ChemicalBook CAS DataBase List 201341-05-1

201341-05-1

Name	Tenofovir disoproxil
CAS	201341-05-1
EINECS(EC#)	111-111-1
Molecular Formula	C19H30N5O10P
MDL Number	MFCD00952920
Molecular Weight	519.44
MOL File	201341-05-1.mol

Synonyms

Tdf SRY Aids080741 Aids-080741 Bis(poc)pmpa Pmpa prodrug Tenofov ir Disoprox Tenofovir disoproxil Testis-determining factor Tenofovir disoproxil, >=98% TenofivirDisoproxilFumarate Tenofovir disoproxil aspartate 202138-50-9 (1:1 Fumarate salt) Gs 4331-05 (*1:1 fumarate salt*) Tenofovirdisoproxil(Fumaratesalt) Bis(isopropyloxymethylcarbonyl)pmpa 9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine (R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)-bis(oxy))bis(methylene) d (R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)-bis(oxy))bis(methylene) diis (R)-(((((1-(6-AMino-9H-purin-9-yl)propan-2-yl)oxy)Methyl)phosphoryl)bis(oxy))bis(Methylene) diisopropyl dicarbonate 5-[[(1r)-2-(6-Amino-9h-Purin-9-Yl)-1-Methylethoxy]Methyl]-2,4,6,8-Tetraoxa-5-Phosphanononanedioic Acid Bis(1-Methylethyl) Ester 5-Oxide 2,4,6,8-Tetraoxa-5-phosphanonanedioicacid, 5-[[(1R)-2-(6-aMino-9H-purin-9-yl)-1-Methylethoxy]Methyl]-,1,9-bis(1-Methylethyl) ester, 5-oxide

Chemical Properties

Boiling point	642.7±65.0 °C(Predicted)
density	1.45±0.1 g/cm3(Predicted)
storage temp.	-20°C
solubility	DMSO: ≥ 38 mg/mL (73.16 mM)
form	Solid
pka	4.20±0.10(Predicted)
color	White to off-white
CAS DataBase Reference	201341-05-1

Hazard Information

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.

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.

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.

storage

Store at -20°C

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