saquinavir

Summary

Summary: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.

Top Publications

  1. Martin R, Butterworth A, Gardiner D, Kirk K, McCarthy J, Skinner Adams T. Saquinavir inhibits the malaria parasite's chloroquine resistance transporter. Antimicrob Agents Chemother. 2012;56:2283-9 pubmed publisher
    The antiretroviral protease inhibitors (APIs) ritonavir, saquinavir, and lopinavir, used to treat HIV infection, inhibit the growth of Plasmodium falciparum at clinically relevant concentrations...
  2. McLean K, VanDeVen N, Sorenson D, Daudi S, Liu J. The HIV protease inhibitor saquinavir induces endoplasmic reticulum stress, autophagy, and apoptosis in ovarian cancer cells. Gynecol Oncol. 2009;112:623-30 pubmed publisher
    ..the need for novel treatment approaches in ovarian cancer, we sought to determine whether the protease inhibitor saquinavir has antineoplastic activity in ovarian cancer cell lines, and to elucidate the mechanism through which this ..
  3. Lamotte C, Landman R, Peytavin G, Mentre F, Gerbe J, Brun Vezinet F, et al. Once-daily dosing of saquinavir soft-gel capsules and ritonavir combination in HIV-1-infected patients (IMEA015 study). Antivir Ther. 2004;9:247-56 pubmed
    This was a prospective pilot study evaluating a saquinavir (SQV) soft-gel capsules (SGC)/ritonavir (RTV)-containing once-daily regimen over a follow-up of 3 months...
  4. Ananworanich J, Kosalaraksa P, Hill A, Siangphoe U, Bergshoeff A, Pancharoen C, et al. Pharmacokinetics and 24-week efficacy/safety of dual boosted saquinavir/lopinavir/ritonavir in nucleoside-pretreated children. Pediatr Infect Dis J. 2005;24:874-9 pubmed
    To assess the pharmacokinetics and 24-week efficacy and safety of dual boosted saquinavir/lopinavir/ritonavir combination in children...
  5. Jain R, Agarwal S, Majumdar S, Zhu X, Pal D, Mitra A. Evasion of P-gp mediated cellular efflux and permeability enhancement of HIV-protease inhibitor saquinavir by prodrug modification. Int J Pharm. 2005;303:8-19 pubmed
    ..for limiting oral bioavailability, tissue penetration and increasing metabolism of the HIV protease inhibitor saquinavir (SQV)...
  6. Maffeo A, Bellomi F, Solimeo I, Bambacioni F, Scagnolari C, De Pisa F, et al. P-glycoprotein expression affects the intracellular concentration and antiviral activity of the protease inhibitor saquinavir in a T cell line. New Microbiol. 2004;27:119-26 pubmed
    ..initially unexpected, phenomenon, a study was undertaken with the aims of investigating whether treatment with saquinavir (SQV) induces Pgp expression in primary or transformed human T cell lines and, primarily, establishing whether ..
  7. Plosker G, Scott L. Saquinavir: a review of its use in boosted regimens for treating HIV infection. Drugs. 2003;63:1299-324 pubmed
    Protease inhibitor boosting involves concurrent administration of a protease inhibitor, such as saquinavir, plus a potent inhibitor of cytochrome P450 (CYP) 3A4, usually ritonavir in subtherapeutic doses...
  8. Donia M, Maksimovic Ivanic D, Mijatovic S, Mojic M, Miljkovic D, Timotijevic G, et al. In vitro and in vivo anticancer action of Saquinavir-NO, a novel nitric oxide-derivative of the protease inhibitor saquinavir, on hormone resistant prostate cancer cells. Cell Cycle. 2011;10:492-9 pubmed
    The NO-derivative of the HIV protease inhibitor saquinavir (Saq-NO) is a nontoxic variant of the parental drug with enhanced anticancer activity on several cell lines...
  9. Berginc K, Trontelj J, Kristl A. The influence of aged garlic extract on the uptake of saquinavir and darunavir into HepG2 cells and rat liver slices. Drug Metab Pharmacokinet. 2010;25:307-13 pubmed
    ..Liver transport of HIV protease inhibitors (saquinavir, darunavir) was assessed in the presence of aged garlic extract, because the HIV-infected often consume garlic ..

More Information

Publications62

  1. Kuo Y, Su F. Transport of stavudine, delavirdine, and saquinavir across the blood-brain barrier by polybutylcyanoacrylate, methylmethacrylate-sulfopropylmethacrylate, and solid lipid nanoparticles. Int J Pharm. 2007;340:143-52 pubmed
    ..of the anti-human immunodeficiency virus (HIV) agents, including stavudine (D4T), delavirdine (DLV), and saquinavir (SQV), across the in vitro blood-brain barrier (BBB) was studied...
  2. Schmitt C, Hofmann C, Riek M, Patel A, Zwanziger E. Effect of saquinavir-ritonavir on cytochrome P450 3A4 activity in healthy volunteers using midazolam as a probe. Pharmacotherapy. 2009;29:1175-81 pubmed publisher
    To investigate the inhibitory potential of multiple doses of ritonavir-boosted saquinavir on the pharmacokinetics of oral midazolam, a cytochrome P450 (CYP) 3A4 model substrate...
  3. Marcelin A, Flandre P, de Mendoza C, Roquebert B, Peytavin G, Valer L, et al. Clinical validation of saquinavir/ritonavir genotypic resistance score in protease-inhibitor-experienced patients. Antivir Ther. 2007;12:247-52 pubmed
    To identify a genotypic score for resistance to saquinavir boosted with ritonavir (SQV/r; 1,000/100 mg twice daily)-based regimens in protease inhibitor (PI)-experienced patients...
  4. Chen X, Venkatesh S. Miniature device for aqueous and non-aqueous solubility measurements during drug discovery. Pharm Res. 2004;21:1758-61 pubmed
    ..compounds, the solubility of carbamazepine in various cosolvent systems, and the pH-solubility profile of saquinavir were determined using the miniature device...
  5. Stoica I, Sadiq S, Coveney P. Rapid and accurate prediction of binding free energies for saquinavir-bound HIV-1 proteases. J Am Chem Soc. 2008;130:2639-48 pubmed publisher
    ..Poisson-Boltzmann surface area (MM/PBSA) technique to the ranking of binding affinities of the inhibitor saquinavir with the wild type (WT) and three resistant mutants of HIV-1 protease: L90M, G48V, and G48V/L90M...
  6. Janneh O, Hartkoorn R, Jones E, Owen A, Ward S, Davey R, et al. Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir. Br J Pharmacol. 2008;155:875-83 pubmed publisher
    ..cells (PBMCs) and examined the effects of manipulation of influx/efflux transporters on the uptake of saquinavir and lopinavir. The expression of hOATPs was studied by PCR...
  7. Wittayanarakul K, Aruksakunwong O, Sompornpisut P, Sanghiran Lee V, Parasuk V, Pinitglang S, et al. Structure, dynamics and solvation of HIV-1 protease/saquinavir complex in aqueous solution and their contributions to drug resistance: molecular dynamic simulations. J Chem Inf Model. 2005;45:300-8 pubmed
    ..to examine detailed information on the structure and dynamical properties of the HIV-1 PR complexed with saquinavir in the three protonated states, monoprotonates at Asp25 (Mono-25) and Asp25'(Mono-25') and diprotonate (Di-Pro) ..
  8. Mudigonda K, Jukanti R, Apte S, Ajjala D, Shrivastava W, Kandikere V, et al. HPLC quantification of the HIV-1 protease inhibitor saquinavir in brain and testis of mice. Biomed Chromatogr. 2006;20:1028-32 pubmed
    A rapid, reliable HPLC method with UV detection (240 nm) was developed and validated for quantitation of saquinavir in mice brain and testis...
  9. Kim S, Kim S, Choi H, Han H. Enhanced systemic exposure of saquinavir via the concomitant use of curcumin-loaded solid dispersion in rats. Eur J Pharm Sci. 2013;49:800-4 pubmed publisher
    The present study aimed to evaluate the effect of curcumin-loaded solid dispersion on the pharmacokinetics of saquinavir in rats...
  10. Leonis G, Steinbrecher T, Papadopoulos M. A contribution to the drug resistance mechanism of darunavir, amprenavir, indinavir, and saquinavir complexes with HIV-1 protease due to flap mutation I50V: a systematic MM-PBSA and thermodynamic integration study. J Chem Inf Model. 2013;53:2141-53 pubmed publisher
    ..on wild-type (WT) and mutated HIV-1 protease (HIV-1 PR) complexes with darunavir, amprenavir, indinavir, and saquinavir to clarify the mechanism of resistance due to the I50V flap mutation...
  11. Kilby J, Hill A, Buss N. The effect of ritonavir on saquinavir plasma concentration is independent of ritonavir dosage: combined analysis of pharmacokinetic data from 97 subjects. HIV Med. 2002;3:97-104 pubmed
    To determine the correlation between ritonavir (RTV) dose and the degree of enhancement of saquinavir (SQV) exposure...
  12. Martin Facklam M, Burhenne J, Ding R, Fricker R, Mikus G, Walter Sack I, et al. Dose-dependent increase of saquinavir bioavailability by the pharmaceutic aid cremophor EL. Br J Clin Pharmacol. 2002;53:576-81 pubmed
    ..g. by cytochrome P450 3A (CYP3A), in both gastrointestinal tract and liver. Many drugs including saquinavir are substrates of both PGP and CYP3A...
  13. Kraus M, Müller Ide H, Rückrich T, Bader J, Overkleeft H, Driessen C. Ritonavir, nelfinavir, saquinavir and lopinavir induce proteotoxic stress in acute myeloid leukemia cells and sensitize them for proteasome inhibitor treatment at low micromolar drug concentrations. Leuk Res. 2014;38:383-92 pubmed publisher
    ..b>Saquinavir, nelfinavir and lopinavir were likewise cytotoxic against primary AML cells, triggered PS-induced apoptosis, ..
  14. Lavielle M, Mentre F. Estimation of population pharmacokinetic parameters of saquinavir in HIV patients with the MONOLIX software. J Pharmacokinet Pharmacodyn. 2007;34:229-49 pubmed
    ..u-psud.fr/~lavielle/monolix/logiciels. In this paper we apply MONOLIX to the analysis of the pharmacokinetics of saquinavir, a protease inhibitor, from concentrations measured after single dose administration in 100 HIV patients, some ..
  15. Walmsley S, Avihingsanon A, Slim J, Ward D, Ruxrungtham K, Brunetta J, et al. Gemini: a noninferiority study of saquinavir/ritonavir versus lopinavir/ritonavir as initial HIV-1 therapy in adults. J Acquir Immune Defic Syndr. 2009;50:367-74 pubmed publisher
    ..multicenter, open-label, noninferiority trial in treatment-naive HIV-1-infected adults randomized to either saquinavir/ritonavir (SQV/r) 1000 mg/100 mg twice a day or lopinavir/ritonavir (LPV/r) 400 mg/100 mg twice a day, each with ..
  16. Molto J, Llibre J, Ribera E, Mínguez C, del Río J, Pedrol E, et al. Saquinavir exposure in HIV-infected patients with chronic viral hepatitis. J Antimicrob Chemother. 2009;63:992-7 pubmed publisher
    ..assess the influence of hepatitis B virus or hepatitis C virus co-infection and the extent of liver fibrosis on saquinavir and ritonavir pharmacokinetics in HIV-infected subjects without liver function impairment...
  17. van der Lugt J, Colbers A, Molto J, Hawkins D, van der Ende M, Vogel M, et al. The pharmacokinetics, safety and efficacy of boosted saquinavir tablets in HIV type-1-infected pregnant women. Antivir Ther. 2009;14:443-50 pubmed
    Pregnancy affects the pharmacokinetics of most protease inhibitors. Saquinavir, when administered in a tablet formulation, has not been studied extensively in this setting...
  18. Valdivieso E, Rangel A, Moreno J, Saugar J, Cañavate C, Alvar J, et al. Effects of HIV aspartyl-proteinase inhibitors on Leishmania sp. Exp Parasitol. 2010;126:557-63 pubmed publisher
    ..amastigotes by the human immunodeficiency virus (HIV) aspartyl-proteinase inhibitors, Ac-Leu-Val-Phenylalaninal, Saquinavir mesylate and Nelfinavir, the latter two being used as part of antiretroviral therapy...
  19. Tommasi C, Bellagamba R, Tempestilli M, D Avolio A, Gallo A, Ivanovic J, et al. Marked increase in etravirine and saquinavir plasma concentrations during atovaquone/proguanil prophylaxis. Malar J. 2011;10:141 pubmed publisher
    ..subtype B infection treated with a salvage regimen including maraviroc, raltegravir, etravirine and unboosted saquinavir who started atovaquone/proguanil prophylaxis, is reported...
  20. Ford J, Boffito M, Wildfire A, Hill A, Back D, Khoo S, et al. Intracellular and plasma pharmacokinetics of saquinavir-ritonavir, administered at 1,600/100 milligrams once daily in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother. 2004;48:2388-93 pubmed
    Ritonavir-boosted saquinavir (SQV/r) is currently licensed as a twice-daily regimen. Reducing the pill burden with once-daily dosing may improve adherence...
  21. Vrouenraets S, Wit F, Fernandez Garcia E, Moyle G, Jackson A, Allavena C, et al. Randomized comparison of metabolic and renal effects of saquinavir/r or atazanavir/r plus tenofovir/emtricitabine in treatment-naïve HIV-1-infected patients. HIV Med. 2011;12:620-31 pubmed publisher
    ..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...
  22. von Hentig N, Muller A, Rottmann C, Wolf T, Lutz T, Klauke S, et al. Pharmacokinetics of saquinavir, atazanavir, and ritonavir in a twice-daily boosted double-protease inhibitor regimen. Antimicrob Agents Chemother. 2007;51:1431-9 pubmed
    The objective of this study was to evaluate the pharmacokinetics of atazanavir (ATV), saquinavir (SQV), and ritonavir (RTV) in a boosted double-protease inhibitor (PI) therapy regimen without reverse transcriptase inhibitors (RTIs)...
  23. Griffin B, O Driscoll C. A comparison of intestinal lymphatic transport and systemic bioavailability of saquinavir from three lipid-based formulations in the anaesthetised rat model. J Pharm Pharmacol. 2006;58:917-25 pubmed
    b>Saquinavir is a lipophilic, poorly water-soluble HIV protease inhibitor that undergoes extensive first-pass metabolism and exhibits poor oral bioavailability...
  24. Saen Oon S, Aruksakunwong O, Wittayanarakul K, Sompornpisut P, Hannongbua S. Insight into analysis of interactions of saquinavir with HIV-1 protease in comparison between the wild-type and G48V and G48V/L90M mutants based on QM and QM/MM calculations. J Mol Graph Model. 2007;26:720-7 pubmed
    b>Saquinavir (SQV) was the first HIV-1 PR inhibitor licensed for clinical use and widely used for acquired immunodeficiency syndrome (AIDS) therapy. Its effectiveness, however, has been hindered by the emergence of resistant mutations...
  25. Jamois C, Smith P, Morrison R, Riek M, Patel A, Schmitt C, et al. Effect of saquinavir/ritonavir (1000/100 mg bid) on the pharmacokinetics of methadone in opiate-dependent HIV-negative patients on stable methadone maintenance therapy. Addict Biol. 2009;14:321-7 pubmed publisher
    This study was performed to determine the effect of two protease inhibitors, saquinavir (SQV, oral 1000 mg bid) boosted by ritonavir (RTV, oral 100 mg bid), on pharmacokinetics (PK) of methadone in opiate-dependent HIV-negative patients ..
  26. Petković F, Blaževski J, Momcilovic M, Timotijevic G, Zocca M, Mijatovic S, et al. Saquinavir-NO inhibits S6 kinase activity, impairs secretion of the encephalytogenic cytokines interleukin-17 and interferon-gamma and ameliorates experimental autoimmune encephalomyelitis. J Neuroimmunol. 2013;259:55-65 pubmed publisher
    NO-hybridization of the HIV protease inhibitor Saquinavir generates a new chemical entity named Saq-NO, that retains the anti-viral activity and exerts lower toxicity...
  27. von Hentig N, Babacan E, Staszewski S, Stürmer M, Doerr H, Lotsch J. Predictive factors for response to a boosted dual HIV-protease inhibitor therapy with saquinavir and lopinavir in extensively pre-treated patients. Antivir Ther. 2007;12:1237-46 pubmed
    ..Patients received lopinavir/ritonavir 400/100 mg and saquinavir 1,000 mg twice daily without reverse transcriptase inhibitors (RTI)...
  28. Bunupuradah T, van der Lugt J, Kosalaraksa P, Engchanil C, Boonrak P, Puthanakit T, et al. Safety and efficacy of a double-boosted protease inhibitor combination, saquinavir and lopinavir/ritonavir, in pretreated children at 96 weeks. Antivir Ther. 2009;14:241-8 pubmed
    ..safety and use of therapeutic drug monitoring (TDM) of a double-boosted protease inhibitor (PI) combination, saquinavir (SQV) and lopinavir/ritonavir (LPV/r), in Thai HIV type-1 (HIV-1)-infected children who had failed on reverse ..
  29. Schutt M, Zhou J, Meier M, Klein H. Long-term effects of HIV-1 protease inhibitors on insulin secretion and insulin signaling in INS-1 beta cells. J Endocrinol. 2004;183:445-54 pubmed
    ..cells were incubated for 48 h with different concentrations of amprenavir, indinavir, nelfinavir, ritonavir or saquinavir, stimulated with 20 mM d-glucose, and insulin determined in the supernatant...
  30. Haas D, Zala C, Schrader S, Piliero P, Jaeger H, Nunes D, et al. Therapy with atazanavir plus saquinavir in patients failing highly active antiretroviral therapy: a randomized comparative pilot trial. AIDS. 2003;17:1339-49 pubmed
    To assess the safety, efficacy of atazanavir (400 and 600 mg)/saquinavir (1200 mg) once daily versus ritonavir/saquinavir (400 mg/400 mg) twice daily with two nucleoside reverse transcriptase inhibitors (NRTIs) in highly active ..
  31. Meaden E, Hoggard P, Newton P, Tjia J, Aldam D, Cornforth D, et al. P-glycoprotein and MRP1 expression and reduced ritonavir and saquinavir accumulation in HIV-infected individuals. J Antimicrob Chemother. 2002;50:583-8 pubmed
    ..of these transporters on human lymphocytes correlated with intracellular concentrations of ritonavir and saquinavir. Drug efflux transporter expression (P-glycoprotein and MRP1) on peripheral blood mononuclear cells isolated ..
  32. Mahajan S, Roy I, Xu G, Yong K, Ding H, Aalinkeel R, et al. Enhancing the delivery of anti retroviral drug "Saquinavir" across the blood brain barrier using nanoparticles. Curr HIV Res. 2010;8:396-404 pubmed
    ..In the current study, we have stably incorporated the antiviral drug, Saquinavir, within Tf-conjugated quantum rods (QRs), which are novel nanoparticles with unique optical properties...
  33. Shah L, Amiji M. Intracellular delivery of saquinavir in biodegradable polymeric nanoparticles for HIV/AIDS. Pharm Res. 2006;23:2638-45 pubmed
    ..poly(epsilon-caprolactone) (PEO-PCL) nanoparticulate system as an intracellular delivery vehicle for saquinavir, an anti-HIV protease inhibitor...
  34. Beloqui A, Solinís M, Gascón A, del Pozo Rodríguez A, des Rieux A, Préat V. Mechanism of transport of saquinavir-loaded nanostructured lipid carriers across the intestinal barrier. J Control Release. 2013;166:115-23 pubmed publisher
    ..lipid carriers (NLCs) as a tool to enhance the oral bioavailability of poorly soluble compounds using saquinavir (SQV), a BCS class IV drug and P-gp substrate as a model drug, and (ii) to study NLC transport mechanisms across ..
  35. Wittayanarakul K, Aruksakunwong O, Saen Oon S, Chantratita W, Parasuk V, Sompornpisut P, et al. Insights into saquinavir resistance in the G48V HIV-1 protease: quantum calculations and molecular dynamic simulations. Biophys J. 2005;88:867-79 pubmed
    ..The G48V is considered the key signature residue mutation of HIV-1 protease developing with saquinavir therapy...
  36. Savoia D, Allice T, Tovo P. Antileishmanial activity of HIV protease inhibitors. Int J Antimicrob Agents. 2005;26:92-4 pubmed
    ..Two HIV protease inhibitors (PI), indinavir and saquinavir, have been shown to block proteasome functions; we therefore investigated their effects on the growth of two ..
  37. Robbins B, Capparelli E, Chadwick E, Yogev R, Serchuck L, Worrell C, et al. Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. Antimicrob Agents Chemother. 2008;52:3276-83 pubmed publisher
    ..o. q12h (with NNRTI). We calculated the LPV inhibitory quotient (IQ), and when the IQ was <15, saquinavir (SQV) 750 mg/m(2) p.o. q12h was added to the regimen. We studied 26 HIV-infected patients...
  38. Boffito M, Maitland D, Dickinson L, Back D, Hill A, Fletcher C, et al. Pharmacokinetics of saquinavir hard-gel/ritonavir and atazanavir when combined once daily in HIV Type 1-infected individuals administered different atazanavir doses. AIDS Res Hum Retroviruses. 2006;22:749-56 pubmed
    The pharmacokinetics and short-term safety of atazanavir 150 and 200 mg, when coadministered with saquinavir/ritonavir 1600/100 mg once daily, were evaluated...
  39. Chi J, Jayewardene A, Stone J, Motoya T, Aweeka F. Simultaneous determination of five HIV protease inhibitors nelfinavir, indinavir, ritonavir, saquinavir and amprenavir in human plasma by LC/MS/MS. J Pharm Biomed Anal. 2002;30:675-84 pubmed
    ..to measure the levels of five HIV protease inhibitors nelfinavir (NFV), indinavir (IDV), ritonavir (RTV), saquinavir (SQV) and amprenavir (APV) in human plasma...
  40. Williams G, Liu A, Knipp G, Sinko P. Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2). Antimicrob Agents Chemother. 2002;46:3456-62 pubmed
    To determine if saquinavir mesylate (saquinavir) is a substrate of human multidrug resistance-associated protein 1 (hMRP1 [ABCC1]) or hMRP2 (cMOAT, or ABCC2), MDCKII cells that overexpress either hMRP1 (MDCKII-MRP1) or hMRP2 (MDCKII-MRP2) ..
  41. Boffito M, Dickinson L, Hill A, Back D, Moyle G, Nelson M, et al. Pharmacokinetics of once-daily saquinavir/ritonavir in HIV-infected subjects: comparison with the standard twice-daily regimen. Antivir Ther. 2004;9:423-9 pubmed
    To evaluate the steady-state pharmacokinetics and safety of two once-daily saquinavir/ritonavir (SQV/RTV) regimens, 1600/100 and 2000/100 mg, in HIV-positive patients...
  42. Dragsted U, Gerstoft J, Pedersen C, Peters B, Duran A, Obel N, et al. Randomized trial to evaluate indinavir/ritonavir versus saquinavir/ritonavir in human immunodeficiency virus type 1-infected patients: the MaxCmin1 Trial. J Infect Dis. 2003;188:635-42 pubmed
    ..virus (HIV) type 1-infected patients assigned indinavir/ritonavir (Idv/Rtv; 800/100 mg 2 times daily) or saquinavir/ritonavir (Sqv/Rtv; 1000/100 mg 2 times daily) in an open-label, randomized (1:1), multicenter, phase 4 design...
  43. Patricia E, Domingo P, Gutierrez M, Gracia M, Fuster M, Molto J, et al. Saquinavir/ritonavir monotherapy as a new nucleoside-sparing maintenance strategy in long-term virologically suppressed HIV-infected patients. Curr HIV Res. 2010;8:467-70 pubmed
    The high antiviral potency and low toxicity of saquinavir/ritonavir (SQV/r) prompted us to assess a viable strategy in chronic virologically suppressed HIV-infected patients. A randomized, multicenter pilot trial...
  44. Ruxrungtham K, Boyd M, Bellibas S, Zhang X, Dorr A, Kolis S, et al. Lack of interaction between enfuvirtide and ritonavir or ritonavir-boosted saquinavir in HIV-1-infected patients. J Clin Pharmacol. 2004;44:793-803 pubmed
    ..The HIV protease inhibitors ritonavir and saquinavir both inhibit cytochrome P450 (CYP450) isoenzymes, and low-dose ritonavir is often used to boost pharmacokinetic ..
  45. Autar R, Boffito M, Hassink E, Wit F, Ananworanich J, Siangphoe U, et al. Interindividual variability of once-daily ritonavir boosted saquinavir pharmacokinetics in Thai and UK patients. J Antimicrob Chemother. 2005;56:908-13 pubmed
    Differential exposure to saquinavir/ritonavir may lead to therapy failure. The objective was to identify factors that influence variability of saquinavir/ritonavir plasma concentrations...
  46. Fontas E, van Leth F, Sabin C, Friis Møller N, Rickenbach M, d Arminio Monforte A, et al. Lipid profiles in HIV-infected patients receiving combination antiretroviral therapy: are different antiretroviral drugs associated with different lipid profiles?. J Infect Dis. 2004;189:1056-74 pubmed
    ..regimens; however, receipt of nelfinavir was associated with reduced risk of lower HDL-c levels, and receipt of saquinavir was associated with lower TC : HDL-c ratios...
  47. Fletcher C, Jiang H, Brundage R, Acosta E, Haubrich R, Katzenstein D, et al. Sex-based differences in saquinavir pharmacology and virologic response in AIDS Clinical Trials Group Study 359. J Infect Dis. 2004;189:1176-84 pubmed
    AIDS Clinical Trials Group study 359 was a controlled study of saquinavir with either ritonavir or nelfinavir, together with delavirdine, adefovir, or both, in indinavir-experienced persons...
  48. Maksimovic Ivanic D, Mijatovic S, Miljkovic D, Harhaji Trajkovic L, Timotijevic G, Mojic M, et al. The antitumor properties of a nontoxic, nitric oxide-modified version of saquinavir are independent of Akt. Mol Cancer Ther. 2009;8:1169-78 pubmed publisher
    Application of the HIV protease inhibitor saquinavir (Saq) to cancer chemotherapy is limited by its numerous side effects. To overcome this toxicity, we modified the original compound by covalently attaching a nitric oxide (NO) group...
  49. Buchanan C, Buchanan N, Edgar K, Little J, Ramsey M, Ruble K, et al. Pharmacokinetics of saquinavir after intravenous and oral dosing of saquinavir: hydroxybutenyl-beta-cyclodextrin formulations. Biomacromolecules. 2008;9:305-13 pubmed
    The current research evaluated the ability of hydroxybutenyl-beta-cyclodextrin (HBenBCD) to enhance saquinavir in vitro solubility and in vivo oral bioavailability; both the base and mesylate salt forms of saquinavir were investigated...
  50. Ribera E, Azuaje C, Lopez R, Domingo P, Curran A, Feijoo M, et al. Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis. J Antimicrob Chemother. 2007;59:690-7 pubmed
    To assess plasma steady-state pharmacokinetics (PK) of rifampicin, isoniazid, saquinavir and ritonavir in HIV and tuberculosis (TB) co-infected patients, and investigate potential interactions between TB drugs and protease inhibitors (PIs)..
  51. Montaner J, Schutz M, Schwartz R, Jayaweera D, Burnside A, Walmsley S, et al. Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patients. MedGenMed. 2006;8:36 pubmed
    ..To evaluate the efficacy and safety of saquinavir-soft-gelatin capsule (SGC)/ritonavir combination (1600 mg/100 mg) vs efavirenz (600 mg) both once daily and ..
  52. Barillari G, Iovane A, Bacigalupo I, Palladino C, Bellino S, Leone P, et al. Ritonavir or saquinavir impairs the invasion of cervical intraepithelial neoplasia cells via a reduction of MMP expression and activity. AIDS. 2012;26:909-19 pubmed publisher
    ..HIV infection, herein we assessed the impact of therapeutic concentrations of HIV-PIs including indinavir (IDV), saquinavir (SQV) or ritonavir (RTV) on cells obtained from CIN or cervical carcinoma lesions of HIV-negative women...
  53. Fröhlich M, Hoffmann M, Burhenne J, Mikus G, Weiss J, Haefeli W. Association of the CYP3A5 A6986G (CYP3A5*3) polymorphism with saquinavir pharmacokinetics. Br J Clin Pharmacol. 2004;58:443-4 pubmed