1. a weak protease inhibitor (trade name Invirase) used in treating HIV (同)Invirase

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/01/01 12:57:08」(JST)

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English Journal

  • Pharmacokinetics of a multipurpose pod-intravaginal ring simultaneously delivering five drugs in an ovine model.
  • Moss JA, Malone AM, Smith TJ, Kennedy S, Nguyen C, Vincent KL, Motamedi M, Baum MM.SourceDepartment of Chemistry, Oak Crest Institute of Science, Pasadena, California, USA.
  • Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2013 Aug;57(8):3994-7. doi: 10.1128/AAC.00547-13. Epub 2013 Jun 10.
  • Multipurpose technologies that simultaneously protect from sexually transmitted infections and unintended pregnancy are urgently needed. Pod-intravaginal rings (IVRs) formulated with the antiretroviral agents (ARVs) tenofovir, nevirapine, and saquinavir and the contraceptives etonogestrel and estrad
  • PMID 23752507
  • 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.
  • Leonis G, Steinbrecher TB, Papadopoulos MG.AbstractThe emergence of HIV-1 drug-resistant mutations is the major problem against AIDS treatment. We employed molecular dynamics (MD) calculations and free energy (MM-PBSA and Thermodynamic Integration) analyses 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. Conformational analysis showed that the protease flaps are increasingly flexible in the I50V complexes. In the WT, stabilization of the HIV-1 PR structure is achieved via inter-flap and water-mediated hydrogen bonding interactions between the flaps. Furthermore, hydrogen bonds between drugs and binding cavity residues (Asp29/29'/30/30') are crucial for effective inhibition. All these interactions were significantly diminished (or absent) in the mutated forms, thus denoting their importance toward binding. Thermodynamic Integration calculations reproduced the experimental data to within ≈1 kcal mol-1 and showed that the I50V mutation results in weaker binding free energies for all analyzed complexes with respect to the WT. It was observed that the loss in binding energy upon mutation was mostly enthalpically driven in all complexes, with the greatest effect coming from the reduction of van der Waals interactions. Our results motivated us to test two novel compounds that have been synthesized to maximize interactions with HIV-1 PR. MM-PBSA and TI calculations showed that compound 3c (Ghosh et al. Bioorg. Med. Chem. Lett. 2012, 22, 2308) is a promising protease inhibitor, which presents very effective binding to the WT PR (ΔGMM-PBSA = - 17.2 kcal mol-1, ΔGexp = - 16.1 kcal mol-1), and upon I50V mutation, the complex binding free energy was weakened by a ΔΔGTI of 1.8 kcal mol-1, comparable to the marketed inhibitors. This predicts that I50V may confer low resistance to 3c. This computational comparative study contributes toward elucidation of the I50V drug-resistance mechanism in HIV-1 PR.
  • Journal of chemical information and modeling.J Chem Inf Model.2013 Jul 8. [Epub ahead of print]
  • The emergence of HIV-1 drug-resistant mutations is the major problem against AIDS treatment. We employed molecular dynamics (MD) calculations and free energy (MM-PBSA and Thermodynamic Integration) analyses on wild type (WT) and mutated HIV-1 protease (HIV-1 PR) complexes with darunavir, amprenavir,
  • PMID 23834142
  • Targeting delivery of saquinavir to the brain using 83-14 monoclonal antibody-grafted solid lipid nanoparticles.
  • Kuo YC, Ko HF.SourceDepartment of Chemical Engineering, National Chung Cheng University, Chia-Yi, Taiwan 62102, Republic of China.
  • Biomaterials.Biomaterials.2013 Jul;34(20):4818-30. doi: 10.1016/j.biomaterials.2013.03.013. Epub 2013 Mar 29.
  • 83-14 monoclonal antibody (MAb) was modified on solid lipid nanoparticles (SLNs) to improve the brain-targeting delivery of saquinavir (SQV). The endocytosis of 83-14 MAb-grafted SQV-loaded SLNs (83-14 MAb/SQV-SLNs) into human brain-microvasscular endothelial cells (HBMECs) was studied by staining c
  • PMID 23545288

Japanese Journal

  • Analysis of the Pharmacokinetic Boosting Effects of Ritonavir on Oral Bioavailability of Drugs in Mice
  • Drug Metabolism and Pharmacokinetics 28(2), 144-152, 2013
  • … The area under the plasma concentration-time curves (AUC) for orally administered saquinavir after coadministration with 50 mg/kg ritonavir dramatically increased (325-fold). … Moreover, the AUC0–12 for saquinavir was affected negligibly by itraconazole. … These results indicate ritonavir mainly affects the first-pass effect of saquinavir in the small intestine, increasing the bioavailability of orally administered saquinavir. …
  • NAID 130004933527
  • Large-Scale Quantum Chemical Calculation on the Complexes of HIV-1 Protease and Inhibitors: A Relationship of Calculation Energies with Drug Effects of Inhibitors
  • Yagi Yoichiro,Hattori Yousuke,Naoshima Yoshinobu
  • 日本シミュレーション学会論文誌 4(2), 41-50, 2012
  • … In addition, similar FMO computations on the complexes of a human protease renin with two HIV-1 protease inhibitors, Ritonavir and Saquinavir, show that the binding energy for Ritonavir with many side effects is negatively larger than that for Saquinavir with few side effects. …
  • NAID 130004544045
  • Garlic Flavonoids and Organosulfur Compounds : Impact on the Hepatic Pharmacokinetics of Saquinavir and Darunavir
  • Drug metabolism and pharmacokinetics 25(6), 521-530, 2010-12-25
  • NAID 10027743722

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Before taking saquinavir, tell your doctor and pharmacist if you are allergic to saquinavir, any other medications, or any of the ingredients in saquinavir capsules or tablets. Your doctor may tell you not to take saquinavir. Ask your ...
Drug information on Saquinavir for patients and consumers. ... Contact your health care provider right away if you have any of the following symptoms that could be signs of heart rhythm problems: Dizziness.

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Saquinavir - Wikipedia, the free Saquinavir (Invirase) | Medicamentos Saquinavir - encyclopedia article Saquinavir - Wikipedia, the free Saquinavir - Wikipedia, the free  effective protease inhibitor Saquinavir

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  • 薬の生物系に対する相互作用:薬理作用 <-化学の視点
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  • 薬物学 materia medica
  • 生薬学
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