Saquinavir (BioDeep_00000018020)
human metabolite blood metabolite Chemicals and Drugs
代谢物信息卡片
(2S)-N-[(2S,3R)-4-[(3S)-3-(Tert-butyl-C-hydroxycarbonimidoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-[(quinolin-2-yl)formamido]butanediimidate
化学式: C38H50N6O5 (670.384249)
中文名称: 沙奎那韦
谱图信息:
最多检出来源 Homo sapiens(blood) 0.53%
分子结构信息
SMILES: CC(C)(C)NC(=O)C1CC2CCCCC2CN1CC(C(CC3=CC=CC=C3)NC(=O)C(CC(=O)N)NC(=O)C4=NC5=CC=CC=C5C=C4)O
InChI: InChI=1S/C38H50N6O5/c1-38(2,3)43-37(49)32-20-26-14-7-8-15-27(26)22-44(32)23-33(45)30(19-24-11-5-4-6-12-24)41-36(48)31(21-34(39)46)42-35(47)29-18-17-25-13-9-10-16-28(25)40-29/h4-6,9-13,16-18,26-27,30-33,45H,7-8,14-15,19-23H2,1-3H3,(H2,39,46)(H,41,48)(H,42,47)(H,43,49)/t26?,27?,30-,31-,32-,33+/m0/s1
描述信息
Saquinavir is only found in individuals that have used or taken this drug. It is 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. [PubChem]Saquinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
同义名列表
12 个代谢物同义名
(2S)-N-[(2S,3R)-4-[(3S)-3-(Tert-butyl-C-hydroxycarbonimidoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-[(quinolin-2-yl)formamido]butanediimidate; (2S)-N-[(2S,3R)-4-[(3S)-3-(tert-butylcarbamoyl)-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)succinamide; (2S)-N-[(2S,3R)-4-[(3S)-3-(tert-butylcarbamoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)butanediamide; Monomethanesulfonate, saquinavir; Saquinavir monomethanesulfonate; Saquinavir mesylate; SCHEMBL1176566; Saquinavir; Saquinivir; Sequinavir; Invirase; SQV
数据库引用编号
9 个数据库交叉引用编号
- PubChem: 3579812
- PubChem: 60787
- HMDB: HMDB0015362
- ChEMBL: CHEMBL296480
- Wikipedia: Saquinavir
- chemspider: 54783
- CAS: 1349873-79-5
- CAS: 127779-20-8
- PMhub: MS000001690
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
1 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Denio A Ridjab, Ignatius Ivan, Fanny Budiman, Dwi Jani Juliawati. Current evidence for the risk of PR prolongation, QRS widening, QT prolongation, from lopinavir, ritonavir, atazanavir, and saquinavir: A systematic review.
Medicine.
2021 Aug; 100(31):e26787. doi:
10.1097/md.0000000000026787. [PMID: 34397829] - Alireza Jalalvand, Somayeh Behjat Khatouni, Zahra Bahri Najafi, Foroozan Fatahinia, Narges Ismailzadeh, Behrokh Farahmand. Computational drug repurposing study of antiviral drugs against main protease, RNA polymerase, and spike proteins of SARS-CoV-2 using molecular docking method.
Journal of basic and clinical physiology and pharmacology.
2021 Jul; 33(1):85-95. doi:
10.1515/jbcpp-2020-0369. [PMID: 34265888] - Yusuke Tanaka, Tri-Hung Nguyen, Estelle J A Suys, Christopher J H Porter. Digestion of Lipid-Based Formulations Not Only Mediates Changes to Absorption of Poorly Soluble Drugs Due to Differences in Solubilization But Also Reflects Changes to Thermodynamic Activity and Permeability.
Molecular pharmaceutics.
2021 04; 18(4):1768-1778. doi:
10.1021/acs.molpharmaceut.1c00015. [PMID: 33729806] - Sekhar Talluri. Molecular Docking and Virtual Screening Based Prediction of Drugs for COVID-19.
Combinatorial chemistry & high throughput screening.
2021; 24(5):716-728. doi:
10.2174/1386207323666200814132149. [PMID: 32798373] - Martiniano Bello, Alberto Martínez-Muñoz, Irving Balbuena-Rebolledo. Identification of saquinavir as a potent inhibitor of dimeric SARS-CoV2 main protease through MM/GBSA.
Journal of molecular modeling.
2020 Nov; 26(12):340. doi:
10.1007/s00894-020-04600-4. [PMID: 33184722] - Teruhisa S Komatsu, Noriaki Okimoto, Yohei M Koyama, Yoshinori Hirano, Gentaro Morimoto, Yousuke Ohno, Makoto Taiji. Drug binding dynamics of the dimeric SARS-CoV-2 main protease, determined by molecular dynamics simulation.
Scientific reports.
2020 10; 10(1):16986. doi:
10.1038/s41598-020-74099-5. [PMID: 33046764] - Zhilong Jia, Xinyu Song, Jinlong Shi, Weidong Wang, Kunlun He. Transcriptome-based drug repositioning for coronavirus disease 2019 (COVID-19).
Pathogens and disease.
2020 06; 78(4):. doi:
10.1093/femspd/ftaa036. [PMID: 32667665] - Donald C Hall, Hai-Feng Ji. A search for medications to treat COVID-19 via in silico molecular docking models of the SARS-CoV-2 spike glycoprotein and 3CL protease.
Travel medicine and infectious disease.
2020 May; 35(?):101646. doi:
10.1016/j.tmaid.2020.101646. [PMID: 32294562] - Francesca L Wood, J Brian Houston, David Hallifax. Importance of the Unstirred Water Layer and Hepatocyte Membrane Integrity In Vitro for Quantification of Intrinsic Metabolic Clearance.
Drug metabolism and disposition: the biological fate of chemicals.
2018 03; 46(3):268-278. doi:
10.1124/dmd.117.078949. [PMID: 29233818] - Mingzhu He, Kai Fan Cheng, Sonya VanPatten, Ona Bloom, Betty Diamond, Yousef Al-Abed. A structural investigation of FISLE-412, a peptidomimetic compound derived from saquinavir that targets lupus autoantibodies.
Bioorganic & medicinal chemistry letters.
2017 10; 27(20):4725-4729. doi:
10.1016/j.bmcl.2017.08.070. [PMID: 28927788] - Xin Wang, Renlingzi Zhang, Yao Tong, Xibing Ding, Shuqing Jin, Xiang Zhao, Jiaying Zong, Zhixia Chen, Timothy R Billiar, Quan Li. High-mobility group box 1 protein is involved in the protective effect of Saquinavir on ventilation-induced lung injury in mice.
Acta biochimica et biophysica Sinica.
2017 Oct; 49(10):907-915. doi:
10.1093/abbs/gmx085. [PMID: 28981603] - Thiago Caon, Jadel Muller Kratz, Gislaine Kuminek, Melina Heller, Gustavo Amadeu Micke, Bibiana Verlindo de Araujo, Letícia Scherer Koester, Cláudia Maria Oliveira Simões. Pharmacokinetics of Saquinavir Mesylate from Oral Self-Emulsifying Lipid-Based Delivery Systems.
European journal of drug metabolism and pharmacokinetics.
2017 Feb; 42(1):135-141. doi:
10.1007/s13318-016-0321-x. [PMID: 26846485] - Sanelisiwe Nzuza, Sindiswa Zondi, Peter M O Owira. Naringin prevents HIV-1 protease inhibitors-induced metabolic complications in vivo.
PloS one.
2017; 12(11):e0183355. doi:
10.1371/journal.pone.0183355. [PMID: 29121676] - J Li, Y Liu, X Yu, J Zhang, J Gu, L Zhao. Reduced Oral Bioavailability and Altered Pharmacokinetics of Saquinavir by Co-administration with Biochanin A in Rats.
Drug research.
2016 Sep; 66(9):484-488. doi:
10.1055/s-0042-110393. [PMID: 27409329] - Jiapeng Li, Yang Liu, Jingru Zhang, Xiaotong Yu, Xiaoling Wang, Libo Zhao. Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats.
Drug design, development and therapy.
2016; 10(?):3699-3706. doi:
10.2147/dddt.s118723. [PMID: 27895462] - Marta Boffito, David Back, José M Gatell. Twenty years of boosting antiretroviral agents: where are we today?.
AIDS (London, England).
2015 Nov; 29(17):2229-33. doi:
10.1097/qad.0000000000000800. [PMID: 26544697] - Yuan He, Deng-ning Xia, Qiu-xia Li, Jin-song Tao, Yong Gan, Chi Wang. Enhancement of cellular uptake, transport and oral absorption of protease inhibitor saquinavir by nanocrystal formulation.
Acta pharmacologica Sinica.
2015 Sep; 36(9):1151-60. doi:
10.1038/aps.2015.53. [PMID: 26256404] - Graciela Cárdenas, M López-González, J F Monzón-Falconi, J L Soto-Hernández, D Perales-Martínez, C López-Vejar. Relation of cerebrospinal fluid/plasma HIV-RNA discordance with neurocognitive impairment.
The National medical journal of India.
2015 Sep; 28(5):228-32. doi:
NULL. [PMID: 27132951] - Nageswara Rao Ramisetti, Narendra Varma Nimmu, Gangu Naidu Challa. Ionic liquid-based dispersive liquid-liquid microextraction followed by RP-HPLC determination of saquinavir in rat serum: application to pharmacokinetics.
Biomedical chromatography : BMC.
2014 Dec; 28(12):1874-80. doi:
10.1002/bmc.3237. [PMID: 24944096] - Christoph Hagen, Stephan Werner, Susana Carregal-Romero, Ashraf N Malhas, Barbara G Klupp, Peter Guttmann, Stefan Rehbein, Katja Henzler, Thomas C Mettenleiter, David J Vaux, Wolfgang J Parak, Gerd Schneider, Kay Grünewald. Multimodal nanoparticles as alignment and correlation markers in fluorescence/soft X-ray cryo-microscopy/tomography of nucleoplasmic reticulum and apoptosis in mammalian cells.
Ultramicroscopy.
2014 Nov; 146(?):46-54. doi:
10.1016/j.ultramic.2014.05.009. [PMID: 24973653] - Hitendra S Mahajan, Milind S Mahajan, Pankaj P Nerkar, Anshuman Agrawal. Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting.
Drug delivery.
2014 Mar; 21(2):148-54. doi:
10.3109/10717544.2013.838014. [PMID: 24128122] - Feng Li, Jie Lu, Xiaochao Ma. CPY3A4-mediated α-hydroxyaldehyde formation in saquinavir metabolism.
Drug metabolism and disposition: the biological fate of chemicals.
2014 Feb; 42(2):213-20. doi:
10.1124/dmd.113.054874. [PMID: 24212380] - Yoshihisa Shitara, Kumiko Takeuchi, Toshiharu Horie. Long-lasting inhibitory effects of saquinavir and ritonavir on OATP1B1-mediated uptake.
Journal of pharmaceutical sciences.
2013 Sep; 102(9):3427-35. doi:
10.1002/jps.23477. [PMID: 23440887] - Ghaith Al-Jayyoussi, Daniel F Price, Danielle Francombe, Glyn Taylor, Mathew W Smith, Chris Morris, Chris D Edwards, Peter Eddershaw, Mark Gumbleton. Selectivity in the impact of P-glycoprotein upon pulmonary absorption of airway-dosed substrates: a study in ex vivo lung models using chemical inhibition and genetic knockout.
Journal of pharmaceutical sciences.
2013 Sep; 102(9):3382-94. doi:
10.1002/jps.23587. [PMID: 23670704] - Ichiro Ieiri, Shyohei Tsunemitsu, Kazuya Maeda, Yukie Ando, Noritomo Izumi, Miyuki Kimura, Naoe Yamane, Tsuyoshi Okuzono, Mariko Morishita, Naoki Kotani, Eri Kanda, Mariko Deguchi, Kyoko Matsuguma, Shunji Matsuki, Takeshi Hirota, Shin Irie, Hiroyuki Kusuhara, Yuichi Sugiyama. Mechanisms of pharmacokinetic enhancement between ritonavir and saquinavir; micro/small dosing tests using midazolam (CYP3A4), fexofenadine (p-glycoprotein), and pravastatin (OATP1B1) as probe drugs.
Journal of clinical pharmacology.
2013 Jun; 53(6):654-61. doi:
10.1002/jcph.62. [PMID: 23381882] - Atsuko Tomaru, Mariko Takeda-Morishita, Hirokazu Banba, Kozo Takayama. Analysis of the pharmacokinetic boosting effects of ritonavir on oral bioavailability of drugs in mice.
Drug metabolism and pharmacokinetics.
2013; 28(2):144-52. doi:
10.2133/dmpk.dmpk-12-rg-057. [PMID: 22971642] - Zhiying Wang, Dhananjay Pal, Ashim K Mitra. Stereoselective evasion of P-glycoprotein, cytochrome P450 3A, and hydrolases by peptide prodrug modification of saquinavir.
Journal of pharmaceutical sciences.
2012 Sep; 101(9):3199-213. doi:
10.1002/jps.23193. [PMID: 22611042] - Maria Martinez-Rebollar, Montserrat Lonca, Iñaki Perez, Dolors Soy, Mercè Brunet, Rosa Martin, Oriol Coll, Sandra Hernandez, Montserrat Laguno, Ana Milinkovic, Maria Larrousse, Marta Calvo, Jose L Blanco, Esteban Martínez, Jose M Gatell, Josep Mallolas. Pharmacokinetic study of saquinavir 500 mg plus ritonavir (1000/100 mg twice a day) in HIV-positive pregnant women.
Therapeutic drug monitoring.
2011 Dec; 33(6):772-7. doi:
10.1097/ftd.0b013e318236376d. [PMID: 22105596] - S M E Vrouenraets, F W N M Wit, E Fernandez Garcia, G J Moyle, A G Jackson, C Allavena, F Raffi, D T Jayaweera, S Mauss, C Katlama, M Fisher, L Slama, W D Hardy, E Dejesus, A van Eeden, P Reiss. Randomized comparison of metabolic and renal effects of saquinavir/r or atazanavir/r plus tenofovir/emtricitabine in treatment-naïve HIV-1-infected patients.
HIV medicine.
2011 Nov; 12(10):620-31. doi:
10.1111/j.1468-1293.2011.00941.x. [PMID: 21819530] - Chiara Tommasi, Rita Bellagamba, Massimo Tempestilli, Antonio D'Avolio, Anna L Gallo, Jelena Ivanovic, Emanuele Nicastri, Leopoldo P Pucillo, Pasquale Narciso. Marked increase in etravirine and saquinavir plasma concentrations during atovaquone/proguanil prophylaxis.
Malaria journal.
2011 May; 10(?):141. doi:
10.1186/1475-2875-10-141. [PMID: 21600016] - Patrice Muret, Caroline Solas. [Evidence-based therapeutic drug monitoring for saquinavir].
Therapie.
2011 May; 66(3):207-12. doi:
NULL. [PMID: 21819804] - Miriam Gyalrong-Steur, J R Bogner, U Seybold. Changes in lipid profiles after switching to a protease inhibitor-containing cART--unfavourable effect of fosamprenavir in obese patients.
European journal of medical research.
2011 Feb; 16(2):85-92. doi:
10.1186/2047-783x-16-2-85. [PMID: 21463988] - R Lledó-García, A Nácher, V G Casabó, M Merino-Sanjuán. A pharmacokinetic model for evaluating the impact of hepatic and intestinal first-pass loss of saquinavir in the rat.
Drug metabolism and disposition: the biological fate of chemicals.
2011 Feb; 39(2):294-301. doi:
10.1124/dmd.110.034488. [PMID: 20978105] - Xiaoping Zhang, Scott Fettner, Elke Zwanziger, Lucy Rowell, Miklos Salgo. Pharmacokinetic interaction study of ritonavir-boosted saquinavir in combination with rifabutin in healthy subjects.
Antimicrobial agents and chemotherapy.
2011 Feb; 55(2):680-7. doi:
10.1128/aac.00992-10. [PMID: 21135186] - Elena Toschi, Cecilia Sgadari, Laura Malavasi, Ilaria Bacigalupo, Chiara Chiozzini, Davide Carlei, Daniela Compagnoni, Stefania Bellino, Roberto Bugarini, Mario Falchi, Clelia Palladino, Patrizia Leone, Giovanni Barillari, Paolo Monini, Barbara Ensoli. Human immunodeficiency virus protease inhibitors reduce the growth of human tumors via a proteasome-independent block of angiogenesis and matrix metalloproteinases.
International journal of cancer.
2011 Jan; 128(1):82-93. doi:
10.1002/ijc.25550. [PMID: 20617515] - Gustavo A Yerino, Emilia K Halabe, Elvira Zini, Ethel C Feleder. Bioequivalence study of two oral tablet formulations containing saquinavir mesylate boosted with ritonavir in healthy male subjects.
Arzneimittel-Forschung.
2011; 61(8):481-7. doi:
10.1055/s-0031-1296231. [PMID: 21950153] - Shamsunder S Dodiya, Sandip S Chavhan, Krutika K Sawant, Aruna G Korde. Solid lipid nanoparticles and nanosuspension formulation of Saquinavir: preparation, characterization, pharmacokinetics and biodistribution studies.
Journal of microencapsulation.
2011; 28(6):515-27. doi:
10.3109/02652048.2011.590612. [PMID: 21728760] - Alan Kennedy, Martina Hennessy, Colm Bergin, Fiona Mulcahy, Susan Hopkins, J Paul Spiers. Ribavirin and interferon alter MMP-9 abundance in vitro and in HIV-HCV-coinfected patients.
Antiviral therapy.
2011; 16(8):1237-47. doi:
10.3851/imp1867. [PMID: 22155905] - Jacek Hajda, Katharina M Rentsch, Christoph Gubler, Hans Steinert, Bruno Stieger, Karin Fattinger. Garlic extract induces intestinal P-glycoprotein, but exhibits no effect on intestinal and hepatic CYP3A4 in humans.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.
2010 Dec; 41(5):729-35. doi:
10.1016/j.ejps.2010.09.016. [PMID: 20933082] - Bilge Diker, Omar Janneh, Rolf P G van Heeswijk, Karen F T Copeland. Comparative efflux of saquinavir, ritonavir and lopinavir from primary human cells.
Drug metabolism letters.
2010 Dec; 4(4):241-5. doi:
10.2174/187231210792928297. [PMID: 20690898] - Shriram M Pathak, Prashant Musmade, Swapnil Dengle, Arumugam Karthik, Krishnamurthy Bhat, Nayanabhirama Udupa. Enhanced oral absorption of saquinavir with Methyl-Beta-Cyclodextrin-Preparation and in vitro and in vivo evaluation.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.
2010 Nov; 41(3-4):440-51. doi:
10.1016/j.ejps.2010.07.013. [PMID: 20656025] - Echeverria Patricia, Pere Domingo, Mar Gutierrez, Mateo Gracia, Monse Fuster, José Molto, Jordi Puig, Nuria Perez-Alvarez, Bonaventura Clotet, Eugenia Negredo. Saquinavir/ritonavir monotherapy as a new nucleoside-sparing maintenance strategy in long-term virologically suppressed HIV-infected patients.
Current HIV research.
2010 Sep; 8(6):467-70. doi:
10.2174/157016210793499358. [PMID: 20636275] - Gregory J Anger, Micheline Piquette-Miller. Impact of hyperlipidemia on plasma protein binding and hepatic drug transporter and metabolic enzyme regulation in a rat model of gestational diabetes.
The Journal of pharmacology and experimental therapeutics.
2010 Jul; 334(1):21-32. doi:
10.1124/jpet.110.165639. [PMID: 20348205] - Martin S Rhee, James A Hellinger, Sandy Sheble-Hall, Calvin J Cohen, David J Greenblatt. Relationship between plasma protease inhibitor concentrations and lipid elevations in HIV patients on a double-boosted protease inhibitor regimen (saquinavir/lopinavir/ritonavir).
Journal of clinical pharmacology.
2010 Apr; 50(4):392-400. doi:
10.1177/0091270009339739. [PMID: 20097936] - C Schmitt, B Kaeser, M Riek, N Bech, C Kreuzer. Effect of saquinavir/ritonavir on P-glycoprotein activity in healthy volunteers using digoxin as a probe.
International journal of clinical pharmacology and therapeutics.
2010 Mar; 48(3):192-9. doi:
10.5414/cpp48192. [PMID: 20197013] - Katja Berginc, Irina Milisav, Albin Kristl. Garlic flavonoids and organosulfur compounds: impact on the hepatic pharmacokinetics of saquinavir and darunavir.
Drug metabolism and pharmacokinetics.
2010; 25(6):521-30. doi:
10.2133/dmpk.dmpk-10-rg-053. [PMID: 20930421] - Eskild Petersen, Huiling Mu, Trine Porsgaard, Lone S Bertelsen. The protease inhibitors ritonavir and saquinavir influence lipid metabolism: a pig model for the rapid evaluation of new drugs.
Antiviral therapy.
2010; 15(2):243-51. doi:
10.3851/imp1509. [PMID: 20386080] - M Bickel, A Bodtländer, G K Knecht, C Stephan, N von Hentig, M Kurowski, P Gute, S Klauke, T Lutz. Once-daily treatment with saquinavir mesylate (2000 mg) and ritonavir (100 mg) together with a fixed-dose combination of abacavir/lamivudine (600/300 mg) or tenofovir/emtricitabine (245/200 mg) in HIV-1-infected patients.
The Journal of antimicrobial chemotherapy.
2009 Dec; 64(6):1260-4. doi:
10.1093/jac/dkp348. [PMID: 19776037] - Upal Roy, Geetika Chakravarty, Kerstin Honer Zu Bentrup, Debasis Mondal. Montelukast is a potent and durable inhibitor of multidrug resistance protein 2-mediated efflux of taxol and saquinavir.
Biological & pharmaceutical bulletin.
2009 Dec; 32(12):2002-9. doi:
10.1248/bpb.32.2002. [PMID: 19952419] - Christophe Schmitt, Carsten Hofmann, Myriam Riek, Arpna Patel, Elke Zwanziger. Effect of saquinavir-ritonavir on cytochrome P450 3A4 activity in healthy volunteers using midazolam as a probe.
Pharmacotherapy.
2009 Oct; 29(10):1175-81. doi:
10.1592/phco.29.10.1175. [PMID: 19792991] - Lisa D Coles, Insong J Lee, Hazem E Hassan, Natalie D Eddington. Distribution of saquinavir, methadone, and buprenorphine in maternal brain, placenta, and fetus during two different gestational stages of pregnancy in mice.
Journal of pharmaceutical sciences.
2009 Aug; 98(8):2832-46. doi:
10.1002/jps.21644. [PMID: 19116954] - Candice Jamois, Patrick Smith, Royce Morrison, Myriam Riek, Arpna Patel, Christophe Schmitt, Peter N Morcos, Xiaoping Zhang. Effect of saquinavir/ritonavir (1000/100 mg bid) on the pharmacokinetics of methadone in opiate-dependent HIV-negative patients on stable methadone maintenance therapy.
Addiction biology.
2009 Jul; 14(3):321-7. doi:
10.1111/j.1369-1600.2009.00158.x. [PMID: 19523046] - Roland Landman, Catherine Capitant, Diane Descamps, Corine Chazallon, Gilles Peytavin, Christine Katlama, Gilles Pialoux, Michelle Bentata, Francoise Brun-Vézinet, Jean-Pierre Aboulker, Patrick Yéni. Efficacy and safety of ritonavir-boosted dual protease inhibitor therapy in antiretroviral-naive HIV-1-infected patients: the 2IP ANRS 127 study.
The Journal of antimicrobial chemotherapy.
2009 Jul; 64(1):118-25. doi:
10.1093/jac/dkp146. [PMID: 19420019] - Jasper van der Lugt, Meena Gorowara, Anchalee Avihingsanon, David Burger, Jintanat Ananworanich, Kancharat Sringam, Stephen Kerr, Ferdinand Wit, Joep Lange, Kiat Ruxrungtham. Reducing the boosting dose of ritonavir does not affect saquinavir plasma concentrations in HIV-1-infected individuals.
AIDS (London, England).
2009 Jun; 23(9):1176-9. doi:
10.1097/qad.0b013e32832b4461. [PMID: 19451794] - Jane M Sayer, John M Louis. Interactions of different inhibitors with active-site aspartyl residues of HIV-1 protease and possible relevance to pepsin.
Proteins.
2009 May; 75(3):556-68. doi:
10.1002/prot.22271. [PMID: 18951411] - José Moltó, Josep Maria Llibre, Esteban Ribera, Carlos Mínguez, Jesús Sánchez del Río, Enric Pedrol, Gabriel Vallecillo, Samandhy Cedeño, Marta Valle, Cristina Miranda, Eugenia Negredo, Bonaventura Clotet. Saquinavir exposure in HIV-infected patients with chronic viral hepatitis.
The Journal of antimicrobial chemotherapy.
2009 May; 63(5):992-7. doi:
10.1093/jac/dkp070. [PMID: 19279052] - Sharon Walmsley, Anchalee Avihingsanon, Jihad Slim, Douglas J Ward, Kiat Ruxrungtham, Jason Brunetta, U Fritz Bredeek, Dushyantha Jayaweera, Carol Jean Guittari, Peter Larson, Malte Schutz, François Raffi. Gemini: a noninferiority study of saquinavir/ritonavir versus lopinavir/ritonavir as initial HIV-1 therapy in adults.
Journal of acquired immune deficiency syndromes (1999).
2009 Apr; 50(4):367-74. doi:
10.1097/qai.0b013e318198a815. [PMID: 19214123] - Torsak Bunupuradah, Jasper van der Lugt, Pope Kosalaraksa, Chulapan Engchanil, Pitch Boonrak, Thanyawee Puthanakit, Tawan Mengthaisong, Apicha Mahanontharit, Pagakrong Lumbiganon, Emily Tompkins, David Burger, Kiat Ruxrungtham, Jintanat Ananworanich. Safety and efficacy of a double-boosted protease inhibitor combination, saquinavir and lopinavir/ritonavir, in pretreated children at 96 weeks.
Antiviral therapy.
2009; 14(2):241-8. doi:
NULL. [PMID: 19430099] - Laure Elens, Sophie Veriter, Vincent Di Fazio, Roger Vanbinst, Daniel Boesmans, Pierre Wallemacq, Vincent Haufroid. Quantification of 8 HIV-protease inhibitors and 2 nonnucleoside reverse transcriptase inhibitors by ultra-performance liquid chromatography with diode array detection.
Clinical chemistry.
2009 Jan; 55(1):170-4. doi:
10.1373/clinchem.2008.108647. [PMID: 19028822] - Jasper van der Lugt, Angela Colbers, Jose Molto, David Hawkins, Marchina van der Ende, Martin Vogel, Christoph Wyen, Malte Schutz, Peter Koopmans, Kiat Ruxrungtham, Clemens Richter, David Burger. The pharmacokinetics, safety and efficacy of boosted saquinavir tablets in HIV type-1-infected pregnant women.
Antiviral therapy.
2009; 14(3):443-50. doi:
NULL. [PMID: 19474478] - Laura Dickinson, Marta Boffito, David J Back, Saye H Khoo, Anton L Pozniak, Peter Mugyenyi, Concepta Merry, Reshma Saskia Autar, David M Burger, Leon J Aarons. Population pharmacokinetics of ritonavir-boosted saquinavir regimens in HIV-infected individuals.
The Journal of antimicrobial chemotherapy.
2008 Dec; 62(6):1344-55. doi:
10.1093/jac/dkn399. [PMID: 18824460] - Clara Lehmann, Norma Jung, Anika Hofmann, Oliver A Cornely, Christoph Wyen, Gerd Fätkenheuer, Pia Hartmann. Nucleoside-free boosted double PI regimen: significant CD4+ T-cell recovery in patients with poor immunologic response despite virologic suppression.
Current HIV research.
2008 Nov; 6(6):555-9. doi:
10.2174/157016208786501526. [PMID: 18991621] - Michel Wagner, Emmanuel Varesio, Gérard Hopfgartner. Ultra-fast quantitation of saquinavir in human plasma by matrix-assisted laser desorption/ionization and selected reaction monitoring mode detection.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2008 Sep; 872(1-2):68-76. doi:
10.1016/j.jchromb.2008.07.009. [PMID: 18657486] - Laura Dickinson, Marta Boffito, Saye H Khoo, Malte Schutz, Leon J Aarons, Anton L Pozniak, David J Back. Pharmacokinetic analysis to assess forgiveness of boosted saquinavir regimens for missed or late dosing.
The Journal of antimicrobial chemotherapy.
2008 Jul; 62(1):161-7. doi:
10.1093/jac/dkn187. [PMID: 18467305] - Pope Kosalaraksa, Torsak Bunupuradah, Chulapan Engchanil, Pitch Boonrak, Jintana Intasan, Pagakrong Lumbiganon, David Burger, Kiat Ruxrungtham, Malte Schutz, Jintanat Ananworanich. Double boosted protease inhibitors, saquinavir, and lopinavir/ritonavir, in nucleoside pretreated children at 48 weeks.
The Pediatric infectious disease journal.
2008 Jul; 27(7):623-8. doi:
10.1097/inf.0b013e31816b4539. [PMID: 18520443] - K Singh, L Dickinson, A Chaikan, D Back, C Fletcher, A Pozniak, G Moyle, M Nelson, B Gazzard, D Herath, M Boffito. Pharmacokinetics and safety of saquinavir/ritonavir and omeprazole in HIV-infected subjects.
Clinical pharmacology and therapeutics.
2008 Jun; 83(6):867-72. doi:
10.1038/sj.clpt.6100375. [PMID: 17898705] - Helen H Usansky, Peidi Hu, Patrick J Sinko. Differential roles of P-glycoprotein, multidrug resistance-associated protein 2, and CYP3A on saquinavir oral absorption in Sprague-Dawley rats.
Drug metabolism and disposition: the biological fate of chemicals.
2008 May; 36(5):863-9. doi:
10.1124/dmd.107.017483. [PMID: 18256206] - Brendan T Griffin, Caitriona M O'Driscoll. An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
Pharmaceutical research.
2008 May; 25(5):1125-33. doi:
10.1007/s11095-007-9473-3. [PMID: 17975709] - Weerawat Manosuthi, Somnuek Sungkanuparph, Kiat Ruxrungtham, Wisit Prasithsirikul, Chatiya Athichathanabadi, Woraphot Tantisiriwat, Chureeratana Bowonwatanuwong, Nopphanath Chumpathat, Achara Chaovavanich. Plasma levels, safety, and 60-week efficacy of a once-daily double-boosted protease inhibitor regimen of atazanavir, saquinavir, and ritonavir.
Journal of acquired immune deficiency syndromes (1999).
2008 Jan; 47(1):127-9. doi:
10.1097/qai.0b013e318157b0da. [PMID: 18156994] - Nils von Hentig, Gabi Nisius, Tessa Lennemann, Pavel Khaykin, Christoph Stephan, Errol Babacan, Schlomo Staszewski, Michael Kurowski, Sebastian Harder, Annette Haberl. Pharmacokinetics, safety and efficacy of saquinavir/ ritonavir 1,000/100 mg twice daily as HIV type-1 therapy and transmission prophylaxis in pregnancy.
Antiviral therapy.
2008; 13(8):1039-46. doi:
NULL. [PMID: 19195329] - Tomasz Pawiński, Piotr Pulik, Beata Gralak, Andrzej Horban. Pharmacokinetic monitoring of HIV-1 protease inhibitors in the antiretroviral therapy.
Acta poloniae pharmaceutica.
2008 Jan; 65(1):93-100. doi:
NULL. [PMID: 18536180] - Vanitha J Sekar, Eric Lefebvre, Kris Mariën, Martine De Pauw, Tony Vangeneugden, Richard M W Hoetelmans. Pharmacokinetic interaction between darunavir and saquinavir in HIV-negative volunteers.
Therapeutic drug monitoring.
2007 Dec; 29(6):795-801. doi:
10.1097/ftd.0b013e31815d23e6. [PMID: 18043478] - P Chetchotisakd, S Anunnatsiri, P Mootsikapun, S Kiertiburanakul, T Anekthananon, C Bowonwatanuwong, B Kowadisaiburana, K Supparatpinyo, K Ruxrungtham. Efficacy and tolerability of a double boosted protease inhibitor (lopinavir + saquinavir/ritonavir) regimen in HIV-infected patients who failed treatment with nonnucleoside reverse transcriptase inhibitors.
HIV medicine.
2007 Nov; 8(8):529-35. doi:
10.1111/j.1468-1293.2007.00506.x. [PMID: 17944686] - Ulrik S Justesen, Zoe Fox, Court Pedersen, Pedro Cahn, Jan Gerstoft, Nathan Clumeck, Marcello Losso, Barry Peters, Niels Obel, Antonella Castagna, Ulrik B Dragsted, Jens D Lundgren. Pharmacokinetics of two randomized trials evaluating the safety and efficacy of indinavir, saquinavir and lopinavir in combination with low-dose ritonavir: the MaxCmin1 and 2 trials.
Basic & clinical pharmacology & toxicology.
2007 Nov; 101(5):339-44. doi:
10.1111/j.1742-7843.2007.00117.x. [PMID: 17910618] - François Raffi, Manuel Battegay, Stefano Rusconi, Milos Opravil, Gary Blick, Roy T Steigbigel, Michael Kraft, Dietmar Neubacher, John P Sabo. Combined tipranavir and enfuvirtide use associated with higher plasma tipranavir concentrations but not with increased hepatotoxicity: sub-analysis from RESIST.
AIDS (London, England).
2007 Sep; 21(14):1977-80. doi:
10.1097/qad.0b013e3282ef8600. [PMID: 17721109] - Jörn Lötsch, Sebastian Harder, Martin Stürmer, Hans-Wilhelm Doerr, Gerd Geisslinger, Schlomo Staszewski, Nils von Hentig. Association of saquinavir plasma concentrations with side effects but not with antiretroviral outcome in patients infected with protease inhibitor-susceptible human immunodeficiency virus type 1.
Antimicrobial agents and chemotherapy.
2007 Sep; 51(9):3264-72. doi:
10.1128/aac.00036-07. [PMID: 17576836] - Shriram M Pathak, A Ranjith Kumar, G Subramanian, N Udupa. Development and validation of a reversed-phase liquid chromatographic method with fluorescence detection for the study of Saquinavir pharmacokinetics in rat plasma.
Analytica chimica acta.
2007 Jul; 594(2):248-56. doi:
10.1016/j.aca.2007.05.028. [PMID: 17586122] - Alan Winston, Patrick W G Mallon, Claudette Satchell, Karen MacRae, Kenneth M Williams, Malte Schutz, Matthew Law, David A Cooper, Sean Emery. The safety, efficacy, and pharmacokinetic profile of a switch in antiretroviral therapy to saquinavir, ritonavir, and atazanavir alone for 48 weeks and a switch in the saquinavir formulation.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.
2007 Jun; 44(11):1475-83. doi:
10.1086/517507. [PMID: 17479946] - Ana Marin-Niebla, Luis Fernando Lopez-Cortes, Rosa Ruiz-Valderas, Pompeyo Viciana, Rosario Mata, Alicia Gutierrez, Rosario Pascual, Magdalena Rodriguez. Clinical and pharmacokinetic data support once-daily low-dose boosted saquinavir (1,200 milligrams saquinavir with 100 milligrams ritonavir) in treatment-naive or limited protease inhibitor-experienced human immunodeficiency virus-infected patients.
Antimicrobial agents and chemotherapy.
2007 Jun; 51(6):2035-42. doi:
10.1128/aac.01136-06. [PMID: 17371813] - J Mallolas, Jl Blanco, P Labarga, A Vergara, A Ocampo, M Sarasa, M Arnedo, Y López-Púa, J García, J Juega, A Guelar, A Terrón, D Dalmau, I García, M Zárraga, E Martínez, X Carné, T Pumarola, R Escayola, Jm Gatell. Inhibitory quotient as a prognostic factor of response to a salvage antiretroviral therapy containing ritonavir-boosted saquinavir. The CIVSA Study.
HIV medicine.
2007 May; 8(4):226-33. doi:
10.1111/j.1468-1293.2007.00464.x. [PMID: 17461850] - F Josephson, A Allqvist, M Janabi, J Sayi, E Aklillu, M Jande, M Mahindi, J Burhenne, Y Bottiger, L L Gustafsson, W E Haefeli, L Bertilsson. CYP3A5 genotype has an impact on the metabolism of the HIV protease inhibitor saquinavir.
Clinical pharmacology and therapeutics.
2007 May; 81(5):708-12. doi:
10.1038/sj.clpt.6100117. [PMID: 17329995] - D William Cameron, Stephen Becker, Martin S King, Barbara da Silva, Cheri Klein, Debbie Tokimoto, Cheryl Foit, Deborah Calhoun, Barry Bernstein, George J Hanna. Exploratory study comparing the metabolic toxicities of a lopinavir/ritonavir plus saquinavir dual protease inhibitor regimen versus a lopinavir/ritonavir plus zidovudine/lamivudine nucleoside regimen.
The Journal of antimicrobial chemotherapy.
2007 May; 59(5):957-63. doi:
10.1093/jac/dkm029. [PMID: 17350990] - Nils von Hentig, Axel Müller, Carsten Rottmann, Timo Wolf, Thomas Lutz, Stephan Klauke, Michael Kurowski, Bruno Oertel, Brenda Dauer, Sebastian Harder, Schlomo Staszewski. Pharmacokinetics of saquinavir, atazanavir, and ritonavir in a twice-daily boosted double-protease inhibitor regimen.
Antimicrobial agents and chemotherapy.
2007 Apr; 51(4):1431-9. doi:
10.1128/aac.00854-06. [PMID: 17296738] - Esteban Ribera, Carlos Azuaje, Rosa M Lopez, Pere Domingo, Adria Curran, Maria Feijoo, Leonor Pou, Paquita Sánchez, Maria Antonia Sambeat, Joan Colomer, Josep Lluis Lopez-Colomes, Manuel Crespo, Vicenç Falcó, Imma Ocaña, Albert Pahissa. Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis.
The Journal of antimicrobial chemotherapy.
2007 Apr; 59(4):690-7. doi:
10.1093/jac/dkl552. [PMID: 17307771] - Dennis R Weller, Richard C Brundage, Henry H Balfour, Heather E Vezina. An isocratic liquid chromatography method for determining HIV non-nucleoside reverse transcriptase inhibitor and protease inhibitor concentrations in human plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2007 Apr; 848(2):369-73. doi:
10.1016/j.jchromb.2006.10.022. [PMID: 17081812] - Sun Ok Choi, Naser L Rezk, Angela D M Kashuba. High-performance liquid chromatography assay for the determination of the HIV-protease inhibitor tipranavir in human plasma in combination with nine other antiretroviral medications.
Journal of pharmaceutical and biomedical analysis.
2007 Mar; 43(4):1562-7. doi:
10.1016/j.jpba.2006.11.017. [PMID: 17236737] - Sreeja Sudhakaran, Craig R Rayner, Jian Li, David C M Kong, Neil M Gude, Roger L Nation. Differential protein binding of indinavir and saquinavir in matched maternal and umbilical cord plasma.
British journal of clinical pharmacology.
2007 Mar; 63(3):315-21. doi:
10.1111/j.1365-2125.2006.02766.x. [PMID: 16981898] - Florian Föger, Krum Kafedjiiski, Herbert Hoyer, Brigitta Loretz, Andreas Bernkop-Schnürch. Enhanced transport of P-glycoprotein substrate saquinavir in presence of thiolated chitosan.
Journal of drug targeting.
2007 Feb; 15(2):132-9. doi:
10.1080/10611860601140798. [PMID: 17365284] - Jennifer R King, Thomas N Kakuda, Sunita Paul, Man Ming Tse, Edward P Acosta, Stephen L Becker. Pharmacokinetics of saquinavir with atazanavir or low-dose ritonavir administered once daily (ASPIRE I) or twice daily (ASPIRE II) in seronegative volunteers.
Journal of clinical pharmacology.
2007 Feb; 47(2):201-8. doi:
10.1177/0091270006296763. [PMID: 17244771] - C Stephan, A Carlebach, C Rottmann, A Haberl, B Dauer, N von Hentig, M Kurowski, S Staszewski. Dose reduction effective in alleviating symptoms of saquinavir toxicity.
International journal of STD & AIDS.
2007 Feb; 18(2):81-4. doi:
10.1258/095646207779949763. [PMID: 17331276] - R Verbesselt, E Van Wijngaerden, J de Hoon. Simultaneous determination of 8 HIV protease inhibitors in human plasma by isocratic high-performance liquid chromatography with combined use of UV and fluorescence detection: amprenavir, indinavir, atazanavir, ritonavir, lopinavir, saquinavir, nelfinavir and M8-nelfinavir metabolite.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2007 Jan; 845(1):51-60. doi:
10.1016/j.jchromb.2006.07.068. [PMID: 16997640] - Anne-Genevieve Marcelin, Philippe Flandre, Carmen de Mendoza, Benedicte Roquebert, Gilles Peytavin, Luisa Valer, Marc Wirden, Sarah Abbas, Christine Katlama, Vincent Soriano, Vincent Calvez. Clinical validation of saquinavir/ritonavir genotypic resistance score in protease-inhibitor-experienced patients.
Antiviral therapy.
2007; 12(2):247-52. doi:
NULL. [PMID: 17503666] - Linda A Dunn, Katherine T Andrews, James S McCarthy, Janelle M Wright, Tina S Skinner-Adams, Peter Upcroft, Jacqueline A Upcroft. The activity of protease inhibitors against Giardia duodenalis and metronidazole-resistant Trichomonas vaginalis.
International journal of antimicrobial agents.
2007 Jan; 29(1):98-102. doi:
10.1016/j.ijantimicag.2006.08.026. [PMID: 17137752] - M Mesquita, M P Guillaume, M Dratwa. First use of tamoxifen in an HIV patient with encapsulating peritoneal sclerosis.
Clinical drug investigation.
2007; 27(10):727-9. doi:
10.2165/00044011-200727100-00008. [PMID: 17803348] - Nils von Hentig, Errol Babacan, Schlomo Staszewski, Martin Stürmer, Hans W Doerr, Jörn Lötsch. Predictive factors for response to a boosted dual HIV-protease inhibitor therapy with saquinavir and lopinavir in extensively pre-treated patients.
Antiviral therapy.
2007; 12(8):1237-46. doi:
NULL. [PMID: 18240863] - Jennifer Ford, Marta Boffito, Desmond Maitland, Andrew Hill, David Back, Saye Khoo, Mark Nelson, Graeme Moyle, Brian Gazzard, Anton Pozniak. Influence of atazanavir 200 mg on the intracellular and plasma pharmacokinetics of saquinavir and ritonavir 1600/100 mg administered once daily in HIV-infected patients.
The Journal of antimicrobial chemotherapy.
2006 Nov; 58(5):1009-16. doi:
10.1093/jac/dkl379. [PMID: 16984898] - E L Mariño, V Albert, M S M Ferrer, P Modamio, C F Lastra. [Development and validation of laboratory methods for antiretroviral quantitation using HPLC].
Farmacia hospitalaria : organo oficial de expresion cientifica de la Sociedad Espanola de Farmacia Hospitalaria.
2006 Nov; 30(6):374-8. doi:
10.1016/s1130-6343(06)74009-0. [PMID: 17298195] - Vanila Faber Palmeira, Lucimar Ferreira Kneipp, Celuta Sales Alviano, André Luis Souza dos Santos. Secretory aspartyl peptidase activity from mycelia of the human fungal pathogen Fonsecaea pedrosoi: effect of HIV aspartyl proteolytic inhibitors.
Research in microbiology.
2006 Nov; 157(9):819-26. doi:
10.1016/j.resmic.2006.07.003. [PMID: 16959473] - Brian P Kearney, Anita Mathias, Angelique Mittan, John Sayre, Ramin Ebrahimi, Andrew K Cheng. Pharmacokinetics and safety of tenofovir disoproxil fumarate on coadministration with lopinavir/ritonavir.
Journal of acquired immune deficiency syndromes (1999).
2006 Nov; 43(3):278-83. doi:
10.1097/01.qai.0000243103.03265.2b. [PMID: 17079992]