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Tenofovir CAS: 147127-20-6
13.4 mg/mL (25℃)
Tenofovir is a kind of Acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor. Used as an anti-HIV agent. Antiviral.
Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC 50 = 1.5 μ M). Antiviral agent.
Nucleoside antiviral medicine are synthetic nucleotide analogs, the chemical has the advantages of simple structure, easy modification and synthesis is the fastest development of antiviral medicine, have developed a series of new high efficiency and low toxicity nucleoside analogs antiviral medicine have been used or will be used in HIV infection and HBV infection treatment. Nucleoside analogues from the drug structure types can be divided into two major categories of purine and pyrimidine, according to the drug action is divided for anti reverse transcriptase (RT) virus medicine, anti hepatitis virus medicine, anti herpes virus medicine and anti other antiviral medicine such as.
Tenofovir is a non cyclic nucleoside antiviral medicine, has the role of inhibition of HBV multi enzyme poly and HIV reverse transcriptase, for active ingredient tenofovir tenofovir bisphosphonates can through direct competition with natural DNA substrate combination and inhibit the viral polymerase and through in the human DNA chain termination. Is the first of the U.S. Food and Drug Administration (FDA) approved the use of HIV-1 infection in the treatment of nucleotide analogs.
Tenofovir is hardly absorbed from the gastrointestinal tract, therefore, esterification into salt, as tenofovir disoproxil fumarate. For Nuo Fuwei, the water soluble, can be quickly absorbed and degraded into active substances for Nuo Fuwei, and then for Nuo Fuwei again into active metabolites for Nuo Fuwei double phosphate. After administration of 1 ~ 2H tenofovir reached peak plasma. Tenofovir and food service when the bioavailability can be increased by about 40%. Tenofovir bisphosphonates intracellular half-life of about 10h, 1 days can be administered 1 times. Since the drug is not in the CYP450 enzyme system, the possibility of interaction with othermedicine is very small. The drug was excreted in the glomerular filtration and active tubular transport system. The drug was excreted in urine from 70% to 80%.
For the treatment of HBV, HIV infection. The product and other reverse transcriptase inhibitors are used for the treatment of HIV-1 infection and hepatitis B.
1. body weakness.
2. tenofovir common adverse reactions are mild to moderate gastrointestinal reaction, including diarrhea, abdominal pain, nausea, vomiting, stomach, lactic acid acidosis, hepatomegaly with fatty liver and pancreatitis, these adverse reactions in either alone or in combination with the use of nucleoside analogues often appear.
3. the metabolic system of low phosphate blood disease (1% incidence); fat accumulation and redistribution, including central obesity, buffalo back, distal end weight loss, breast augmentation, the pool of Xing syndrome.
4. may cause lactic acidosis associated with fatty degeneration, hepatomegaly etc..
5. nervous system: dizziness, headache.
6. respiratory system: breathing difficulties.
7. skin: drug eruption.
Category: Antibiotic Drugs API