ArticleAntimicrobial agents and chemotherapy2010
Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed, 47 citations in OpenAlex.
- Next-Generation Lipid Prodrugs Orally Deliver Tenofovir via Enhanced Chylomicron Incorporation.ACS pharmacology & translational science · 2025Article
- The Application of Prodrugs as a Tool to Enhance the Properties of Nucleoside Reverse Transcriptase Inhibitors.Viruses · 2023Review
- Hypo-osmolar rectal douche tenofovir formulation prevents simian/human immunodeficiency virus acquisition in macaques.JCI insight · 2022Article
- HPLC-Based Purification and Isolation of Potent Anti-HIV and Latency Reversing Daphnane Diterpenes from the Medicinal PlantViruses · 2022Article
- Inhibitors of HIV-1 Nef-Mediated Activation of the Myeloid Src-Family Kinase Hck Block HIV-1 Replication in Macrophages and Disrupt MHC-I Downregulation.ACS infectious diseases · 2022Article
- Investigational drugs with dual activity against HBV and HIV (Review).Experimental and therapeutic medicine · 2021Review
- Hepatitis B: Current Status of Therapy and Future Therapies.Gastroenterology clinics of North America · 2020Review
- Overview of Biologically Active Nucleoside Phosphonates.Frontiers in chemistry · 2020Review
- Phosphonate prodrugs: an overview and recent advances.Future medicinal chemistry · 2019Review
- Development of rectal enema as microbicide (DREAM): Preclinical progressive selection of a tenofovir prodrug enema.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2019Article
- Validation and implementation of liquid chromatographic-mass spectrometric (LC-MS) methods for the quantification of tenofovir prodrugs.Journal of pharmaceutical and biomedical analysis · 2018Article
- β-D-2'-C-Methyl-2,6-diaminopurine Ribonucleoside Phosphoramidates are Potent and Selective Inhibitors of Hepatitis C Virus (HCV) and Are Bioconverted Intracellularly to Bioactive 2,6-Diaminopurine and Guanosine 5'-Triphosphate Forms.Journal of medicinal chemistry · 2015Article
- Investigational reverse transcriptase inhibitors for the treatment of HIV.Expert opinion on investigational drugs · 2015Review
- Structure-activity relationships of a novel capsid targeted inhibitor of HIV-1 replication.Journal of chemical information and modeling · 2014Article
- Evaluation of PD 404,182 as an anti-HIV and anti-herpes simplex virus microbicide.Antimicrobial agents and chemotherapy · 2014Article
- Update on tenofovir toxicity in the kidney.Pediatric nephrology (Berlin, Germany) · 2013Review
- Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases.Nature reviews. Drug discovery · 2013Review
- Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors.Antimicrobial agents and chemotherapy · 2012Article
- Inhibiting early-stage events in HIV-1 replication by small-molecule targeting of the HIV-1 capsid.Journal of virology · 2012Article
- Practical Considerations For Developing Nucleoside Reverse Transcriptase Inhibitors.Drug discovery today. Technologies · 2012Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CMX157 is a lipid (1-0-hexadecyloxypropyl) conjugate of the acyclic nucleotide analog tenofovir (TFV) with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. CMX157 was consistently >300-fold more active than tenofovir against multiple viruses in several different cell systems. CMX157 was active against all major subtypes of HIV-1 and HIV-2 in fresh human peripheral blood mononuclear cells (PBMCs) and against all HIV-1 strains evaluated in monocyte-derived macrophages, with 50% effective concentrations (EC(50)s) ranging between 0.20 and 7.2 nM. The lower CMX157 EC(50)s can be attributed to better cellular uptake of CMX157, resulting in higher intracellular levels of the active antiviral anabolite, TFV-diphosphate (TFV-PP), inside target cells. CMX157 produced >30-fold higher levels of TFV-PP in human PBMCs exposed to physiologically relevant concentrations of the compounds than did TFV. Unlike conventional prodrugs, including TFV disoproxil fumarate (Viread), CMX157 remains intact in plasma, facilitating uptake by target cells and decreasing relative systemic exposure to TFV. There was no detectable antagonism with CMX157 in combination with any marketed antiretroviral drug, and it possessed an excellent in vitro cytotoxicity profile. CMX157 is a promising clinical candidate to treat wild-type and antiretroviral drug-resistant HIV, including strains that fail to respond to all currently available nucleoside/nucleotide reverse transcriptase inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.