生物活性

• 描述Tenofovir Disoproxil fumarate (TVF), an antiviral drug, is a nucleotide reverse transcriptase inhibitor approved for treating HIV and chronic Hepatitis B. Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Moreover, experiments showed that TFV induced apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage^[3]. Tenofovir Disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice^[4]. Tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil fumarate administration is safe and effective in the woodchuck model of chronic HBV infection^[5].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  human bone marrow cells	-	Cytotoxic assay	24 h	Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9 μM	20439609
  human HeLa P4/R5 cells	-	Function assay	-	Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7 μM	19596885
  human HeLa P4/R5 cells	-	Function assay	-	Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4 μM	19596885

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• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01671982	HIV	Phase 1	Completed	-	Thailand ... more >> Sanpatong Hospital Sanpatong, Chiang Mai, Thailand, 20120 HIV-NAT Bangkok, Thailand, 10330 Nakornping Hospital Chiang Mai, Thailand Chonburi Hospital Chonburi, Thailand, 20000 Phayao Hospital Phayao, Thailand, 56000 Collapse <<
  NCT01745822	Hepatitis B Chronic Infection ... more >> Pregnancy Collapse <<	Phase 3	Active, not recruiting	October 2018	Thailand ... more >> Prapokklao Hospital Chantha Buri, Chanta Buri, Thailand, 22000 Mae Chan Hospital Mae Chan, Chiangrai, Thailand, 57110 Banglamung Hospital Bang Lamung, Chon Buri, Thailand, 20150 Maharat Nakhon Ratchasima Hospital Nakhon Ratchasima, Nakhon Ratchasrima, Thailand, 30000 Chiang Kham Hospital Chiang Kham, Phayao, Thailand, 56110 Bhumibol Adulyadej Hospital Bangkok, Thailand, 10220 Nopparat Rajathanee Hospital Bangkok, Thailand, 10230 Health Promotion Center Region 10 Chiang Mai, Thailand, 50100 Nakornping Hospital Chiang Mai, Thailand, 50180 Chiangrai Prachanukroh Hospital Chiang Rai, Thailand, 57000 Chonburi Regional Hospital Chon Buri, Thailand, 20000 Khon Kaen Hospital Khon Kaen, Thailand, 40000 Lampang Hospital Lampang, Thailand, 52000 Lamphun Hospital Lamphun, Thailand, 51000 Phayao Provincial Hospital Phayao, Thailand, 56000 Samutprakarn Hospital Samut Prakan, Thailand, 10280 Samutsakhon Hospital Samut Sakhon, Thailand, 74000 Collapse <<
  NCT02174276	Chronic Hepatitis B	Phase 2	Completed	-	-

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• 参考文献

• [1] Chen JZ, Liao ZW, et al. Efficacy and safety of tenofovir disoproxil fumarate in preventing vertical transmission of hepatitis B in pregnancies with high viral load. Sci Rep. 2017 Jun 23;7(1):4132.

  [2] Birkus G, Hitchcock MJ, Cihlar T. Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.

  [3] Murphy RA, Stafford RM, Petrasovits BA, Boone MA, Valentovic MA. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3):531.

  [4] Musumeci G, Bon I, Lembo D, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017;7:41018.

  [5] Wahl A, Ho PT, Denton PW, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017;7:41098.

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