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Tenofovir alafenamide versus tenofovir disoproxil fumarate, coformulated with elvitegravir, cobicistat, and emtricitabine, for initial treatment of HIV-1 infection: two randomised, double-blind, phase 3, non-inferiority trials
Paul E. Sax et al.
LANCET (2015)
An integrated map of HIV genome-wide variation from a population perspective
Guangdi Li et al.
RETROVIROLOGY (2015)
An Odyssey in antiviral drug development-50 years at the Rega Institute: 1964-2014 - Erik De Clercq
Erik De Clercq
ACTA PHARMACEUTICA SINICA B (2015)
In Vitro Resistance Selection with Doravirine (MK-1439), a Novel Nonnucleoside Reverse Transcriptase Inhibitor with Distinct Mutation Development Pathways
Meizhen Feng et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2015)
Safety, tolerability and pharmacokinetics of doravirine, a novel HIV non-nucleoside reverse transcriptase inhibitor, after single and multiple doses in healthy subjects
Matt S. Anderson et al.
ANTIVIRAL THERAPY (2015)
A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women
Annalene Nel et al.
AIDS (2014)
Week 48 results from a randomized clinical trial of rilpivirine/emtricitabine/tenofovir disoproxil fumarate vs. efavirenz/emtricitabine/tenofovir disoproxil fumarate in treatment-naive HIV-1-infected adults
Calvin Cohen et al.
AIDS (2014)
In Vitro Characterization of MK-1439, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor
Ming-Tain Lai et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2014)
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses
Bernard Cote et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)
Tenofovir Alafenamide Vs. Tenofovir Disoproxil Fumarate in Single Tablet Regimens for Initial HIV-1 Therapy
Paul E. Sax et al.
JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES (2014)
4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) Inhibits HIV-1 Reverse Transcriptase with Multiple Mechanisms
Eleftherios Michailidis et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2014)
Quantification of 2′-deoxy-2′-β-fluoro-4′-azidocytidine in rat and dog plasma using liquid chromatography-quadrupole time-of-flight and liquid chromatography-triple quadrupole mass spectrometry: Application to bioavailability and pharmacokinetic studies
Youmei Peng et al.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS (2014)
Azvudine, A Novel Nucleoside Reverse Transcriptase Inhibitor Showed Good Drug Combination Features and Better Inhibition on Drug-Resistant Strains than Lamivudine In Vitro
Rui-Rui Wang et al.
PLOS ONE (2014)
Development of dapivirine vaginal ring for HIV prevention
Brid Devlin et al.
ANTIVIRAL RESEARCH (2013)
Antiviral Activity, Safety, and Pharmacokinetics/Pharmacodynamics of Tenofovir Alafenamide as 10-Day Monotherapy in HIV-1–Positive Adults
Peter J. Ruane et al.
JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES (2013)
Mechanism for Effective Lymphoid Cell and Tissue Loading Following Oral Administration of Nucleotide Prodrug GS-7340
Darius Babusis et al.
MOLECULAR PHARMACEUTICS (2013)
In Vitro Resistance Profile of the Candidate HIV-1 Microbicide Drug Dapivirine
Susan M. Schader et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2012)
Response of Simian Immunodeficiency Virus to the Novel Nucleoside Reverse Transcriptase Inhibitor 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine In Vitro and In Vivo
Michael Murphey-Corb et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2012)
Cobicistat Boosts the Intestinal Absorption of Transport Substrates, Including HIV Protease Inhibitors and GS-7340, In Vitro
Eve-Irene Lepist et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2012)
Novel nucleoside analogue FNC is effective against both wild-type and lamivudine-resistant HBV clinical isolates
Yubing Zhou et al.
ANTIVIRAL THERAPY (2012)
Vaginal Microbicide Gel for Delivery of IQP-0528, a Pyrimidinedione Analog with a Dual Mechanism of Action against HIV-1
Alamelu Mahalingam et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2011)
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase
Robert Gomez et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2011)
The Nonnucleoside Reverse Transcriptase Inhibitor MIV-150 in Carrageenan Gel Prevents Rectal Transmission of Simian/Human Immunodeficiency Virus Infection in Macaques
R. Singer et al.
JOURNAL OF VIROLOGY (2011)
Rilpivirine versus efavirenz with tenofovir and emtricitabine in treatment-naive adults infected with HIV-1 (ECHO): a phase 3 randomised double-blind active-controlled trial
Jean-Michel Molina et al.
LANCET (2011)
TMC278, a Next-Generation Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI), Active against Wild-Type and NNRTI-Resistant HIV-1
Hilde Azijn et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2010)
Pharmacokinetics and Disposition of Rilpivirine (TMC278) Nanosuspension as a Long-Acting Injectable Antiretroviral Formulation
Gerben Van 't Klooster et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2010)
Preexposure Chemoprophylaxis for HIV Prevention in Men Who Have Sex with Men.
Robert M. Grant et al.
NEW ENGLAND JOURNAL OF MEDICINE (2010)
Safety and Availability of Dapivirine (TMC120) Delivered from an Intravaginal Ring
J. Romano et al.
AIDS RESEARCH AND HUMAN RETROVIRUSES (2009)
Safety and Pharmacokinetics of Dapivirine Delivery From Matrix and Reservoir Intravaginal Rings to HIV-Negative Women
Annalene Nel et al.
JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES (2009)
The Design, Synthesis, and Antiviral Activity of Monofluoro and Difluoro Analogues of 4′-Azidocytidine against Hepatitis C Virus Replication: The Discovery of 4′-Azido-2′-deoxy-2′-fluorocytidine and 4′-Azido-2′-dideoxy-2′,2′-difluorocytidine
David B. Smith et al.
JOURNAL OF MEDICINAL CHEMISTRY (2009)
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations
Thomas J. Tucker et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
2 '-deoxy-4 '-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants
Atsushi Kawamoto et al.
INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY (2008)
Discovery of 3-{5-[(6-Amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): A Potent, Orally Bioavailable HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor with Improved Potency against Key Mutant Viruses
Thomas J. Tucker et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
2′-deoxy-4′-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2′-α-hydroxyl groups
Klaus Klumpp et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2008)
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2
Robert W. Buckheit et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2008)
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA Polymerases of 4′-ethynyl-2-fluoro-2′-deoxyadenosine
Hirotorao Nakata et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2007)
Design, synthesis, and antiviral properties of 4′-substituted ribonucleosides as inhibitors of hepatitis C virus replication:: The discovery of R1479
David B. Smith et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains
Celine Mordant et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2007)
Nucleotide HIV reverse transcriptase inhibitors: tenofovir and beyond
Tomas Cihlar
CURRENT OPINION IN HIV AND AIDS (2006)
Short-term antiviral activity of TMC278 -: a novel NNRTI -: in treatment-naive HIV-1-infected subjects
Frank Goebel et al.
AIDS (2006)
Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant
E Muraglia et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Long-term, controlled release of the HIV microbicide TMC120 from silicone elastomer vaginal rings
RK Malcolm et al.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2005)
Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue
WA Lee et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2005)
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1
J Guillemont et al.
JOURNAL OF MEDICINAL CHEMISTRY (2005)
In search of a novel anti-HIV drug:: Multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6dimethylphenyl] amino]-2-pyrimidinyl]amino]-benzonitrile (R278474, rilpivirine)
PAJ Janssen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2005)
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1
K Andries et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2004)
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides
Y Van Herrewege et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2004)
A series of diaryltriazines and diarylpyrimidines are highly potent nonnucleoside reverse transcriptase inhibitors with possible applications as microbicides
Y Van Herrewege et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2004)
Evolution of anti-HIV drug candidates.: Part 1:: From α-anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)
DW Ludovici et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2001)
Evolution of anti-HIV drug candidates part 2:: Diaryltriazine (DATA) analogues
DW Ludovici et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2001)
Evolution of anti-HIV drug candidates.: Part 3:: Diarylpyrimidine (DAPY) analogues
DW Ludovici et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2001)
Practical synthesis, separation, and stereochemical assignment of the PMPA pro-drug GS-7340
H Chapman et al.
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS (2001)
Purification of PMPA amidate prodrugs by SMB chromatography and X-ray crystallography of the diastereomerically pure GS-7340
H Chapman et al.
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS (2001)