Update on rilpivirine: a new potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV replication. 2013

Gerasimos J Zaharatos, and Mark A Wainberg
Division of Infectious Diseases, Jewish General Hospital, Montreal, Canada.

BACKGROUND A combination of antiretroviral drugs (ARVs) is necessary to achieve sustained virologic suppression of HIV viral load (< 50 copies/mL). Rilpivirine (RPV) is a potent new non-nucleoside reverse transcriptase inhibitor (NNRTI) that has the potential to be part of effective ARV combinations. Here, we review currently available data on RPV from the standpoint of virologic suppression and efficacy, drug-drug interactions safety, and resistance. METHODS This review presents data on the results of clinical trials involving RPV. The topics considered include antiviral potency, dosing, clinical utility, drug resistance, toxicity profile, and pharmacokinetics. CONCLUSIONS RPV is a potent new addition to the antiretroviral family of drugs for use in combination therapy in previously untreated HIV-infected patients. However, caution needs to be exercised in administration of RPV to patients who initiated therapy with viral loads > 100,000 viral RNA copies/mL.

UI MeSH Term Description Entries
D009570 Nitriles Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE. Nitrile
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D002784 Cholesterol The principal sterol of all higher animals, distributed in body tissues, especially the brain and spinal cord, and in animal fats and oils. Epicholesterol
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D003404 Creatinine Creatinine Sulfate Salt,Krebiozen,Salt, Creatinine Sulfate,Sulfate Salt, Creatinine
D003875 Drug Eruptions Adverse cutaneous reactions caused by ingestion, parenteral use, or local application of a drug. These may assume various morphologic patterns and produce various types of lesions. Dermatitis Medicamentosa,Dermatitis, Adverse Drug Reaction,Maculopapular Drug Eruption,Maculopapular Exanthem,Morbilliform Drug Reaction,Morbilliform Exanthem,Drug Eruption,Drug Eruption, Maculopapular,Drug Eruptions, Maculopapular,Drug Reaction, Morbilliform,Drug Reactions, Morbilliform,Eruption, Drug,Eruption, Maculopapular Drug,Eruptions, Drug,Eruptions, Maculopapular Drug,Exanthem, Maculopapular,Exanthem, Morbilliform,Exanthems, Maculopapular,Exanthems, Morbilliform,Maculopapular Drug Eruptions,Maculopapular Exanthems,Morbilliform Drug Reactions,Morbilliform Exanthems,Reaction, Morbilliform Drug,Reactions, Morbilliform Drug
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004359 Drug Therapy, Combination Therapy with two or more separate preparations given for a combined effect. Combination Chemotherapy,Polychemotherapy,Chemotherapy, Combination,Combination Drug Therapy,Drug Polytherapy,Therapy, Combination Drug,Chemotherapies, Combination,Combination Chemotherapies,Combination Drug Therapies,Drug Polytherapies,Drug Therapies, Combination,Polychemotherapies,Polytherapies, Drug,Polytherapy, Drug,Therapies, Combination Drug
D004562 Electrocardiography Recording of the moment-to-moment electromotive forces of the HEART as projected onto various sites on the body's surface, delineated as a scalar function of time. The recording is monitored by a tracing on slow moving chart paper or by observing it on a cardioscope, which is a CATHODE RAY TUBE DISPLAY. 12-Lead ECG,12-Lead EKG,12-Lead Electrocardiography,Cardiography,ECG,EKG,Electrocardiogram,Electrocardiograph,12 Lead ECG,12 Lead EKG,12 Lead Electrocardiography,12-Lead ECGs,12-Lead EKGs,12-Lead Electrocardiographies,Cardiographies,ECG, 12-Lead,EKG, 12-Lead,Electrocardiograms,Electrocardiographies, 12-Lead,Electrocardiographs,Electrocardiography, 12-Lead

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