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Saquinavir

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1. Saquinavir plus methylprednisolone ameliorates experimental acute lung injury (PubMed)

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 previously investigated. In this study, the effects of SQV on lipopolysaccharide (LPS)-mediated

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2018 Brazilian Journal of Medical and Biological Research

2. Saquinavir Ameliorates Liver Warm Ischemia-Reperfusion-Induced Lung Injury via HMGB-1- and P38/JNK-Mediated TLR-4-Dependent Signaling Pathways (PubMed)

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

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2017 Mediators of inflammation

3. Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells (PubMed)

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

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2017 Oncology letters

4. The HIV-protease inhibitor saquinavir reduces proliferation, invasion and clonogenicity in cervical cancer cell lines (PubMed)

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, clonogenicity and radiosensitivity were evaluated by crystal violet staining. Proteasomal activities were assessed using a cell-based assay and immunoblotting. Cell cycle was analyzed by propidium

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2016 Oncology letters

5. Saquinavir Loaded Acetalated Dextran Microconfetti – a Long Acting Protease Inhibitor Injectable (PubMed)

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. Grinding techniques were then used to process these scaffolds into injectables which are termed saquinavir microconfetti. Microconfetti was analyzed for in vitro and in vivo release

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2016 Pharmaceutical research

6. Saquinavir

Saquinavir Saquinavir Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Saquinavir Saquinavir Aka: Saquinavir , Invirase From Related (...) Chapters II. Mechanism III. Disadvantages Weak effect Expensive May worsen resistance for better drugs IV. Adverse Effects Rash Interval (rare) V. Drug Interactions supplements (do not use with Saquinavir) Reduces Saquinavir concentrations by 50% Levels may remain reduced even after stopiing VI. Dosing Saquinavir 600 mg PO tid ($572/month) If taken without food, may have no antiviral activity Take within 2 hours after a full meal Meals increase absorption and decrease GI upset VII. References Images

2018 FP Notebook

7. Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats (PubMed)

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 of RESV on P-gp and CYP 3A activities in vitro and in vivo on oral SQV pharmacokinetics in rats.In vitro

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2016 Drug design, development and therapy

8. Factors responsible for the variability of saquinavir absorption: studies using an instrumented dog model. (PubMed)

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 absorbed from the gut was insignificantly different from that of unlabeled saquinavir, suggesting first-pass gut metabolism was unimportant. The bioavailability of saquinavir under fasting condition

2016 Pharmaceutical research

9. Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients

Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search (...) for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100). Please remove one or more studies before adding more. Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been

2014 Clinical Trials

10. Pharmacokinetic Interaction Between Nevirapine and Saquinavir-sgc in HIV-1 Infected Patients

Pharmacokinetic Interaction Between Nevirapine and Saquinavir-sgc in HIV-1 Infected Patients Pharmacokinetic Interaction Between Nevirapine and Saquinavir-sgc in HIV-1 Infected Patients - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100). Please remove one or more (...) studies before adding more. Pharmacokinetic Interaction Between Nevirapine and Saquinavir-sgc in HIV-1 Infected Patients The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our for details. ClinicalTrials.gov Identifier: NCT02184286 Recruitment Status : Terminated First Posted : July 9, 2014 Last Update Posted : July 14, 2014 Sponsor: Boehringer Ingelheim

2014 Clinical Trials

11. CPY3A4-Mediated α-Hydroxyaldehyde Formation in Saquinavir Metabolism (PubMed)

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 in human liver microsomes. Among these novel metabolites, one α-hydroxyaldehyde produced from SQV N

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2014 Drug Metabolism and Disposition

12. New-Onset Saquinavir-Induced Diabetes (PubMed)

New-Onset Saquinavir-Induced Diabetes 24265371 2014 12 11 2018 12 02 1935-5548 36 12 2013 Dec Diabetes care Diabetes Care New-onset saquinavir-induced diabetes. e199 10.2337/dc13-1645 van Zoelen Marieke A D MA Corresponding author: Marieke A.D. van Zoelen, m.a.d.vanzoelen@umcutrecht.nl. Hoepelman A I M AI de Valk H W HW eng Case Reports Letter United States Diabetes Care 7805975 0149-5992 0 Blood Glucose 0 HIV Protease Inhibitors 0 Hypoglycemic Agents 0 Insulin L3JE09KZ2F Saquinavir IM Adult (...) Blood Glucose metabolism Diabetes Mellitus blood chemically induced drug therapy Follow-Up Studies HIV Infections drug therapy HIV Protease Inhibitors adverse effects therapeutic use HIV-1 Humans Hypoglycemic Agents therapeutic use Insulin therapeutic use Male Saquinavir adverse effects therapeutic use 2013 11 23 6 0 2013 11 23 6 0 2014 12 17 6 0 ppublish 24265371 36/12/e199 10.2337/dc13-1645 PMC3836088 Ann Pharmacother. 2000 May;34(5):580-4 10852083 Cancer Res. 2005 Sep 15;65(18):8256-65 16166302 J

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2013 Diabetes Care

13. Saquinavir

Saquinavir Saquinavir Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Saquinavir Saquinavir Aka: Saquinavir , Invirase From Related (...) Chapters II. Mechanism III. Disadvantages Weak effect Expensive May worsen resistance for better drugs IV. Adverse Effects Rash Interval (rare) V. Drug Interactions supplements (do not use with Saquinavir) Reduces Saquinavir concentrations by 50% Levels may remain reduced even after stopiing VI. Dosing Saquinavir 600 mg PO tid ($572/month) If taken without food, may have no antiviral activity Take within 2 hours after a full meal Meals increase absorption and decrease GI upset VII. References Images

2015 FP Notebook

14. A Study of Ritonavir-Boosted Invirase (Saquinavir) in Treatment-Naïve HIV-1 Infected Patients

A Study of Ritonavir-Boosted Invirase (Saquinavir) in Treatment-Naïve HIV-1 Infected Patients A Study of Ritonavir-Boosted Invirase (Saquinavir) in Treatment-Naïve HIV-1 Infected Patients - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100). Please remove one (...) or more studies before adding more. A Study of Ritonavir-Boosted Invirase (Saquinavir) in Treatment-Naïve HIV-1 Infected Patients The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our for details. ClinicalTrials.gov Identifier: NCT01638650 Recruitment Status : Completed First Posted : July 12, 2012 Last Update Posted : November 2, 2016 Sponsor: Hoffmann

2012 Clinical Trials

15. Thorough QT/QTc study of ritonavir-boosted saquinavir following multiple-dose administration of therapeutic and supratherapeutic doses in healthy participants. (PubMed)

Thorough QT/QTc study of ritonavir-boosted saquinavir following multiple-dose administration of therapeutic and supratherapeutic doses in healthy participants. The effect of saquinavir-boosted ritonavir at therapeutic (1000/100 mg twice daily [bid]) and supratherapeutic (1500/100 mg bid) doses was evaluated in a double-blind, placebo- and positive-controlled (moxifloxacin 400 mg) 4-way crossover thorough QT/QTc study. Least squares mean estimated study-specific QTc (QTcS) change from dense (...) ddQTcS(dense) >60 ms. More participants with ≥1 adverse event received saquinavir/ritonavir. PubMed search and Roche postmarketing data did not reveal publications or reports directly presenting the effect of saquinavir on QT/QTc or causing torsade de pointes.

2012 Journal of clinical pharmacology

16. Targeting SVCT for enhanced drug absorption: Synthesis and in vitro evaluation of a novel vitamin C conjugated prodrug of saquinavir (PubMed)

Targeting SVCT for enhanced drug absorption: Synthesis and in vitro evaluation of a novel vitamin C conjugated prodrug of saquinavir In order to improve oral absorption, a novel prodrug of saquinavir (Saq), ascorbyl-succinic-saquinavir (AA-Su-Saq) targeting sodium dependent vitamin C transporter (SVCT) was synthesized and evaluated. Aqueous solubility, stability and cytotoxicity were determined. Affinity of AA-Su-Saq towards efflux pump P-glycoprotein (P-gp) and recognition of AA-Su-Saq by SVCT (...) were studied. Transepithelial permeability across polarized MDCK-MDR1 and Caco-2 cells were determined. Metabolic stability of AA-Su-Saq in rat liver microsomes was investigated. AA-Su-Saq appears to be fairly stable in both DPBS and Caco-2 cells with half lives of 9.65 and 5.73 h, respectively. Uptake of [(3)H]Saquinavir accelerated by 2.7 and 1.9 fold in the presence of 50 μM Saq and AA-Su-Saq in MDCK-MDR1 cells. Cellular accumulation of [(14)C]AA diminished by about 50-70% relative to control

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2011 International journal of pharmaceutics

17. Observational Study on Predictors of Response to Invirase (Saquinavir) Treatment in Treatment-naïve Patients With HIV Infection

Observational Study on Predictors of Response to Invirase (Saquinavir) Treatment in Treatment-naïve Patients With HIV Infection Observational Study on Predictors of Response to Invirase (Saquinavir) Treatment in Treatment-naïve Patients With HIV Infection - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have (...) reached the maximum number of saved studies (100). Please remove one or more studies before adding more. Observational Study on Predictors of Response to Invirase (Saquinavir) Treatment in Treatment-naïve Patients With HIV Infection The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our for details. ClinicalTrials.gov Identifier: NCT01297127 Recruitment

2011 Clinical Trials

18. Bioequivalence study of two oral tablet formulations containing saquinavir mesylate boosted with ritonavir in healthy male subjects. (PubMed)

Bioequivalence study of two oral tablet formulations containing saquinavir mesylate boosted with ritonavir in healthy male subjects. Saquinavir (SAQ) mesylate (CAS 149845-06-7) is a potent inhibitor of the HIV-1 protease indicated in combination with other antiretrovirals for the management of HIV-1 infection. The objective of this study was to compare rate and extent of absorption and to assess the bioequivalence between a new pharmaceutical equivalent tablet formulation containing 500 mg

2011 Arzneimittel-Forschung

19. Randomized comparison of metabolic and renal effects of saquinavir/r or atazanavir/r plus tenofovir/emtricitabine in treatment-naïve HIV-1-infected patients. (PubMed)

Randomized comparison of metabolic and renal effects of saquinavir/r or atazanavir/r plus tenofovir/emtricitabine in treatment-naïve HIV-1-infected patients. The aim of the study was to compare the effects on lipids, body composition and renal function of once-daily ritonavir-boosted saquinavir (SQV/r) or atazanavir (ATV/r) in combination with tenofovir/emtricitabine (TDF/FTC) over 48 weeks.An investigator-initiated, randomized, open-label, multinational trial comparing SQV/r 2000/100 mg

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2011 HIV medicine

20. Safety and Efficacy in HIV-1-Infected Patients Treated with Ritonavir-Boosted Saquinavir Mesylate (PubMed)

Safety and Efficacy in HIV-1-Infected Patients Treated with Ritonavir-Boosted Saquinavir Mesylate OBJECTIVE: To evaluate the safety, tolerability, and efficacy of ritonavir-boosted saquinavir 1000/100 mg twice daily administered as a 500 mg film-coated tablet in HIV-1-infected patients. METHODS: In this open-label, observational, 24-week survey conducted in 8 European countries, eligible HIV-infected participants had been prescribed saquinavir/ritonavir in combination with other nonprotease (...) increased by 75 cells/microL. In the subpopulation analysis, the greatest efficacy benefits occurred in participants who were treatment-naïve and in those not having received prior PI therapy. CONCLUSIONS: Treatment with the saquinavir 500 mg film-coated tablet resulted in few grade 3 or 4 AEs and was well tolerated and effective in a broad population of patients.

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2010 Archives of drug information

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