Tenofovir disoproxil fumarate Raw Materials Powder 202138-50-9

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Tenofovir disoproxil fumarate Powder Usage and Synthesis.

Tenofovir disoproxil fumarate (TDF), a nucleotide reverse transcriptase inhibitor, is an orally available open-cyclic nucleotide phosphate pre-drug that is rapidly converted to tenofovir for efficacy after oral absorption.

TDF is now the recommended first-line anti-HIV drug with the highest sales due to its high bioavailability, precise efficacy and good tolerability.

Patent literature reported the synthetic method of tenofovir disoproxil fumarate, but there are some intermediates with many impurities, low optical purity, difficult operation, low yield, unqualified fumaric acid content and unsuitable for industrial production.

Uses and functions of Tenofovir disoproxil fumarate.

Nucleotide reverse transcriptase inhibitor, a prodrug of tenofovir (PMPA, 2), clinically used primarily for the treatment of human immunodeficiency virus infections.

Pharmacological Effects of Tenofovir disoproxil fumarate Raw.

Tenofovir ester is tenofovir diisopropoxymethyl fenvalerate, the ester precursor of tenofovir, an acyclic adenosine 5'-monophosphate analogue with broad-spectrum antiviral effects, inhibiting the reverse transcriptase of HIV-1 and HIV-2 and the HBV polymerase, and thus inhibiting viral replication.

After oral administration, TDF is hydrolysed to tenofovir, which is phosphorylated by cellular kinases into the pharmacologically active metabolite tenofovir diphosphate, which competes with 5'-triphosphate deoxyadenylate and participates in the synthesis of viral DNA, and enters the viral DNA and inhibits viral replication due to the blockage of DNA elongation by the lack of 3'-OH.

Production method of Bulk Tenofovir disoproxil fumarate Powder.

Tenofovir circulates via the kidney via glomerular filtration and active tubular secretion.Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2.

In MRP4 overexpressing cells, Tenofovir accumulates to five-fold lower levels and MRP inhibitors increase its accumulation.

In human hepatoblastoma (liver cancer) cells, skeletal muscle cells (SkMCs) or renal proximal tubular epithelial cells, Tenofovir did not significantly affect mitochondrial DNA (mtDNA).

In HepG2 cells or SkMCs, Tenofovir elevated lactate production by less than 20%.

In HepG2 cells and human primary hepatocytes, Tenofovir was efficiently phosphorylated by tenofovir diphosphate (TFV-DP).

In a cell-based assay, the 50% effective concentration of Tenofovir against HBV was 1.1 mM, which was increased 50-fold by the addition of the pre-bis-isoproxil moiety. In vitro and in the clinic, Tenofovir was fully active against lamivudine-resistant HBV.

Tenofovir inhibited the proliferation of hepatogenic hepatocellular carcinoma cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively.

Tenofovir had weaker effects on the proliferation and viability of renal proximal tubular epithelial cells than cidofovir, which has potentially relevant nucleotide analogue-induced renal tubular dysfunction.

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