Tenofovir Alafenamide Hemifumarate CAS 1392275-56-7

Tenofovir Alafenamide Fumarate (TAF) is a novel nucleoside reverse transcriptase inhibitor (NRTI) developed by Gilead Sciences in the United States. It is a new drug approved by the US Food and Drug Administration (FDA) for the treatment of adult chronic hepatitis B in the past decade; Pure Tenofovir alafenamide hemifumarate powder is a white to off white solid. Compared to the previous product, Tenofovir disoproxilfumarate 300mg, it only requires less than one tenth of the dosage to achieve similar antiviral effects.

What are the differences between TAF and other products?

Like Sofosbuvir, the development of Tenofovir alafenamide hemifumarate powder has brought huge wealth to Gilead. However, if we compare the differences of TAF, we need to start with its predecessors. Adefovir dipivoxil, Gilead's first hepatitis B drug (adefovir dipivoxil is a precursor product of adefovir, because of its low bioavailability, it has developed adefovir dipivoxil that is easy to be hydrolyzed by esterase). Although adefovir dipivoxil can quickly and effectively inhibit the virus, thus significantly improving liver histology, biochemistry, serology and other key indicators. However, its ability to inhibit HBV is weaker than that of lamivudine, reducing viral load by around 104 per year. If you encounter a serious hepatitis B patient, the virus may not be dropped to the undetectable level, and the body may have been unable to operate. In addition, this product has mild nephrotoxicity, and long-term use can cause permanent damage to the proximal tubules, leading to decreased reabsorption of phosphorus, increased excretion of urinary phosphorus, and continuous release of bone phosphorus into the bloodstream, resulting in bone mineralization balance disruption and decreased bone density, leading to osteomalacia.
In response to these issues, Gilead introduced tenofovir disoproxil and was approved by the FDA for anti HBV treatment in 2008. Multiple studies abroad have shown that TDF has strong anti HBV effects, low drug resistance, and is effective against CHB treated with various NAs. Its antiviral effect is very strong, and it has 8 years of zero drug resistance data. It can be said that it is an ideal drug for hepatitis B treatment with "high efficiency and low drug resistance". The only disadvantage is that long-term use may cause damage to the kidney and bone density.
And TAF is launched as an upgraded version of TDF (Tenofovir Axetil). Compared with tenofovir disoproxil fumarate 202138-50-9, TAF overcomes some of the shortcomings of TDF, and the 96 week efficacy and safety results of TAF's Phase III study show that TAF did not find drug resistance while maintaining a high viral inhibition rate. On November 10, 2016, TAF drug was approved by FDA based on the 48 week results of study108 and study110 studies to treat hepatitis B patients with compensatory liver disease.
Through the first 48 weeks of research, it was found that compared to TDF, 25mg had a significant effect on viral load, which was not inferior to 300mg. It also significantly improved laboratory parameters of the patient's bones and kidneys, and the proportion of patients with normal transaminase levels also increased.
Moreover, through the 96 week study results, the drug resistance of TAF has been well confirmed. Even under high viral inhibition rates, no drug resistance was found, and the parameters of renal function and bone density have a smaller impact. At the same time, patients who were previously treated with TDF also underwent dressing changes. After switching to TAF, no drug resistance was observed, and transaminase serum levels quickly returned to normal. Renal function and bone density also began to improve at 24 weeks.

Our company can provide you with abundant raw material support in your research career related to physical health, including but not limited to:Sofosbuvir,Adefovir,Adefovir dipivoxil,TDF,TAF and so on.If you are interested, please contact us viaemail:sales6@faithfulbio.com

Why is TAF so popular?

In fact, before TAF, there were interferon α, polyethylene glycol interferon α, and common nucleoside analogues such as lamivudine, telbivudine, entecavir, adefovir and adefovir dipivoxil for oral use, tenofovir and tenofovir dipivoxil. However, there are all kinds of defects and problems, such as: interferon has the disadvantages of high price and many adverse reactions, and oral nucleoside drugs have the problems of poor response, easy drug resistance, easy recurrence after withdrawal, accompanied by certain nephrotoxicity, decreased blood phosphorus and easy to cause osteoporosis.
According to the 96-week efficacy and safety results of the third phase study of tenofovir dipivoxil (TAF):
1. In contrast, TAF has a very high rate of return:
TAF did not find drug resistance while maintaining a high virus inhibition rate. In addition, TAF has the advantage of low dosage. Compared with TDF, TAF only needs one tenth of TDF dosage to achieve the same antiviral effect as TDF.
2. TAF has better bone safety.
Compared with the original hepatitis B drug, TAF can effectively improve the bone safety factor and reduce the risk of osteoporosis. Under normal dosage, TAF decreased hip bone density by-0.29% vs-2.16% compared with TDF. The bone mineral density of spine decreased by -0.88% vs -2.51%, and TAF can greatly slow down the bone mineral density loss of patients with hepatitis B.

3. TAF has better renal safety.

The decrease of glomerular filtration rate (eGFR) is an important index in the diagnosis of chronic kidney disease, and its decrease reflects the health status of renal function. TAF and TDF were 1.2 mL/min vs 5.4 mL/min when the ratio of eGFR (glomerular filtration rate) to baseline decreased. Moreover, we can analogize that the efficacy of using 25mg TAF can compete with that of 300mg TDF, so it is understandable that using less 275mg of the product will bring much less harm to the kidney.

In contrast, TAF has a satisfactory price.
Although this product is not listed in China at present, it is said that Mylan Company announced on December 11, 2017 that TAF officially authorized generic drugs to be listed in India, and the cost was ridiculously low. Of course, many pharmaceutical companies in China are also stepping up their scientific research, and some breakthroughs have been made.If you have purchasing needs in the pure Tenofovir Alafenamide Fumarate powder and would like to obtain a suitable price, please contact us via email:sales6@faithfulbio.com

What is the pharmacological action of TAF?

TAF is degraded into active substance tenofovir in blood, and then enters into liver cells to be converted into active metabolite tenofovir diphosphate (DP), which inhibits virus polymerase by directly and competitively combining with natural deoxyribose substrate, and inhibits reverse transcriptase by inserting the termination chain into human DNA, thereby inhibiting HIV virus replication by inhibiting the activity of HIV-1 reverse transcriptase, and further exerting anti-hepatitis B virus infection (HBV) and acquired immune syndrome.
In addition, this product not only contributes to medicine, but Tenofovir-ella phenamine fumarate raw material also can be used as a solvent in electroplating industry and a catalyst for alkylation esterification and polymerization.

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Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China,Can provide you with a good price.Our company can provide various Sofosbuvir,Adefovir,Adefovir dipivoxil,TDF,TAF,interferon α, polyethylene glycol interferon α and common nucleoside analogues etc. If you are interested, please contact us

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