The Use of the Protease Inhibitor, Saquinavir, to Treat Anal Cancer Spheroids Derived from HPV Transgenic Mice. Anal cancer is associated with high-risk human papillomavirus infection and oncoprotein expression. We have identified several protease inhibitors, used to treat HIV, that decrease oncogene expression. The aim of this project is to determine whether the protease inhibitor, Saquinavir was performed in an American Association for Accreditation of Laboratory Animal Care approved facility. Spheroids were placed in treatment groups: no treatment, vehicle (dimethyl sulfoxide), and 15 μM Saquinavir. Spheroids were imaged immediately prior to treatment and 24-hours post-treatment. Spheroid diameters were measured using ImageJ and mean percent reduction was calculated for each spheroid
Saquinavir An official website of the United States government Here's how you know Log inAccess keysNCBI HomepageMyNCBI HomepageMain ContentMain NavigationBookshelfSearch databaseBooksAll DatabasesAssemblyBiocollectionsBioProjectBioSampleBooksClinVarConserved DomainsdbGaPdbVarGeneGenomeGEO DataSetsGEO ProfilesGTRHomoloGeneIdentical Protein GroupsMedGenMeSHNLM and EffectsSummary of Use during LactationNo published information is available on the use of saquinavir during breastfeeding. Saquinavir is not a recommended agent during breastfeeding.[1,2]Drug LevelsMaternal Levels. Relevant published information was not found as of the revision date.Infant Levels. Relevant published information was not found as of the revision date.Effects in Breastfed InfantsRelevant
Saquinavir plus methylprednisolone ameliorates experimental acute lung injury Glucocorticoid insensitivity is an important barrier to the treatment of several inflammatory diseases, including acute lung injury (ALI). Saquinavir (SQV) is an inhibitor of the human immunodeficiency virus protease, and the therapeutic effects of SQV in ALI accompanied with glucocorticoid insensitivity have not been
Saquinavir Ameliorates Liver Warm Ischemia-Reperfusion-Induced Lung Injury via HMGB-1- and P38/JNK-Mediated TLR-4-Dependent Signaling Pathways Liver ischemia and reperfusion (I/R) induce local and distant tissue injuries, contributing to morbidity and mortality in a wider range of pathologies. This is especially seen under uncontrolled aseptic inflammatory conditions, leading to injury of remote organs, such as lung injury, and even failure. Saquinavir (SQV) is a kind of HIV protease inhibitor that possesses an anti-inflammatory property. In this study, we investigated whether SQV suppresses Toll-like receptor 4- (TLR4-) dependent signaling pathways of high-mobility group box 1 (HMGB1) and P38/JNK, conferring protection against murine liver I/R-induced lung injury. To investigate our
Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells A reduced incidence and decreased clinical progression of uterine cervical intraepithelial neoplasia (CIN) has been observed in women infected with human immunodeficiency virus (HIV) treated with HIV-protease inhibitors (PIs). The HIV-PIs saquinavir (SQV) and ritonavir (RTV) have been demonstrated to efficiently inhibit invasion of human primary CIN cells by downregulating the expression of matrix metalloproteinase (MMP)-9. The present study further investigated the molecular mechanisms underlying the activity of SQV and RTV in CIN. The results of the present study indicate that the treatment of human primary CIN cells with SQV or RTV
The HIV-protease inhibitor saquinavir reduces proliferation, invasion and clonogenicity in cervical cancer cell lines Innovative therapies in cervical cancer (CC) remain a priority. Recent data indicate that human immunodeficiency virus (HIV)-protease inhibitors used in highly active antiretroviral therapy can exert direct antitumor activities also in HIV-free preclinical and clinical models . The aim of the present study was to evaluate the antineoplastic effects of various HIV-protease inhibitors (indinavir, ritonavir and saquinavir) on primary and established CC cell lines. Two CC cell lines established in our laboratory and four commercially available CC cell lines were treated with indinavir, ritonavir and saquinavir at different concentrations and for different times. Proliferation
Saquinavir Loaded Acetalated Dextran Microconfetti – a Long Acting Protease Inhibitor Injectable Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral injectables that deliver drug for months at a time have moved into late phase clinical trials. Unfortunately, these solid phase crystal formulations have inherent drawbacks in potential dose dumping and a greater likelihood for burst release of drug compared to polymeric formulations. Using electrospinning, acetalated dextran scaffolds containing the protease inhibitor saquinavir were created
Factors responsible for the variability of saquinavir absorption: studies using an instrumented dog model. To study the effect of dose and food on the bioavailability of saquinavir in dogs. A Youden Square block design was used for six female mongrel dogs (20-24 kg) who received six saquinavir treatments. The six randomized treatments were 1 mg/kg intravenous infusion over 30 min; 200, 400, 600 , and 800 mg of saquinavir in the form of 200-mg capsules given orally with food; and 400 mg of saquinavir given orally after an overnight fast. A 200-mg 14C-saquinavir capsule was used to replace one of the 200-mg unlabeled saquinavir capsules in the 200- and 800-mg oral study. Absorption of saquinavir from the gut was variable. (F(A): 49-95%). The 14C-saquinavir study shows that the total radioactivity
Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats The intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicated to have modulatory effects on P-gp and CYP 3A. Therefore, this study was to investigate the effects
CPY3A4-Mediated α-Hydroxyaldehyde Formation in Saquinavir Metabolism Saquinavir (SQV) is a protease inhibitor widely used for the treatment of human immunodeficiency virus (HIV) infection. We profiled SQV metabolism in mice using a metabolomic approach. Thirty SQV metabolites were identified in mouse feces and urine, of which 20 are novel. Most metabolites observed in mice were recapitulated
infections), atazanavir, indinavir, nelfinavir, ritonavir and saquinavir (medicines used in HIV-positive patients), clarithromycin and telithromycin (antibiotics), and nefazodone (used to treat depression). Why has Toviaz been approved?The CHMP decided that Toviaz’s benefits are greater than its risks and recommended that it be given marketing authorisation. Other information about ToviazThe European
with moderate inhibitors (e.g. cyclosporine, itraconazole,ritonavir, nelfinavir, saquinavir, tipranavir, posaconazole, and tacrolimus). Patients who are taking the P-glycoprotein inhibitors verapamil and quinidine should take the dabigatran dose 2 hours prior to adose of verapamil or quinidine. No dosage adjustment to dabigatran is recommended for patientsconcurrently taking these interacting medications
this transport system can increase systemic exposure to dabigatran. Concomitant use of the strong P-glycoprotein inhibitors (e.g. ketoconazole, dronedarone) is contraindicated. Caution is advised if taken with moderate inhibitors (e.g. cyclosporine, itraconazole, ritonavir, nelfinavir, saquinavir, tipranavir, posaconazole, and tacrolimus). Patients who are taking the P-glycoprotein inhibitors verapamil