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99% Pharmaceutical Raw Materials Tenofovir Used As An Anti-HIV Agent 147127-20-6
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1.Basic info:
Product Name:Tenofovir
CAS:147127-20-6
MF: C9H14N5O4P
MW:287.21
Chemical Properties:White Crystalline Powder
2.Product Description:
Antiviral drugs, Tenofovir is an acyclic nucleoside antiviral reverse transcriptase inhibitor. The active substance is Tenofovir disoproxil, while tenofovir is a prodrug that is used because of its better absorption in the gut.
Tenofovir can inhibit viral polymerase through direct competitively combine with natural deoxyribose or by insertion to terminate chain of human DNA. It is the first nucleotide analogs to treat HIV-1 infection that approved by the US Food and Drug Administration (FDA).Tenofovir is a main medicine in AIDS cocktail therapy, researches has shown that it can effectively improve the monkeys` ability on prevention of immunodeficiency virus (similar to the human AIDS virus).
Tenofovir is hardly absorbed through the gastrointestinal tract, for this reason, prodrug of Tenofovir has been developed by esterification, and then to make tenofovir fumarate ester. Tenofovir ester is water-soluble, can be rapidly absorbed and degraded into the active tenofovir, and then was metabolized to the active Tenofovir disoproxil. Tenofovir will reach the peak of plasma Concentration within 1-2 h after administration.
3.Product Usage:
When combined with food service, the bioavailability of Tenofovir can be increased by 40%. Intracellular half-life of Tenofovir disoproxil is about 10 h, it needs dosing everyday. Because Tenofovir is not a CYP-450 substrate, this may decrease the possibility of interactions with other drugs caused by CYP450. Elimination of Tenofovir is by glomerular filtration and active tubular secretion. Approximately 70% to 80% is recovered in urine as unchanged drug. Elimination half-life is approximately 17 h.
Indications: Tenofovir is indicated for the treatment of HIV, HBV infection. This product also can cooperated with other reverse transcriptase inhibitors for HIV-1 infection and hepatitis B treatment.
Every coin has two sides. Tenofovir also has some adverse effects we should notice. The most common side effects associated with Tenofovir include asthenia. Tenofovir has also been implicated in mild to moderate gastrointestinal reactions such as nausea,vomiting, diarrhea, and asthenia. Less frequent side effects include hepatotoxicity, abdominal pain, and flatulence,bloating, lactic acidosis, hepatomegaly with fatty liver, pancreatitis and so on. these adverse effects are common with the use of nucleoside analogues either separately or when combined with other drugs.
Tenofovir can also lead to metabolic system hypophosphatemia (1% incidence); fat accumulation and redistribution, including central obesity, buffalo hump, peripheral wasting, breast enlargement, Cushing syndrome.Tenofovir may cause lactic acidosis, hepatomegaly with steatosis-related and so on.At the same time, it may make nervous system: dizziness, headache.Sometimes, it may leads to respiratory system: dyspnea.Tenofovir may cause skin herpes.
