Fosamprenavir (BioDeep_00000033320)

human metabolite blood metabolite Chemicals and Drugs

代谢物信息卡片

{[(2R,3S)-1-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid

化学式: C25H36N3O9PS (585.1909776)
中文名称: 福沙那韦
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)OP(=O)(O)O)S(=O)(=O)C3=CC=C(C=C3)N
InChI: InChI=1S/C25H36N3O9PS/c1-18(2)15-28(39(33,34)22-10-8-20(26)9-11-22)16-24(37-38(30,31)32)23(14-19-6-4-3-5-7-19)27-25(29)36-21-12-13-35-17-21/h3-11,18,21,23-24H,12-17,26H2,1-2H3,(H,27,29)(H2,30,31,32)/t21-,23-,24+/m0/s1

描述信息

Fosamprenavir is only found in individuals that have used or taken this drug. It is a prodrug of amprenavir, an inhibitor of human immunodeficiency virus (HIV) protease.Fosamprenavir is rapidly hydrolyzed to amprenavir by cellular phosphatases in the gut epithelium as it is absorbed. Amprenavir is an inhibitor of HIV-1 protease. During HIV replication, HIV protease cleaves viral polypeptide products of the Gag and Gag-Pol genes to form structural proteins of the virion core and essential viral enzymes. Amprenavir interferes with this process by binding to the active site of HIV-1 protease, thereby preventing the processing of viral Gag and Gag-Pol polyprotein precursors, resulting in the formation of immature non-infectious viral particles.
J - Antiinfectives for systemic use > J05 - Antivirals for systemic use > J05A - Direct acting antivirals > J05AE - Protease inhibitors
D000890 - Anti-Infective Agents > D000998 - Antiviral Agents > D000084762 - Viral Protease Inhibitors
D000890 - Anti-Infective Agents > D000998 - Antiviral Agents > D044966 - Anti-Retroviral Agents
C471 - Enzyme Inhibitor > C783 - Protease Inhibitor > C97366 - HIV Protease Inhibitor
C254 - Anti-Infective Agent > C281 - Antiviral Agent > C1660 - Anti-HIV Agent
D004791 - Enzyme Inhibitors > D011480 - Protease Inhibitors

同义名列表

9 个代谢物同义名

{[(2R,3S)-1-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid; (3-(((4-Aminophenyl)sulfonyl)(2-methylpropyl)amino)-1-(phenylmethyl)-2-(phosphonooxy)propyl)carbamic acid C-(tetrahydro-3-furanyl) ester; Fosamprenavir calcium; Fos-amprenavir; fosamprenavir; GW908 CPD; VX175 CPD; FOS-apv; Lexiva

数据库引用编号

10 个数据库交叉引用编号

ChEBI: CHEBI:82941
KEGG: C12723
PubChem: 131536
HMDB: HMDB0015416
DrugBank: DB01319
ChEMBL: CHEMBL1664
Wikipedia: Fosamprenavir
chemspider: 116245
CAS: 1257693-05-2
CAS: 226700-79-4

分类词条

Aminobenzenesulfonamides

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

9606 - Homo sapiens: -

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

Ahizechukwu C Eke, Jiajia Wang, Khadija Amin, David E Shapiro, Alice Stek, Elizabeth Smith, Nahida Chakhtoura, Michael Basar, Kathleen George, Katherine M Knapp, Esaú C João, Kittipong Rungruengthanakit, Edmund Capparelli, Sandra Burchett, Mark Mirochnick, Brookie M Best. Fosamprenavir with Ritonavir Pharmacokinetics during Pregnancy. Antimicrobial agents and chemotherapy. 2020 03; 64(4):. doi: 10.1128/aac.02260-19. [PMID: 32015036]
Akiko Fukuda, Takako Nagao, Tomomi Kitaichi, Ichiro Koga, Akihiro Kobayashi, Toshiyuki Miura. Safety analysis of Lexiva tablets 700 (fosamprenavir calcium hydrate) in post-marketing surveillance in Japan. Current medical research and opinion. 2020 03; 36(3):455-464. doi: 10.1080/03007995.2019.1700495. [PMID: 31794279]
Marlies Braeckmans, Joachim Brouwers, Imke Masuy, Cécile Servais, Jan Tack, Patrick Augustijns. The influence of gastric motility on the intraluminal behavior of fosamprenavir. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2020 Jan; 142(?):105117. doi: 10.1016/j.ejps.2019.105117. [PMID: 31682976]
Murugaiah A M Subbaiah, Sandhya Mandlekar, Sridhar Desikan, Thangeswaran Ramar, Lakshumanan Subramani, Mathiazhagan Annadurai, Salil D Desai, Sarmistha Sinha, Susan M Jenkins, Mark R Krystal, Murali Subramanian, Srikanth Sridhar, Shweta Padmanabhan, Priyadeep Bhutani, Rambabu Arla, Shashyendra Singh, Jaydeep Sinha, Megha Thakur, John F Kadow, Nicholas A Meanwell. Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. Journal of medicinal chemistry. 2019 04; 62(7):3553-3574. doi: 10.1021/acs.jmedchem.9b00002. [PMID: 30938524]
Ivy Song, Julie Borland, Shuguang Chen, Amanda Peppercorn, Toshihiro Wajima, Stephen C Piscitelli. Effect of fosamprenavir-ritonavir on the pharmacokinetics of dolutegravir in healthy subjects. Antimicrobial agents and chemotherapy. 2014 Nov; 58(11):6696-700. doi: 10.1128/aac.03282-14. [PMID: 25155604]
April M Barbour, Leonid Gibiansky, Mary Beth Wire. Population pharmacokinetic modeling and simulation of amprenavir following fosamprenavir/ritonavir administration for dose optimization in HIV infected pediatric patients. Journal of clinical pharmacology. 2014 Feb; 54(2):206-14. doi: 10.1002/jcph.205. [PMID: 25272370]
Mark Cotton, Haseena Cassim, Noris Pavía-Ruz, Harmony P Garges, Teodora Perger, Susan L Ford, Mary Beth Wire, Naomi Givens, Lisa L Ross, Yu Lou, Jörg Sievers, Katharine Cheng. Pharmacokinetics, safety and antiviral activity of fosamprenavir/ritonavir-containing regimens in HIV-infected children aged 4 weeks to 2 years-48-week study data. The Pediatric infectious disease journal. 2014 Jan; 33(1):57-62. doi: 10.1097/inf.0b013e3182a1123a. [PMID: 23811743]
Claudia Fortuny, Dan Duiculescu, Katharine Cheng, Harmony P Garges, Mark Cotton, Desamparados Pérez Tamarirt, Susan L Ford, Mary Beth Wire, Naomi Givens, Lisa L Ross, Yu Lou, Teodora Perger, Jörg Sievers. Pharmacokinetics and 48-week safety and antiviral activity of fosamprenavir-containing regimens in HIV-infected 2- to 18-year-old children. The Pediatric infectious disease journal. 2014 Jan; 33(1):50-6. doi: 10.1097/inf.0b013e3182a1126a. [PMID: 23811744]
Manoli Vourvahis, Anna Plotka, Laure Mendes da Costa, Annie Fang, Jayvant Heera. Pharmacokinetic interaction between maraviroc and fosamprenavir-ritonavir: an open-label, fixed-sequence study in healthy subjects. Antimicrobial agents and chemotherapy. 2013 Dec; 57(12):6158-64. doi: 10.1128/aac.01098-13. [PMID: 24080663]
Robin Wood, Joseph C Gathe, Naomi Givens, Sangeeta Sedani, Katharine Cheng, Jörg Sievers. Long-term safety study of fosamprenavir-containing regimens in HIV-1-infected patients. HIV clinical trials. 2013 Sep; 14(5):183-91. doi: 10.1310/hct1405-183. [PMID: 24144895]
Princy Kumar, Edwin DeJesus, Gregory Huhn, Louis Sloan, Catherine Butkus Small, Howard Edelstein, Franco Felizarta, Ritche Hao, Lisa Ross, Britt Stancil, Keith Pappa, Belinda Ha. Evaluation of cardiovascular biomarkers in a randomized trial of fosamprenavir/ritonavir vs. efavirenz with abacavir/lamivudine in underrepresented, antiretroviral-naïve, HIV-infected patients (SUPPORT): 96-week results. BMC infectious diseases. 2013 Jun; 13(?):269. doi: 10.1186/1471-2334-13-269. [PMID: 23741991]
Claudio Ucciferri, Katia Falasca, Francesca Vignale, Marta Di Nicola, Eligio Pizzigallo, Jacopo Vecchiet. Improved metabolic profile after switch to darunavir/ritonavir in HIV positive patients previously on protease inhibitor therapy. Journal of medical virology. 2013 May; 85(5):755-9. doi: 10.1002/jmv.23543. [PMID: 23508901]
Michelle S Cespedes, Delivette Castor, Susan L Ford, Doreen Lee, Yu Lou, Gary E Pakes, Judith A Aberg. Steady-state pharmacokinetics, cord blood concentrations, and safety of ritonavir-boosted fosamprenavir in pregnancy. Journal of acquired immune deficiency syndromes (1999). 2013 Apr; 62(5):550-4. doi: 10.1097/qai.0b013e318285d918. [PMID: 23314414]
José L Casado, Ignacio de Los Santos, María Del Palacio, Lucio García-Fraile, María J Pérez-Elías, Jesús Sanz, Santiago Moreno. Lipid-lowering effect and efficacy after switching to etravirine in HIV-infected patients with intolerance to suppressive HAART. HIV clinical trials. 2013 Jan; 14(1):1-9. doi: 10.1310/hct1401-1. [PMID: 23372109]
A Degli Antoni, L E Weimer, R Manfredi, V Fragola, C Ferrari. A reduced grade of liver fibro-steatosis after raltegravir, maraviroc and fosamprenavir in an HIV/HCV co-infected patient with chronic hepatitis, cardiomyopathy, intolerance to nelfinavir and a marked increase of serum creatine phosphokinase levels probably related to integrase inhibitor use. The West Indian medical journal. 2012 Dec; 61(9):932-6. doi: 10.7727/wimj.2011.194. [PMID: 24020238]
L Gallelli, O Staltari, C Palleria, G Di Mizio, G De Sarro, B Caroleo. A case of adverse drug reaction induced by dispensing error. Journal of forensic and legal medicine. 2012 Nov; 19(8):497-8. doi: 10.1016/j.jflm.2012.04.026. [PMID: 23084317]
Stefano Rusconi, Vania Giacomet, Chiara Mameli, Alessandra Viganò, Ottavia Viganò, Fulvio Adorni, Massimo Galli, Gian Vincenzo Zuccotti. Efficacy and safety of a dual boosted protease inhibitor-based regimen, atazanavir and fosamprenavir/ritonavir, against HIV: experience in a pediatric population. BMC infectious diseases. 2012 Aug; 12(?):179. doi: 10.1186/1471-2334-12-179. [PMID: 22866946]
Valerie A Gruber, Petrie M Rainey, David E Moody, Gene D Morse, Qing Ma, Sudha Prathikanti, Patricia A Pade, Anika A H Alvanzo, Elinore F McCance-Katz. Interactions between buprenorphine and the protease inhibitors darunavir-ritonavir and fosamprenavir-ritonavir. Clinical infectious diseases : an official publication of the Infectious Diseases Society of America. 2012 Feb; 54(3):414-23. doi: 10.1093/cid/cir799. [PMID: 22100576]
Yu Ming Paul Lam, Kristin L McBride, Janaki Amin, Damien V Cordery, Anthony D Kelleher, David A Cooper, Kersten K Koelsch. Switching virally suppressed, treatment-experienced patients to a raltegravir-containing regimen does not alter levels of HIV-1 DNA. PloS one. 2012; 7(3):e31990. doi: 10.1371/journal.pone.0031990. [PMID: 22396745]
José R Santos, José Moltó, Josep M Llibre, Eugenia Negredo, Isabel Bravo, Arelly Ornelas, Bonaventura Clotet, Roger Paredes. Antiretroviral simplification with darunavir/ritonavir monotherapy in routine clinical practice: safety, effectiveness, and impact on lipid profile. PloS one. 2012; 7(5):e37442. doi: 10.1371/journal.pone.0037442. [PMID: 22666357]
Vincenzo Esposito, Paolo Chiodini, Rosaria Viglietti, Roberto Parrella, Giovanni Parrella, Adelaide Maddaloni, Vincenzo Sangiovanni, Miriam Gargiulo, Nicola Abrescia, Antonio Chirianni. Safety of fosamprenavir in a cohort of HIV-1-infected patients with co-morbidities. In vivo (Athens, Greece). 2011 Sep; 25(5):813-9. doi: NULL. [PMID: 21753139]
M Saumoy, Jm Tiraboschi, M Gutierrez, J Niubó, P Domingo, A Vila, D Podzamczer. Viral response in stable patients switching to fosamprenavir/ritonavir monotherapy (the FONT Study). HIV medicine. 2011 Aug; 12(7):438-41. doi: 10.1111/j.1468-1293.2010.00898.x. [PMID: 21729229]
Sainath Gaddam, Lata Pablani, Vinod Chainani, Ravi Raj Kavuda, Tarun Nagrani, Georges Abou Rjaili, Meekoo Dhar, James C Lafferty. Complete recovery of ischemic cardiomyopathy from thrombotic thrombocytopenic purpura. Clinical Medicine Insights. Cardiology. 2011 Mar; 5(?):29-33. doi: 10.4137/cmc.s6130. [PMID: 21487455]
Luke C Swenson, Graham Pollock, Brian Wynhoven, Theresa Mo, Winnie Dong, Robert S Hogg, Julio S G Montaner, P Richard Harrigan. 'Dynamic range' of inferred phenotypic HIV drug resistance values in clinical practice. PloS one. 2011 Feb; 6(2):e17402. doi: 10.1371/journal.pone.0017402. [PMID: 21390218]
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]
Theodoros Kelesidis, Otto O Yang, Judith S Currier, Kaveh Navab, Alan M Fogelman, Mohamad Navab. HIV-1 infected patients with suppressed plasma viremia on treatment have pro-inflammatory HDL. Lipids in health and disease. 2011 Feb; 10(?):35. doi: 10.1186/1476-511x-10-35. [PMID: 21345230]
Jacques Gasnault, Dominique Costagliola, Houria Hendel-Chavez, Anne Dulioust, Sophie Pakianather, Anne-Aurélie Mazet, Marie-Ghislaine de Goer de Herve, Rémi Lancar, Anne-Sophie Lascaux, Lydie Porte, Jean-François Delfraissy, Yassine Taoufik. Improved survival of HIV-1-infected patients with progressive multifocal leukoencephalopathy receiving early 5-drug combination antiretroviral therapy. PloS one. 2011; 6(6):e20967. doi: 10.1371/journal.pone.0020967. [PMID: 21738597]
Takeshi Nishijima, Hirokazu Komatsu, Hiroyuki Gatanaga, Takahiro Aoki, Koji Watanabe, Ei Kinai, Haruhito Honda, Junko Tanuma, Hirohisa Yazaki, Kunihisa Tsukada, Miwako Honda, Katsuji Teruya, Yoshimi Kikuchi, Shinichi Oka. Impact of small body weight on tenofovir-associated renal dysfunction in HIV-infected patients: a retrospective cohort study of Japanese patients. PloS one. 2011; 6(7):e22661. doi: 10.1371/journal.pone.0022661. [PMID: 21799928]
C Stephan, H Jaeger, A Carganico, G Knecht, T Lutz, C Mayr, F A Mosthaf, S Koeppe, M Mueller, E Wolf, A Tappe, E Wellmann, H Knechten. Safety and efficacy after switch to a saquinavir-containing antiretroviral regimen in protease inhibitor pretreated HIV-positive patients. European journal of medical research. 2010 Sep; 15(9):369-76. doi: 10.1186/2047-783x-15-9-369. [PMID: 20952345]
Rama Mallipeddi, Lisa Cencia Rohan. Progress in antiretroviral drug delivery using nanotechnology. International journal of nanomedicine. 2010 Aug; 5(?):533-47. doi: 10.2147/ijn.s7681. [PMID: 20957115]
Mehmet Gumustas, Sibel A Ozkan. Electrochemical evaluation and determination of antiretroviral drug fosamprenavir using boron-doped diamond and glassy carbon electrodes. Analytical and bioanalytical chemistry. 2010 May; 397(1):189-203. doi: 10.1007/s00216-009-3334-3. [PMID: 19998025]
A D Luber, D V Condoluci, P D Slowinski, M Andrews, K Olson, C A Peloquin, K A Pappa, G E Pakes. Steady-state amprenavir and tenofovir pharmacokinetics after coadministration of unboosted or ritonavir-boosted fosamprenavir with tenofovir disoproxil fumarate in healthy volunteers. HIV medicine. 2010 Mar; 11(3):193-9. doi: 10.1111/j.1468-1293.2009.00765.x. [PMID: 19863619]
Paul A Randell, Akil G Jackson, Marta Boffito, David J Back, John F Tjia, Jessica Taylor, Sundhiya Mandalia, Graeme J Moyle. Effect of boosted fosamprenavir or lopinavir-based combinations on whole-body insulin sensitivity and lipids in treatment-naive HIV-type-1-positive men. Antiviral therapy. 2010; 15(8):1125-32. doi: 10.3851/imp1675. [PMID: 21149919]
María J Pérez-Elías, María Larrousse Morellon, Enrique Ortega, José Hernández-Quero, Maribel Rodríguez-Torres, Bonaventura Clotet, Franco Felizarta, Felix Gutiérrez, Juan A Pineda, Garrett Nichols, Yu Lou, Mary Beth Wire. Pharmacokinetics of fosamprenavir plus ritonavir in human immunodeficiency virus type 1-infected adult subjects with hepatic impairment. Antimicrobial agents and chemotherapy. 2009 Dec; 53(12):5185-96. doi: 10.1128/aac.00632-09. [PMID: 19667283]
Andrew Hill, Jasper van der Lugt, Will Sawyer, Marta Boffito. How much ritonavir is needed to boost protease inhibitors? Systematic review of 17 dose-ranging pharmacokinetic trials. AIDS (London, England). 2009 Nov; 23(17):2237-45. doi: 10.1097/qad.0b013e328332c3a5. [PMID: 19809270]
Carosi, Lazzarin, Stellbrink, Moyle, Rugina, Staszewski, Givens, Ross, Granier, Ait-Khaled, Leather, Nichols. Study of once-daily versus twice-daily fosamprenavir plus ritonavir administered with abacavir/lamivudine once daily in antiretroviral-naïve HIV-1-infected adult subjects. HIV clinical trials. 2009 Nov; 10(6):356-67. doi: 10.1310/hct1006-356. [PMID: 20133266]
Josep M Llibre. First-line boosted protease inhibitor-based regimens in treatment-naive HIV-1-infected patients--making a good thing better. AIDS reviews. 2009 Oct; 11(4):215-22. doi: . [PMID: 19940948]
Valerio Tozzi, Pietro Balestra, Maria Flora Salvatori, Chrysoula Vlassi, Giuseppina Liuzzi, Maria Letizia Giancola, Marinella Giulianelli, Pasquale Narciso, Andrea Antinori. Changes in cognition during antiretroviral therapy: comparison of 2 different ranking systems to measure antiretroviral drug efficacy on HIV-associated neurocognitive disorders. Journal of acquired immune deficiency syndromes (1999). 2009 Sep; 52(1):56-63. doi: 10.1097/qai.0b013e3181af83d6. [PMID: 19731418]
Jean-Michel Molina, Mounir Ait-Khaled, Roberto Rinaldi, Giovanni Penco, Jean-Guy Baril, Roberto Cauda, Vicente Soriano, Gilles Pialoux, Mary Beth Wire, Yu Lou, Naomi Givens, Charles Craig, W Garrett Nichols, Inês Barbosa, Jane Yeo. Fosamprenavir/ritonavir in advanced HIV disease (TRIAD): a randomized study of high-dose, dual-boosted or standard dose fosamprenavir/ritonavir in HIV-1-infected patients with antiretroviral resistance. The Journal of antimicrobial chemotherapy. 2009 Aug; 64(2):398-410. doi: 10.1093/jac/dkp198. [PMID: 19515730]
Marypeace McRae, Patrick G Clay, Peter L Anderson, Alan G Glaros. Pharmacokinetics of concurrent administration of fosamprenavir and atazanavir without ritonavir in human immunodeficiency virus-negative subjects. Pharmacotherapy. 2009 Aug; 29(8):937-42. doi: 10.1592/phco.29.8.937. [PMID: 19637947]
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]
Thuy Le, Jennifer Chiarella, Birgitte B Simen, Bozena Hanczaruk, Michael Egholm, Marie L Landry, Kevin Dieckhaus, Marc I Rosen, Michael J Kozal. Low-abundance HIV drug-resistant viral variants in treatment-experienced persons correlate with historical antiretroviral use. PloS one. 2009 Jun; 4(6):e6079. doi: 10.1371/journal.pone.0006079. [PMID: 19562031]
Laura Dickinson, Marta Boffito, David Back, Laura Waters, Laura Else, Geraint Davies, Saye Khoo, Anton Pozniak, Leon Aarons. Population pharmacokinetics of ritonavir-boosted atazanavir in HIV-infected patients and healthy volunteers. The Journal of antimicrobial chemotherapy. 2009 Jun; 63(6):1233-43. doi: 10.1093/jac/dkp102. [PMID: 19329800]
David A Parks, H Clay Jennings, Christopher Taylor, Gary E Pakes, Edward P Acosta. Steady-state amprenavir, tenofovir, and emtricitabine pharmacokinetics before and after reducing ritonavir boosting of a fosamprenavir/tenofovir/emtricitabine regimen from 200 mg to 100 mg once daily (TELEX II). HIV clinical trials. 2009 May; 10(3):160-7. doi: 10.1310/hct1003-160. [PMID: 19632955]
Belinda Ha, Qiming M Liao, Lynn P Dix, Keith A Pappa. Virologic response and safety of the abacavir/lamivudine fixed-dose formulation as part of highly active antiretroviral therapy: analyses of six clinical studies. HIV clinical trials. 2009 Mar; 10(2):65-75. doi: 10.1310/hct1002-65. [PMID: 19487176]
Francesca Gatti, Paola Nasta, Arianna Loregian, Massimo Puoti, Alessandro Matti, Silvana Pagni, Daniel Gonzalez de Requena, Katiela Prestini, Saverio G Parisi, Stefano Bonora, Giorgio Palù, Giampiero Carosi. Unboosted fosamprenavir is associated with low drug exposure in HIV-infected patients with mild-moderate liver impairment resulting from HCV-related cirrhosis. The Journal of antimicrobial chemotherapy. 2009 Mar; 63(3):575-8. doi: 10.1093/jac/dkn525. [PMID: 19151039]
Emanuela Lattuada, Massimiliano Lanzafame, Carmela Grosso, Fabio Soldani, Fabiana Corsini, Silvia Storato, Sandro Vento. Optimal fosamprenavir regimen to prevent lipid abnormalities. Acta bio-medica : Atenei Parmensis. 2009; 80(3):200-2. doi: NULL. [PMID: 20578411]
Antonella Mandas, Eugenio Luigi Iorio, Maria Gabriella Congiu, Cinzia Balestrieri, Antonello Mereu, Daniela Cau, Sandra Dessì, Nicoletta Curreli. Oxidative imbalance in HIV-1 infected patients treated with antiretroviral therapy. Journal of biomedicine & biotechnology. 2009; 2009(?):749575. doi: 10.1155/2009/749575. [PMID: 19884983]
Linda Wittkop, Daniel Commenges, Isabelle Pellegrin, Dominique Breilh, Didier Neau, Denis Lacoste, Jean-Luc Pellegrin, Geneviève Chêne, François Dabis, Rodolphe Thiébaut. Alternative methods to analyse the impact of HIV mutations on virological response to antiviral therapy. BMC medical research methodology. 2008 Oct; 8(?):68. doi: 10.1186/1471-2288-8-68. [PMID: 18945369]
Juan A Pineda, Maria-Jesús Pérez-Elías, José M Peña, Isabel Luque, Felipe Rodríguez-Alcantara. Low rate of adverse hepatic events associated with fosamprenavir/ritonavir-based antiretroviral regimens. HIV clinical trials. 2008 Sep; 9(5):309-13. doi: 10.1310/hct0905-309. [PMID: 18977719]
Ying-Jun Cao, Patrick F Smith, Mary Beth Wire, Yu Lou, Charles T Lancaster, Roger C Causon, George E Bigelow, Elizabeth Martinez, Edward J Fuchs, Christine Radebaugh, Sarah McCabe, Craig W Hendrix. Pharmacokinetics and pharmacodynamics of methadone enantiomers after coadministration with fosamprenavir-ritonavir in opioid-dependent subjects. Pharmacotherapy. 2008 Jul; 28(7):863-74. doi: 10.1592/phco.28.7.863. [PMID: 18576901]
B Masquelier, K L Assoumou, D Descamps, L Bocket, J Cottalorda, A Ruffault, A G Marcelin, L Morand-Joubert, C Tamalet, C Charpentier, G Peytavin, Z Antoun, F Brun-Vézinet, D Costagliola. Clinically validated mutation scores for HIV-1 resistance to fosamprenavir/ritonavir. The Journal of antimicrobial chemotherapy. 2008 Jun; 61(6):1362-8. doi: 10.1093/jac/dkn127. [PMID: 18390885]
Anthony J Busti, Amy M Bain, Ronald G Hall, Roger G Bedimo, Richard D Leff, Claudia Meek, Reza Mehvar. Effects of atazanavir/ritonavir or fosamprenavir/ritonavir on the pharmacokinetics of rosuvastatin. Journal of cardiovascular pharmacology. 2008 Jun; 51(6):605-10. doi: 10.1097/fjc.0b013e31817b5b5a. [PMID: 18520949]
Olga Delgado, Melchor Riera, Javier Murillas, Pere Ventayol. [Plasma levels following the switch from amprenavir to fosamprenavir in HIV-infected patients under antiretroviral treatment with lopinavir/ritonavir]. Enfermedades infecciosas y microbiologia clinica. 2008 Mar; 26(3):182-3. doi: 10.1157/13116760. [PMID: 18358222]
Susan L Ford, Ya-Chi Chen, Yu Lou, Julie Borland, Sherene S Min, Geoffrey J Yuen, Mark J Shelton. Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects. Antimicrobial agents and chemotherapy. 2008 Feb; 52(2):534-8. doi: 10.1128/aac.00724-07. [PMID: 18056271]
Eric Dailly, François Raffi, Charlotte Biron, C Allavena, P Jolliet. Impact of nevirapine or efavirenz co-administration on ritonavir-boosted amprenavir pharmacokinetics in HIV-infected patients. Fundamental & clinical pharmacology. 2008 Feb; 22(1):101-4. doi: 10.1111/j.1472-8206.2007.00556.x. [PMID: 18251726]
Hassane Izzedine, Isabelle Brocheriou, Marc-Antoine Valantin, Laurent Camous, Edward Bourry, Alain Baumelou, Gilbert Deray, Christine Katlama. A case of acute renal failure associated with diffuse infiltrative lymphocytosis syndrome. Nature clinical practice. Nephrology. 2008 Feb; 4(2):110-4. doi: 10.1038/ncpneph0674. [PMID: 18227804]
Ighovwerha Ofotokun, Edward P Acosta, Jeffrey L Lennox, Yi Pan, Kirk A Easley. Pharmacokinetics of an indinavir-ritonavir-fosamprenavir regimen in patients with human immunodeficiency virus. Pharmacotherapy. 2008 Jan; 28(1):74-81. doi: 10.1592/phco.28.1.74. [PMID: 18154477]
Ronald W Falcon, Thomas N Kakuda. Drug interactions between HIV protease inhibitors and acid-reducing agents. Clinical pharmacokinetics. 2008; 47(2):75-89. doi: 10.2165/00003088-200847020-00001. [PMID: 18193914]
J William Critchfield, Delandy H Young, Timothy L Hayes, Jerome V Braun, Juan C Garcia, Richard B Pollard, Barbara L Shacklett. Magnitude and complexity of rectal mucosa HIV-1-specific CD8+ T-cell responses during chronic infection reflect clinical status. PloS one. 2008; 3(10):e3577. doi: 10.1371/journal.pone.0003577. [PMID: 18974782]
Manon J van der Lee, Audrey A M Blenke, Gerard A Rongen, Corrien P W G M Verwey-van Wissen, Peter P Koopmans, Cristina Pharo, David M Burger. Interaction study of the combined use of paroxetine and fosamprenavir-ritonavir in healthy subjects. Antimicrobial agents and chemotherapy. 2007 Nov; 51(11):4098-104. doi: 10.1128/aac.01243-06. [PMID: 17846135]
Elena Seminari, Anna De Bona, Gianluca Gentilini, Laura Galli, Giulia Schira, Nicola Gianotti, Caterina Uberti-Foppa, Armando Soldarini, Fernanda Dorigatti, Adriano Lazzarin, Antonella Castagna. Amprenavir and ritonavir plasma concentrations in HIV-infected patients treated with fosamprenavir/ritonavir with various degrees of liver impairment. The Journal of antimicrobial chemotherapy. 2007 Oct; 60(4):831-6. doi: 10.1093/jac/dkm282. [PMID: 17684056]
Leah Tong, Truc K Phan, Kelly L Robinson, Darius Babusis, Robert Strab, Siddhartha Bhoopathy, Ismael J Hidalgo, Gerald R Rhodes, Adrian S Ray. Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. Antimicrobial agents and chemotherapy. 2007 Oct; 51(10):3498-504. doi: 10.1128/aac.00671-07. [PMID: 17664327]
Joachim Brouwers, Jan Tack, Patrick Augustijns. Parallel monitoring of plasma and intraluminal drug concentrations in man after oral administration of fosamprenavir in the fasted and fed state. Pharmaceutical research. 2007 Oct; 24(10):1862-9. doi: 10.1007/s11095-007-9307-3. [PMID: 17443397]
A D Luber, R Brower, D Kim, R Silverman, C A Peloquin, I Frank. Steady-state pharmacokinetics of once-daily fosamprenavir/ritonavir and atazanavir/ritonavir alone and in combination with 20 mg omeprazole in healthy volunteers. HIV medicine. 2007 Oct; 8(7):457-64. doi: 10.1111/j.1468-1293.2007.00496.x. [PMID: 17760738]
Erica Bastiani, Fabio Benedetti, Federico Berti, Pietro Campaner, Elena Donadel, Michela Montagna, Mario Regazzi, Serena Rinaldi, Adriano Savoini, Romina Venturini. Development and evaluation of an immunoassay for the monitoring of the anti-HIV drug amprenavir. Journal of immunological methods. 2007 Aug; 325(1-2):35-41. doi: 10.1016/j.jim.2007.05.009. [PMID: 17597142]
Mary B Wire, Charles H Ballow, Julie Borland, Mark J Shelton, Yu Lou, Geoffrey Yuen, Jiang Lin, Eric W Lewis. Fosamprenavir plus ritonavir increases plasma ketoconazole and ritonavir exposure, while amprenavir exposure remains unchanged. Antimicrobial agents and chemotherapy. 2007 Aug; 51(8):2982-4. doi: 10.1128/aac.00008-07. [PMID: 17517848]
Isabelle Pellegrin, Dominique Breilh, Gaelle Coureau, Sébastien Boucher, Didier Neau, Patrick Merel, Denis Lacoste, Hervé Fleury, Marie-Claude Saux, Jean-Luc Pellegrin, Estibaliz Lazaro, François Dabis, Rodolphe Thiébaut. Interpretation of genotype and pharmacokinetics for resistance to fosamprenavir-ritonavir-based regimens in antiretroviral-experienced patients. Antimicrobial agents and chemotherapy. 2007 Apr; 51(4):1473-80. doi: 10.1128/aac.00481-06. [PMID: 17296739]
Peter J Ruane, Andrew D Luber, Mary Beth Wire, Yu Lou, Mark J Shelton, C Tracey Lancaster, Keith A Pappa. Plasma amprenavir pharmacokinetics and tolerability following administration of 1,400 milligrams of fosamprenavir once daily in combination with either 100 or 200 milligrams of ritonavir in healthy volunteers. Antimicrobial agents and chemotherapy. 2007 Feb; 51(2):560-5. doi: 10.1128/aac.00560-06. [PMID: 17088488]
Paul A Pham, Craig W Hendrix, Patricia Barditch-Crovo, Teresa Parsons, Wasif Khan, Michelle Parish, Christine Radebaugh, Kathryn A Carson, Gary E Pakes, Roula Qaqish, Charles Flexner. Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or fosamprenavir with lopinavir/ritonavir, with or without efavirenz. Antiviral therapy. 2007; 12(6):963-9. doi: . [PMID: 17926651]
Edwin DeJesus, Peter J Piliero, Kim Summers, Mary Beth Wire, Daniel S Stein, Amanda Masterman, Yu Lou, Sherene S Min, Mark J Shelton. Interaction between fosamprenavir, with and without ritonavir, and nevirapine in human immunodeficiency virus-infected subjects. Antimicrobial agents and chemotherapy. 2006 Sep; 50(9):3157-9. doi: 10.1128/aac.00093-06. [PMID: 16940117]
Frank J Piacenti. An update and review of antiretroviral therapy. Pharmacotherapy. 2006 Aug; 26(8):1111-33. doi: 10.1592/phco.26.8.1111. [PMID: 16863488]
Joseph C Gathe, Robin Wood, Ian Sanne, Edwin DeJesus, Dirk Schürmann, Andrzej Gladysz, Cindy Garris, Naomi Givens, Robert Elston, Jane Yeo. Long-term (120-Week) antiviral efficacy and tolerability of fosamprenavir/ritonavir once daily in therapy-naive patients with HIV-1 infection: an uncontrolled, open-label, single-arm follow-on study. Clinical therapeutics. 2006 May; 28(5):745-54. doi: 10.1016/j.clinthera.2006.05.011. [PMID: 16861096]
Mark J Shelton, Susan L Ford, Julie Borland, Yu Lou, Mary B Wire, Sherene S Min, Zhengyu G Xue, Geoffrey Yuen. Coadministration of esomeprazole with fosamprenavir has no impact on steady-state plasma amprenavir pharmacokinetics. Journal of acquired immune deficiency syndromes (1999). 2006 May; 42(1):61-7. doi: 10.1097/01.qai.0000219770.97303.43. [PMID: 16639341]
Mary B Wire, Katherine L Baker, Lori S Jones, Mark J Shelton, Yu Lou, Greg J Thomas, M Michelle Berrey. Ritonavir increases plasma amprenavir (APV) exposure to a similar extent when coadministered with either fosamprenavir or APV. Antimicrobial agents and chemotherapy. 2006 Apr; 50(4):1578-80. doi: 10.1128/aac.50.4.1578-1580.2006. [PMID: 16569890]
Jennifer J Kiser, Kenneth A Lichtenstein, Peter L Anderson, Courtney V Fletcher. Effects of esomeprazole on the pharmacokinetics of atazanavir and fosamprenavir in a patient with human immunodeficiency virus infection. Pharmacotherapy. 2006 Apr; 26(4):511-4. doi: 10.1592/phco.26.4.511. [PMID: 16553510]
Mark J Shelton, Mary Beth Wire, Yu Lou, Brigette Adamkiewicz, Sherene S Min. Pharmacokinetic and safety evaluation of high-dose combinations of fosamprenavir and ritonavir. Antimicrobial agents and chemotherapy. 2006 Mar; 50(3):928-34. doi: 10.1128/aac.50.3.928-934.2006. [PMID: 16495253]
Bente Magny Bergersen. Cardiovascular risk in patients with HIV Infection: impact of antiretroviral therapy. Drugs. 2006; 66(15):1971-87. doi: 10.2165/00003495-200666150-00006. [PMID: 17100407]
Mary Beth Wire, Mark J Shelton, Scott Studenberg. Fosamprenavir : clinical pharmacokinetics and drug interactions of the amprenavir prodrug. Clinical pharmacokinetics. 2006; 45(2):137-68. doi: 10.2165/00003088-200645020-00002. [PMID: 16485915]
Romina Quercia, Elisabeth Garnier, Virginie Ferré, Pascale Morineau, Bénédicte Bonnet, Claire Soulard, François Raffi. Salvage therapy with ritonavir-boosted amprenavir/fosamprenavir: virological and immunological response in two years follow-up. HIV clinical trials. 2005 Mar; 6(2):73-80. doi: 10.1310/mv8b-2ybd-gam7-ptxx. [PMID: 15983891]
Angela Dm Kashuba, Camlin Tierney, Gerald F Downey, Edward P Acosta, Emanuel N Vergis, Karin Klingman, John W Mellors, Susan H Eshleman, Trevor R Scott, Ann C Collier. Combining fosamprenavir with lopinavir/ritonavir substantially reduces amprenavir and lopinavir exposure: ACTG protocol A5143 results. AIDS (London, England). 2005 Jan; 19(2):145-52. doi: 10.1097/00002030-200501280-00006. [PMID: 15668539]
Philip H Keiser, Michael G Sension, Edwin DeJesus, Allan Rodriguez, Jeffrey F Olliffe, Vanessa C Williams, John H Wakeford, Jerry W Snidow, Anne D Shachoy-Clark, Julie W Fleming, Gary E Pakes, Jaime E Hernandez. Substituting abacavir for hyperlipidemia-associated protease inhibitors in HAART regimens improves fasting lipid profiles, maintains virologic suppression, and simplifies treatment. BMC infectious diseases. 2005 Jan; 5(?):2. doi: 10.1186/1471-2334-5-2. [PMID: 15647105]
Cédric Arvieux, Olivier Tribut. Amprenavir or fosamprenavir plus ritonavir in HIV infection: pharmacology, efficacy and tolerability profile. Drugs. 2005; 65(5):633-59. doi: 10.2165/00003495-200565050-00005. [PMID: 15748098]
Susan L Ford, Mary B Wire, Yu Lou, Katherine L Baker, Daniel S Stein. Effect of antacids and ranitidine on the single-dose pharmacokinetics of fosamprenavir. Antimicrobial agents and chemotherapy. 2005 Jan; 49(1):467-9. doi: 10.1128/aac.49.1.467-469.2005. [PMID: 15616339]
Ed Wilkins. Pharmacokinetics of Telzir (fosamprenavir). Journal of HIV therapy. 2004 Nov; 9(4):87-91. doi: . [PMID: 15731740]
Marta Boffito, Laura Dickinson, Andrew Hill, David Back, Graeme Moyle, Mark Nelson, Chris Higgs, Carl Fletcher, Brian Gazzard, Anton Pozniak. Steady-State pharmacokinetics of saquinavir hard-gel/ritonavir/fosamprenavir in HIV-1-infected patients. Journal of acquired immune deficiency syndromes (1999). 2004 Nov; 37(3):1376-84. doi: 10.1097/01.qai.0000136060.65716.1a. [PMID: 15483467]
Stephen Becker, Lorna Thornton. Fosamprenavir: advancing HIV protease inhibitor treatment options. Expert opinion on pharmacotherapy. 2004 Sep; 5(9):1995-2005. doi: 10.1517/14656566.5.9.1995. [PMID: 15330736]
Joseph C Gathe, Prudence Ive, Robin Wood, Dirk Schürmann, Nicholaos C Bellos, Edwin DeJesus, Andrzej Gladysz, Cindy Garris, Jane Yeo. SOLO: 48-week efficacy and safety comparison of once-daily fosamprenavir /ritonavir versus twice-daily nelfinavir in naive HIV-1-infected patients. AIDS (London, England). 2004 Jul; 18(11):1529-37. doi: 10.1097/01.aids.0000131332.30548.92. [PMID: 15238771]
Mary Beth Wire, Charles Ballow, Sandra L Preston, Craig W Hendrix, Peter J Piliero, Yu Lou, Daniel S Stein. Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers. AIDS (London, England). 2004 Apr; 18(6):897-907. doi: 10.1097/00002030-200404090-00007. [PMID: 15060437]
Mark Mirochnick, Edmund Capparelli. Pharmacokinetics of antiretrovirals in pregnant women. Clinical pharmacokinetics. 2004; 43(15):1071-87. doi: 10.2165/00003088-200443150-00002. [PMID: 15568888]
Robin Wood, Keikawus Arasteh, Hans-Jürgen Stellbrink, Eugenio Teofilo, François Raffi, Richard B Pollard, Joseph Eron, Jane Yeo, Judith Millard, Mary Beth Wire, Odin J Naderer. Six-week randomized controlled trial to compare the tolerabilities, pharmacokinetics, and antiviral activities of GW433908 and amprenavir in human immunodeficiency virus type 1-infected patients. Antimicrobial agents and chemotherapy. 2004 Jan; 48(1):116-23. doi: 10.1128/aac.48.1.116-123.2004. [PMID: 14693528]
Amalia Rodriguez-French, Jack Boghossian, Glenda E Gray, Jeffrey P Nadler, Arnaldo R Quinones, Gladys E Sepulveda, Judith M Millard, Paul G Wannamaker. The NEAT study: a 48-week open-label study to compare the antiviral efficacy and safety of GW433908 versus nelfinavir in antiretroviral therapy-naive HIV-1-infected patients. Journal of acquired immune deficiency syndromes (1999). 2004 Jan; 35(1):22-32. doi: 10.1097/00126334-200401010-00003. [PMID: 14707788]
Jeffrey Nadler. New anti-HIV protease inhibitors provide more treatment options. AIDS patient care and STDs. 2003 Nov; 17(11):551-64. doi: 10.1089/108729103322555944. [PMID: 14746663]
Pierre Vierling, Jacques Greiner. Prodrugs of HIV protease inhibitors. Current pharmaceutical design. 2003; 9(22):1755-70. doi: 10.2174/1381612033454441. [PMID: 12871195]
Naumann I Chaudry, Joseph J Eron, Odin J Naderer, Arlene S Pereira, M B Wire, Susan A Fiscus, Angela D M Kashuba. Effects of formulation and dosing strategy on amprenavir concentrations in the seminal plasma of human immunodeficiency virus type 1-infected men. Clinical infectious diseases : an official publication of the Infectious Diseases Society of America. 2002 Sep; 35(6):760-2. doi: 10.1086/342389. [PMID: 12203175]
Christine Falcoz, Julian M Jenkins, Carole Bye, Timothy C Hardman, Kathy B Kenney, Scott Studenberg, H Fuder, William T Prince. Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. Journal of clinical pharmacology. 2002 Aug; 42(8):887-98. doi: 10.1177/009127002401102803. [PMID: 12162471]