201341-05-1 Usage
Description
Different sources of media describe the Description of 201341-05-1 differently. You can refer to the following data:
1. Tenofovir disoproxil belongs to a class of medications called antiretroviral known as a nucleotide reverse transcriptase inhibitor, which is commonly used to treat the infection caused by the human immunodeficiency virus (HIV) generally in combination with other antiviral agents. It can also be used for prevention of HIV/AIDS among those people who are at high risk before exposure, such as injection through sexual transmission or injection of drugs. It functions by blocking reverse transcriptase, an enzyme vital to viral duplication in people infected HIV. Besides, it is effective to treat chronic hepatitis B, in which it helps prevent the enzymes needed for the hepatitis B virus to reproduce from working properly. However, tenofovir disoproxil does not cure HIV/AIDS or hepatitis B. It helps lower the amount of HIV or hepatitis B virus in the body and slow down the progression of the disease. Tenofovir was patented in 1996 and approved for use in the United States in 2001.
2. Tenofovir disoproxil is a prodrug in a manner similar to that of adefovir dipivoxil. In both cases, the phosphate esters are removed through the action of plasma esterase, leading in this case to tenofovir, which differs from adefovir by the presence of the indicated methyl group. Tenofovir disoproxil exhibits good bioavailability (25%), which is improved in the presence of food (35%). The drug is approved for the treatment of HIV infections in adult patients. Tenofovir diphosphate is an HIV RT inhibitor. The active form of tenofovir is the tenofovir diphosphate, which competes with dATP for incorporation into viral DNA, and when incorporated, tenofovir diphosphate results in premature termination of DNA growth and inhibition of DNA polymerase. Tenofovir disoproxil is indicated for treatment-experienced patients with HIV-1. The drug also appears to be effective in treatment-naive patients, but initial approval is for treatment-experienced patients. The drug is administered as one tablet taken once daily. It is recommended that the drug be combined with other RT inhibitors or HIV PIs, which results in additive or synergistic activity.
References
https://en.wikipedia.org/wiki/Tenofovir_disoproxil
http://bodyandhealth.canada.com/drug/getdrug/viread
https://www.drugbank.ca/drugs/DB00300
Uses
Tenofovir Disoproxil is a therapeutic option for nucleos(t)ide analog (NA)-experienced chronic hepatitis B (CHB) patients infected with hepatitis B virus (HBV). Also, it is an intermediate used in the synthesis of Tenofovir Disoproxil Dimer (T018515), which is a Tenofovir Disoproxil impurity.
Definition
ChEBI: An organic phosphonate that is the disoproxil ester of tenofovir. A prodrug for tenofovir, an HIV-1 reverse transcriptase inhibitor, tenofovir disoproxil is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.
General Description
Tenofovir disoproxil is a prodrug analogously with abacavir.Plasma and tissue esterases cleave the phosphateprotecting groups, releasing the active drug. The bioavailabilityof tenofovir is about 35% when administered withfood. The drug is approved by the Food and DrugAdministration (FDA) for the treatment of HIV infectionsin adult patients. Recommendations are for the drug to beadministered with other RT inhibitors or PIs to achievesynergism.
Clinical Use
Nucleoside reverse transcriptase inhibitor:
Treatment of HIV in combination with other
antiretroviral drugs
Treatment of hepatitis B in compensated liver
disease
Drug interactions
Potentially hazardous interactions with other drugs
Antivirals: avoid with adefovir and cidofovir; reduces
concentration of atazanavir, also concentration of
tenofovir possibly increased; increased didanosine
concentration resulting in increased toxicity
(e.g. pancreatitis and lactic acidosis) - avoid;
concentration increased by lopinavir and telaprevir.
Co-administration with other drugs that are actively
secreted via the tubular anionic transporter.
Orlistat: absorption possibly reduced by orlistat.
Metabolism
Tenofovir is excreted mainly in the urine by both active
tubular secretion and glomerular filtration.
Check Digit Verification of cas no
The CAS Registry Mumber 201341-05-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,1,3,4 and 1 respectively; the second part has 2 digits, 0 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 201341-05:
(8*2)+(7*0)+(6*1)+(5*3)+(4*4)+(3*1)+(2*0)+(1*5)=61
61 % 10 = 1
So 201341-05-1 is a valid CAS Registry Number.
InChI:InChI=1/C19H30N5O10P/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22)/t14-/m1/s1
201341-05-1Relevant articles and documents
Green synthesis improvement of tenofovir disoproxil
Wang, Gang,Xie, Yong Mei,Wang, Xing Hua
, p. S255 - S258 (2014)
Polyethylene glycol, known as 'Green Chemical', is a catalyst for the synthesis of tenofovir disoproxil. Some technological parameters were discussed by adoptting via single-factor experiments. Through the catalytic reaction, not only tenofovir disoproxil yield was improved but also by-products was reduced obviously. The results showed that the optimal conditions were as follows: 0.6 equiv PEG-600, 4.0 equiv triethylamine, 6.0 equiv N-methyl-2-pyrrolidone and temperature at 50°C for 16 h with a yield of 65.12 %.
METHODS FOR IMPROVING PURITY OF TENOFOVIR DISOPROXIL FUMARATE, AND COMPOSITIONS THEREOF
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Paragraph 0188; 0196; 0198; 0200; 0202; 0204; 0206, (2020/07/16)
Methods for producing tenofovir disoproxil fumarate with improved purity are provided. In particular, methods for producing tenofovir disoproxil fumarate with reduced levels of chloromethyl isopropyl carbonate are described. Also described are compositions containing tenofovir disoproxil fumarate with improved purity, and an analysis method that can be used to determine the purity of such compositions with improved accuracy and sensitivity.
Amorphous semi-tenoforvirdisoproxilfumarate tablet and preparation method thereof
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Paragraph 0054; 0057-0058, (2019/11/12)
The invention relates to the technical field of medicine and discloses an amorphous semi-tenoforvirdisoproxilfumarate tablet and a preparation method thereof. The amorphous semi-tenoforvirdisoproxilfumarate tablet is prepared from, by weight, 35-60 parts of amorphous semi-tenoforvirdisoproxilfumarate, 30-60 parts of a filler, 2-10 parts of a disintegrating agent, 3-8 parts of a binding agent and 0.1-2 parts of a lubricating agent. The amorphous semi-tenoforvirdisoproxilfumarate is taken as the raw material drug, and the tablet obtained on the basis of not adopting special auxiliary materials and equipment has good stability and is not easy to degrade; wet particles are dried through a fluidized bed, and high efficiency, simple operation and good particle fluidity are achieved; the entire process is good in stability, and related substances, crystal forms and the like do not change and are good in stability in the long-term storage process; simple process and good economic benefit are achieved.
