

Liu

2020

Journal of Medical Virology

1,151

1,178

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An outbreak of a novel coronavirus (COVID-19 or 2019-CoV) infection has posed significant threats to international health and the economy. In the absence of treatment for this virus, there is an urgent need to find alternative methods to control the spread of disease. Here, we have conducted an online search for all treatment options related to coronavirus infections as well as some RNA-virus infection and we have found that general treatments, coronavirus-specific treatments, and antiviral treatments should be useful in fighting COVID-19. We suggest that the nutritional status of each infected patient should be evaluated before the administration of general treatments and the current children's RNA-virus vaccines including influenza vaccine should be immunized for uninfected people and health care

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Section: Nelfinavirmentioning

confidence: 99%

Potential interventions for novel coronavirus in China: A systematic review

Zhang

Liu

2020

Journal of Medical Virology

1,151

1,178

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“…A unique mutation of the protease gene confers resistance. Diarrhoea is the most frequently reported adverse event in patients receiving nelfinavir-based combination therapy, together with rash, nausea, headache and asthenia Nelfinavir is metabolised by the cytochrome P450 system [27]. Although less effective than other PIs, nelfinavir is positioned as an alternative agent for the treatment of adults and adolescents with HIV infection and is an option for those unable to tolerate other protease inhibitors, as well as in pregnant and paediatric patients with HIV infection, due to prolonged viral suppression, good tolerability, a unique resistance profile [28,29].…”

Section: Hiv-1 Pismentioning

confidence: 99%

HIV Protease Inhibitors: Effect on the Opportunistic Protozoan Parasites

Alfonso

Monzote²

2011

Open Med Chem J

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The impact of highly active antiretroviral therapy (HAART) in the natural history of AIDS disease has been allowed to prolong the survival of people with HIV infection, particularly whose with increased HIV viral load. Additionally, the antiretroviral therapy could exert a certain degree of protection against parasitic diseases. A number of studies have been evidenced a decrease in the incidence of opportunistic parasitic infections in the era of HAART. Although these changes have been attributed to the restoration of cell-mediated immunity, induced by either non-nucleoside reverse transcriptase inhibitors or HIV protease inhibitors, in combination with at least two nucleoside reverse transcriptase inhibitors included in HAART, there are evidence that the control of these parasitic infections in HIV-positive persons under HAART, is also induced by the inhibition of the proteases of the parasites. This review focuses on the principal available data related with therapeutic HIV-protease inhibitors and their in vitro and in vivo effects on the opportunistic protozoan parasites.

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“…However, diarrhea of moderate to severe intensity can occur in patients receiving multi-drug therapy [21-23]. The mechanisms underlying antiretroviral-induced diarrhea are unclear.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of HIV protease and nucleoside reverse transcriptase inhibitors on proliferation, necrosis, apoptosis in intestinal epithelial cells and electrolyte and water transport and epithelial barrier function in mice

et al. 2010

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BackgroundProtease inhibitors (PI's) and reverse transcriptase drugs are important components of highly active antiretroviral therapy (HAART) for treating human acquired immunodeficiency syndrome (AIDS). Long-term clinical therapeutic efficacy and treatment compliance of these agents have been limited by undesirable side-effects, such as diarrhea. This study aims to investigate the effects of selected antiretroviral agents on intestinal histopathology and function in vivo and on cell proliferation and death in vitro.MethodsSelected antiretroviral drugs were given orally over 7 days, to Swiss mice, as follows: 100 mg/kg of nelfinavir (NFV), indinavir (IDV), didanosine (DDI) or 50 mg/kg of zidovudine (AZT). Intestinal permeability measured by lactulose and mannitol assays; net water and electrolyte transport, in perfused intestinal segments; and small intestinal morphology and cell apoptosis were assessed in treated and control mice. In vitro cell proliferation was evaluated using the WST-1 reagent and apoptosis and necrosis by flow cytometry analysis.ResultsNFV, IDV, AZT and DDI caused significant reductions in duodenal and in jejunal villus length (p < 0.05). IDV and AZT increased crypt depth in the duodenum and AZT increased crypt depth in the jejunum. NFV, AZT and DDI significantly decreased ileal crypt depth. All selected antiretroviral drugs significantly increased net water secretion and electrolyte secretion, except for DDI, which did not alter water or chloride secretion. Additionally, only NFV significantly increased mannitol and lactulose absorption. NFV and IDV caused a significant reduction in cell proliferation in vitro at both 24 h and 48 h. DDI and AZT did not alter cell proliferation. There was a significant increase in apoptosis rates in IEC-6 cells after 24 h with 70 ug/mL of NFV (control: 4.7% vs NFV: 22%) while IDV, AZT and DDI did not show any significant changes in apoptosis compared to the control group. In jejunal sections, IDV and NFV significantly increased the number of TUNEL positive cells.ConclusionThe PI's, NFV and IDV, increased cell apoptosis in vivo, water and electrolyte secretion and intestinal permeability and decreased villus length and cell proliferation. NFV was the only drug tested that increased cell apoptosis in vitro. The nucleoside reverse transcriptase inhibitors, AZT and DDI, did not affect cell apoptosis or proliferation. These findings may partly explain the intestinal side-effects associated with PI's.

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Nelfinavir

Cited by 81 publications

References 29 publications

Potential interventions for novel coronavirus in China: A systematic review

Potential interventions for novel coronavirus in China: A systematic review

HIV Protease Inhibitors: Effect on the Opportunistic Protozoan Parasites

Evaluation of HIV protease and nucleoside reverse transcriptase inhibitors on proliferation, necrosis, apoptosis in intestinal epithelial cells and electrolyte and water transport and epithelial barrier function in mice

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