Tenofovir exalidex - CAS 911208-73-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a highly potent prodrug of the antiviral tenofovir, appeared safe and well-tolerated in patients with hepatitis B, according to a presentation at The Liver Meeting 2017. Tenofovir exalidex results in decreased circulating levels, lowering systemic exposure and thereby reducing the potential for renal and bone side effects.
White to off-white solid powder
3-(hexadecyloxy)propyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate; Tenofovir exalidex; HDP-Tenofovir; Tenofovir; CMX-157; CMX157; CMX 157
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
706.9±70.0 °C at 760 Torr
1.18±0.1 g/cm3
Canonical SMILES:
1.Alkoxyalkyl prodrugs of acyclic nucleoside phosphonates enhance oral antiviral activity and reduce toxicity: current state of the art.
Hostetler KY Antiviral Res. 2009 May;82(2):A84-98.
Although the acyclic nucleoside phosphonates cidofovir, adefovir and tenofovir are approved for treating human cytomegalovirus, hepatitis B and HIV infections, respectively, their utility is limited by low oral bioavailability, renal toxicity and poor cell penetration. Research over the past decade has shown that these undesirable features can be eliminated by esterifying the compounds with an alkoxyalkyl group, in effect disguising them as lysophospholipids. In this modified form, the drugs are readily taken up in the gastrointestinal tract and have a prolonged circulation time in plasma. The active metabolite also has a long half life within cells, permitting infrequent dosing. Because these modified drugs are not recognized by the transport mechanisms that cause the accumulation of acyclic nucleoside phosphonates in renal tubular cells, they lack nephrotoxicity. Alkoxyalkyl esterification also markedly increases the in vitro antiviral activity of acyclic nucleoside phosphonates by improving their delivery into cells. For example, an alkoxyalkyl ester of cyclic-cidofovir, a less soluble compound, retains anti-CMV activity for 3 months following a single intravitreal injection. Two of these novel compounds, hexadecyloxypropyl-cidofovir (CMX001) and hexadecyloxypropyl-tenofovir (CMX157) are now in clinical development.
2.The antiretroviral drug pipeline: prospects and implications for future treatment research.
Flexner C;Saag M Curr Opin HIV AIDS. 2013 Nov;8(6):572-8. doi: 10.1097/COH.0000000000000011.
PURPOSE OF REVIEW: ;A number of investigational antiretroviral drugs in clinical development could alter the future treatment landscape for resource-limited settings and contribute to optimized therapy for HIV infection.;RECENT FINDINGS: ;Several nucleoside reverse transcriptase inhibitors (NRTIs) are in development, including festinavir (BMS-986001), a thymidine analogue similar to stavudine but with reduced potential for toxicity, CMX-157, a hexadecyloxypropyl conjugate of tenofovir and tenofovir alafenamide (GS-7340), a prodrug of tenofovir achieving much higher intracellular triphosphate concentrations with a lower dose than tenofovir disoproxil fumarate. MK-1439 is a well tolerated once-daily non-NRTI (NNRTI) with activity against most NNRTI-associated resistance mutations. Albuvirtide is a long-acting parenteral fusion inhibitor related to enfuvirtide, and BMS-663068 is an oral HIV attachment/entry inhibitor. Ibalizumab (formerly TNX-355) is an mAb that binds to CD4 and lowers HIV plasma viral RNA in infected patients. Cenicriviroc is a CCR5-antagonist that also has activity against the inflammatory chemokine CCR2. The integrase strand transfer inhibitor (InSTI) dolutegravir was recently approved in the U.
3.Validation and implementation of liquid chromatographic-mass spectrometric (LC-MS) methods for the quantification of tenofovir prodrugs.
Hummert P;Parsons TL;Ensign LM;Hoang T;Marzinke MA J Pharm Biomed Anal. 2018 Apr 15;152:248-256. doi: 10.1016/j.jpba.2018.02.011. Epub 2018 Feb 8.
BACKGROUND: ;The nucleotide reverse transcriptase inhibitor tenofovir (TFV) is widely administered in a disoproxil prodrug form (tenofovir disoproxil fumarate, TDF) for HIV management and prevention. Recently, novel prodrugs tenofovir alafenamide fumarate (TAF) and hexadecyloxypropyl tenofovir (CMX157) have been pursued for HIV treatment while minimizing adverse effects associated with systemic TFV exposure. Dynamic and sensitive bioanalytical tools are required to characterize the pharmacokinetics of these prodrugs in systemic circulation. Two parallel methods have been developed, one to combinatorially quantify TAF and TFV, and a second method for CMX157 quantification, in plasma.;METHODS: ;K;2;EDTA plasma was spiked with TAF and TFV, or CMX157. Following the addition of isotopically labeled internal standards and sample extraction via solid phase extraction (TAF and TFV) or protein precipitation (CMX157), samples were subjected to liquid chromatographic-tandem mass spectrometric (LC-MS/MS) analysis. For TAF and TFV, separation occurred using a Zorbax Eclipse Plus C18 Narrow Bore RR, 2.1 × 50 mm, 3.5 μm column and analytes were detected on an API5000 mass analyzer; CMX157 was separated using a Kinetex C8, 2.
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CAS 911208-73-6 Tenofovir exalidex

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