nelfinavir

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「a protease inhibitor (trade name Viracept) used in treating HIV usually in combination with other drugs」
Viracept

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/04/15 14:48:31」(JST)

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英文文献

  • Yeast cells as a tool for analysis of HIV-1 protease susceptibility to protease inhibitors, a comparative study.
  • Ravaux I, Perrin-East C, Attias C, Cottalorda J, Durant J, Dellamonica P, Gluschankof P, Stein A, Tamalet C.Author information Service des Maladies Infectieuses Hôpital de la Conception, 147 Bd Baille, 13385 Marseille Cedex 05, France. Electronic address: isabelle.ravaux@ap-hm.fr.AbstractHIV develops drug resistance at a high rate under drug selection pressure. Resistance tests are recommended to help physicians optimize antiretroviral drug therapies. For this purpose, genotypic and phenotypic tests have been developed. In order to propose a new phenotypic test that will be less laborious, expensive, and time consuming than the standard ones, a new procedure to measure HIV-1 protease susceptibility to protease inhibitor (PIs) in Saccharomyces cerevisiae yeast cells was developed. This procedure is based on HIV-1 protease expression in yeast. While the viral protein induces yeast cell death, its inhibition by PIs in the culture medium allows the cell to grow in a dose-dependent manner. In a comparative study of standard genotypic analysis vs. yeast cell-based phenotypic tests, performed on HIV-1 protease coding DNA in 17 different plasma samples from infected individuals, a clear match was found between the results obtained using the two technologies. This suggests that the yeast-based procedure is at least as accurate as standard genotypic test in defining susceptibility to protease inhibitors. This encouraging result should be the basis for large-scale validation of the new phenotypic resistance test.
  • Journal of virological methods.J Virol Methods.2014 Jan;195:180-4. doi: 10.1016/j.jviromet.2013.08.019. Epub 2013 Sep 18.
  • HIV develops drug resistance at a high rate under drug selection pressure. Resistance tests are recommended to help physicians optimize antiretroviral drug therapies. For this purpose, genotypic and phenotypic tests have been developed. In order to propose a new phenotypic test that will be less lab
  • PMID 24056262
  • Comparative analysis of ER stress response into HIV protease inhibitors: Lopinavir but not darunavir induces potent ER stress response via ROS/JNK pathway.
  • Taura M, Kariya R, Kudo E, Goto H, Iwawaki T, Amano M, Suico MA, Kai H, Mitsuya H, Okada S.Author information Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Kumamoto, 860-0811, Japan.AbstractHIV protease inhibitor (PI)-induced ER stress has been associated with adverse effects. Although it is a serious clinical problem for HIV/AIDS patients, comparative analyses of ER stress induction by clinically used PIs have rarely been done. Especially, there is no report on the differential ER stress response between lopinavir (LPV) and darunavir (DRV), although these PIs are the most clinically used PIs. We show here that LPV induces the most potent CHOP expression, ER stress marker, among the 9 Food and Drug Administration (FDA)-approved PIs in human peripheral blood mononuclear cells, several human epithelial cells, and mouse embryonic fibroblasts. LPV induced the most potent ROS production and JNK activation in 9 PIs. A comparison among the most clinically used PIs, ritonavir (RTV), LPV, and DRV, revealed that LPV potently and RTV moderately but not DRV induced ER stress via ROS-dependent JNK activation rather than proteasome inhibition. Finally, we analyzed ER stress induction in tissues of mice intraperitoneally injected with RTV, LPV, and DRV. RTV and LPV but not DRV showed ER stress induction in several mice tissues. In conclusion, we first identify LPV as the most potent ER stress inducing PI among 9 FDA-approved PIs in human cells, and although clinical verification is necessary, we show here that DRV has the advantage of less ROS and ER stress induction potential compared with LPV in vitro and in vivo.
  • Free radical biology & medicine.Free Radic Biol Med.2013 Dec;65:778-88. doi: 10.1016/j.freeradbiomed.2013.08.161. Epub 2013 Aug 20.
  • HIV protease inhibitor (PI)-induced ER stress has been associated with adverse effects. Although it is a serious clinical problem for HIV/AIDS patients, comparative analyses of ER stress induction by clinically used PIs have rarely been done. Especially, there is no report on the differential ER str
  • PMID 23973637
  • Broad-spectrum antivirals for the emerging Middle East respiratory syndrome coronavirus.
  • Chan JF, Chan KH, Kao RY, To KK, Zheng BJ, Li CP, Li PT, Dai J, Mok FK, Chen H, Hayden FG, Yuen KY.Author information State Key Laboratory of Emerging Infectious Diseases, The University of Hong Kong, Hong Kong, China; Department of Microbiology, The University of Hong Kong, Hong Kong, China; Research Centre of Infection and Immunology, The University of Hong Kong, Hong Kong, China.AbstractOBJECTIVES: Middle East respiratory syndrome coronavirus (MERS-CoV) has emerged to cause fatal infections in patients in the Middle East and traveler-associated secondary cases in Europe and Africa. Person-to-person transmission is evident in outbreaks involving household and hospital contacts. Effective antivirals are urgently needed.
  • The Journal of infection.J Infect.2013 Dec;67(6):606-16. doi: 10.1016/j.jinf.2013.09.029. Epub 2013 Oct 3.
  • OBJECTIVES: Middle East respiratory syndrome coronavirus (MERS-CoV) has emerged to cause fatal infections in patients in the Middle East and traveler-associated secondary cases in Europe and Africa. Person-to-person transmission is evident in outbreaks involving household and hospital contacts. Effe
  • PMID 24096239

和文文献

  • Pharmacokinetics of Human Immunodeficiency Virus Protease Inhibitor, Nelfinavir, in Poloxamer 407-Induced Hyperlipidemic Model Rats(Biopharmacy)
  • , , [他], ,
  • Biological & pharmaceutical bulletin 32(2), 269-275, 2009-02-01
  • … The effect of hyperlipidemia (HL) on the pharmacokinetics of nelfinavir (NFV), a human immunodeficiency virus protease inhibitor, was investigated, focusing on the change of NFV distribution in plasma using poloxamer 407-induced HL model rats (HL rats). …
  • NAID 110007042143
  • High Molecular Weight Form of Adiponectin in Antiretroviral Drug-induced Dyslipidemia in HIV-Infected Japanese Individuals Based on in vivo and in vitro Analyses
  • , , , , ,
  • Internal Medicine 48(20), 1799-1875, 2009
  • … EFV, ritonavir (RTV) and nelfinavir (NFV) inhibited the expression of adiponectin mRNA in mature 3T3-L1 and to a greater extent in pre-mature 3T3-L1. …
  • NAID 130000122185
  • Synthesis and Biological Evaluation of Novel Isopropanolamine Derivatives as Non-peptide Human Immunodeficiency Virus Protease Inhibitors
  • , , [他], , , ,
  • Chemical & pharmaceutical bulletin 56(8), 1147-1152, 2008-08-01
  • … Novel potential human immunodeficiency virus (HIV) protease inhibitors were designed by a combination of nelfinavir and amprenavir motifs. …
  • NAID 110006838323

関連リンク

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the nelfinavir (Viracept) EMA drug label. *Disclaimer: The contents of this page have not been endorsed by the EMA and are ...
nelfinavir /nel·fin·a·vir/ (nel-fin´ah-vir) an HIV protease inhibitor that causes formation of immature, noninfectious viral particles; used as the mesylate salt in the treatment of HIV infection. nel·fin·a·vir (nĕl-fĭn′ə-vîr) n. A protease-inhibiting ...

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