GS-7340 hemifumarate

作者:摄影门户

配置参数

  • 类型:三脚架
  • 最低工作高度:390mm
  • 最高工作高度:1480mm
  • 最大负荷:60Kg
  • 三脚架类型:三脚架
  • 其他性能:GS-h110液压云台+GS-110PRO双级碳纤三角架

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"目录号: HY-15232A

"目录号: HY-15232B

Anti-infection-

Anti-infection-

GS-7340(Tenofovir alafenamide)是抗病毒药物替诺福韦(Tenofovir)的前体药物,相比TFV disoproxil fumarate,GS-7340能更好的将TFV送达淋巴细胞和组织。

GS-7340 (Tenofovir alafenamide) hemifumarate 是 Tenofovir (TFV) 的前体,Tenofovir (TFV) 是一种HIV-1核苷酸逆转录酶抑制剂。

HIVReverse Transcriptase

HIVReverse Transcriptase

相关产品

相关产品

Dolutegravir-Maraviroc-Elvitegravir-Atazanavir sulfate-Tenofovir Disoproxil Fumarate-Tipranavir-Triciribine-Emtricitabine-Efavirenz-Miltefosine-Ritonavir-Delavirdine mesylate-Lamivudine-Abacavir-BI 224436-

Dolutegravir-Maraviroc-Elvitegravir-Atazanavir sulfate-Tenofovir Disoproxil Fumarate-Tipranavir-Triciribine-Emtricitabine-Efavirenz-Miltefosine-Ritonavir-Delavirdine mesylate-Lamivudine-Abacavir-BI 224436-

生物活性

生物活性

Description

Description

GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.IC50 value:Target: NRTI; HIV reverse transcriptase inhibitorGS-7340 reduces first-pass clearance to be an effective oral prodrug, its permeability and stability were characterized in vitro and detailed pharmacokinetic studies were completed in dogs. GS-7340 showed concentration-dependent permeability through monolayers of caco-2 cells and dose-dependent oral bioavailability in dogs, increasing from 1.7% at 2 mg/kg to 24.7% at 20 mg/kg, suggesting saturable intestinal efflux transport [1]. Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg [2].

GS-7340 (Tenofovir alafenamide) hemifumarate is an investigational oral prodrug of theHIV-1nucleotide reverse transcriptase inhibitor Tenofovir (TFV).

Clinical Trial

IC50& Target

NCT01671787

HIV-1, NRTIs[1];)

Gilead Sciences

In Vitro

Chronic Hepatitis B

Tenofovir disoproxil fumarate (TDF) serves as a control for CatA-independent prodrug activation. Baseline antiviral activities (mean EC50±standard deviation) obtained in the absence of a protease inhibitors (PI) are determined from 6 independent donors for GS-7340 (EC50=5.3±1.2 nM) and TDF (EC50=2.8±1.1 nM) and are used to calculate fold change EC50s from four independent donors under conditions of PI pretreatment[1];). GS-7340 antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50of 3.5 nM compared to a mean EC50of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT[2];).

March 2012

In Vivo

Phase 1

GS-7340 is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF)[1];).

NCT02357602

References

University of North Carolina, Chapel Hill-Gilead Sciences

[1].Birkus G, et al. Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors. Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22.

Healthy

[2].Callebaut C, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2015 Oct;59(10):5909-16.

March 2015

Phase 1

NCT02957994

Asian Pacific Liver Center at St. Vincent Medical Center

Hepatitis B

December 22, 2016

Phase 4

NCT00042289

National Institute of Allergy and Infectious Diseases (NIAID)-Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)

HIV Infections

March 2003

Phase 4

NCT02957864

Erasmus Medical Center-Gilead Sciences

Renal Insufficiency,Chronic-Hiv-Therapeutic Agent Toxicity

October 2016

Phase 4

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