Tenofovir - A Wonder Drug For Covid -19 Published Sep 18, 2020 by pharmaffiliates As the coronavirus pandemic swept through major part of the world in 2020, the US Food and Drug Administration has approved antiviral drugs Ribavirin, Remdesivir, Sofosbuvir, Galidesivir, and Tenofovir as potent drugs against SARS-CoV-2 since they tightly bind to its RdRp. In this article we shall focus on anti HIV drug Tenofovir, as a latest Spanish study reveals that rates of contracting COVID-19 are lower among people with HIV taking antiretroviral therapy like Tenofovir as compared to individuals in the general population. Tenofovir which is available as Tenofovir disoproxil fumarate is a prodrug of Tenofovir which is then phosphorylated to Tenofovir diphosphate. Tenofovir diphosphate inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate, deoxyadenosine 5'-triphosphate, and by DNA chain termination. Studies and tests reveals Tenofovir is potent drug against coronavirus as well. Scientists and medicinal facility is constantly in search of a treatment against the deadly pandemic. In order to develop of drug molecule for new disease, knowledge about its impurities and its ill effects on human health shall be given immense importance. Studies reveal that there is an enormous interest in impurity profiling of drugs in pharmaceutical parlance. The presence of undesirable chemicals, even in trivial quantity may influence the efficacy and safety of the pharmaceutical products. Many Pharmacopoeias viz United States Pharmacopeia (USP), Indian Pharmacopoeia (IP), and British Pharmacopoeia (BP), European Pharmacopoeia (EU) have designed monographs to ensure minimum acceptable quality of drug substances and drug products for users. Many regulatory agencies give critical attention to the monograph included in pharmacopoeia on impurity profiling. Some of the known (Pharmacopeial) and unknown impurities (non-pharmacopeial) of Tenofovir are tabulated below. These impurities are identified, isolated, purified and characterized after enormous research. Name of Impurity Cas No. (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((propoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Isopropyl Carbonate Fumarate NA Tenofovir Alafenamide Fumarate 379270-38-9 ((Hydroxy(((1-(6-((((9-((2R)-2-((hydroxy(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-9H-purin-6-yl)amino)methyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)oxy)methyl Isopropyl Carbonate NA P-[[(1S)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]-phosphonic Acid Monoethyl Ester 1255525-18-8 Isopropyl ((S)-((((S)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate NA Isopropyl ((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-D-alaninate 2053424-82-9 DisoproxilDisoproxilDimethylcarbamoyl NA (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(methoxy)phosphoryl)oxy)methyl isopropyl Carbonate NA 4-(((Isopropoxycarbonyl)oxy)methoxy)-4-oxobut-2-enoic Acid NA (R)-(((1-(6-(Ethylamino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic Acid NA (R)-(((1-(6-Amino-3H-purin-3-yl)propan-2-yl)oxy)methyl)phosphonic Acid 1643116-24-8 Tenofovir hydrate 206184-49-8 (((1-(6-((((9-(2-(Phosphonomethoxy)propyl)-9H-purin-6-yl)amino)methyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic Acid NA ((Hydroxy((((R)-1-(6-(methyleneamino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)oxy)methyl isopropyl Carbonate 1962114-91-5 Tenofovir AlafenamideGlycosamine NA Isopropyl (phenoxy(((1-(6-((3,5,6-trihydroxy-2-oxo-4-((3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)alaninate NA (((1-(6-(Methyleneamino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic Acid NA Tenofovir - API 147127-20-6 Tenofovir - Impurity B 4121-40-8 and 1446486-33-4 Desmethyl Tenofovir Disoproxil Fumarate NA ((((((R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(ethoxy)phosphoryl)oxy)methyl Isopropyl Carbonate Fumarate NA Diethylaminocarboxymethyl POC Tenofovir (Mixture of Diastereomers) 1246812-23-6 nPOC-POC Tenofovir Fumarate (Mixture of Diastereomers) NA 6N-Hydroxymethyl Tenofovir Disoproxil 1244022-53-4 Tenofovir Disoproxil Fumarate 1422284-15-8 Isopropyl Tenofovir 1346597-36-1 9-(2-Propenyl)adenine 4121-39-5 Mono-POC Methyl Tenofovir (Mixture of Diastereomers) 1246812-16-7 Isopropyl ((S)-((((S)-1-(6-((hydroxymethyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate NA Mono-POC Ethyl Tenofovir (Mixture of Diastereomers) 1796539-92-8 ((S)-((((R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alanine NA MOC-POC Tenofovir Fumarate Salt (Mixture of Diastereomers) NA ((((((R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((methoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Isopropyl Carbonate NA Mono-POC Tenofovir (Mixture of Diastereomers) 211364-69-1 (((((1-(6-((((9-(2-((bis(((Isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-9H-purin-6-yl)amino)methyl)amino)-9H-purin-9-yl)propan-2-yl)oxy)methyl)(hydroxy)phosphoryl)oxy)methyl Isopropyl Carbonate NA Mono-POC Tenofovir 6-Isopropyl Carbamate (Mixture of Diastereomers) 1244022-56-7 Tetraisopropyl ((((((((methylenebis(azanediyl))bis(9H-purine-6,9-diyl))bis(propane-1,2-diyl))bis(oxy))bis(methylene))bis(oxo-l5-phosphanetriyl))tetrakis(oxy))tetrakis(methylene)) Tetracarbonate NA nPOC-POC Tenofovir (Mixture of Diastereomers) 1217542-13-6 rac Tenofovir 107021-12-5 Tenofovir Monomethyl Ester 1796539-83-7 Ethyl Tenofovir 1796545-19-1 Tenofovir Disoproxil Fumarate 202138-50-9 Isopropyl ((S)-((((S)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-D-alaninate NA (S)-Tenofovir Disoproxil Fumarate 1432630-26-6 Isopropyl ((S)-((((S)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-D-alaninate NA Tenofovir Phosphate, (mixture of diastereomers) 1432630-26-6 (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Ethyl Carbonate Fumarate NA Tenofovir Disoproxil Dimer 1093279-76-5 (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Diethylcarbamate Fumarate NA Tenofovir DisoproxilIsopropoxycarbonyl 1244022-54-5 (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((methoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Isopropyl Carbonate Fumarate NA Tenofovir Diphosphate Triethylamine Salt (mixture of diastereomers) NA Isopropyl (9-(2-((bis(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-9H-purin-6-yl)carbamate NA Tenofovir Dibenzyloxy Isopropyl Carbamate 1391052-09-7 P-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)-N-(1-isopropoxy-1-oxopropan-2-yl)phosphonamidic Acid NA Tenofovir Isopropyl Carbamate 1391053-20-5 ((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(hydroxy)phosphoryl)alanine NA Mono-POC Isopropyl Tenofovir (Mixture of Diastereomers) 1246812-40-7 ((Alanyloxy)(((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)alanine NA Tenofovir Alafenamide 379270-37-8 bis(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)diphosphonic Acid NA Tenofovir (S)-Isomer 147127-19-3 DEC-POC PMPA Tenofovir 1422284-17-0 MOC-POC Tenofovir 1246812-43-0 Tri-POC Tenofovir Dimer 1093279-77-6 Tenofovir Dimer Triethylammonium Salt NA Tenofovir AlafenamideHemifumarate 1392275-56-7 Tenofovir Mono POC Dimer 1962114-92-6 Desmethyl Tenofovir Disoproxil 365417-53-4 Tenofovir Disoproxil Ethyl Ester 1422284-16-9 Tenofovir Trimer Impurity 1 NA Tenofovir Trimer Impurity 2 NA Emtricitabine Tenofovir Disoproxil Dimer NA Emtricitabine Tenofovir Monosoproxil Dimer NA Tenofovir Disoproxil Fumarate Impurity(N6-CH2OH-POC PMPA) NA (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(isopropoxy)phosphoryl)oxy)methyl Isopropyl Carbonate NA [[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]monophenylester 379270-35-6 Isopropyl ((R)-((((S)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-D-alaninate NA N-[(R)-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-L-alanine 1-Methylethyl Ester 383365-04-6 Tenofovir Dimer 1607007-18-0 P-((((R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)-N-((S)-1-isopropoxy-1-oxopropan-2-yl)phosphonamidic Acid 851456-00-3 Tenofovir Diphosphate 166403-66-3 ((Tosyloxy)methyl)phosphonic Acid 161760-09-4 (bis(((Isopropoxycarbonyl)oxy)methoxy)phosphoryl)methyl 4-methylbenzenesulfonate NA Tenofovir Disoproxil 201341-05-1 Tenofovir Disoproxil (S)-Isomer 1280130-08-6 Isopropyl (((((7-((S)-2-((bis(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-7H-purin-6-yl)amino)methyl)(9-((2R)-2-((hydroxy(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-9H-purin-6-yl)amino)methyl)(9-((2S)-2-((hydroxy(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)methoxy)propyl)-9H-purin-6-yl)carbamate NA (((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(((methoxycarbonyl)oxy)methoxy)phosphoryl)oxy)methyl Isopropyl Carbonate NA ((Hydroxy((((2R)-1-(6-((hydroxymethyl)amino)-4,5-dihydro-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)oxy)methyl isopropyl Carbonate NA Fumaric Acid compound with ((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(hydroxy)phosphoryl)oxy)methyl Isopropyl Carbonate (1:1) NA The impurities shall be available for research or quality control purpose to the pharmaceutical industries so that the antiviral drug against Covid-19 is developed and manufactured in bulk and is freely available to mankind. The impurities and other research compounds shall be available with Certificate of Analysis and other supporting data required fulfilling the Regulatory requirements. Also the research compounds must be highly pure and readily available. Sourcing these research materials is a tedious task but Pharmaffiliates Analytics and synthetics P. Ltd. has made the choice easier. Pharmaffiliates fulfills all the above requirements and is a worldwide manufacturer/supplier/exporter of Reference standards, Research material and Quality products. Our accreditations include ISO 9001:2015, ISO 2001:17025, ISO Guide 34, USFDA, DSIR and Ilac. Leave a Reply
