Biomaterial Database

Raltegravir: a review of its pharmacokinetics, pharmacology and clinical studies. 2010

David M Burger

Department of Pharmacy, 864 Radboud University Nijmegen Medical Center, Geert Grooteplein 10, 6525 GA Nijmegen, the Netherlands. D.Burger@akf.umcn.nl

BACKGROUND Raltegravir is the first HIV-integrase inhibitor licensed by the FDA. METHODS A PubMed search was conducted for all published reports up to 1 May 2010 related to raltegravir pharmacokinetics, pharmacology, drug-drug interactions and clinical studies in HIV-infected patients. Also included in this review are the updated European and US Prescriber's Information (European Medicines Agency and the FDA) and abstracts from recent international scientific meetings. RESULTS After reading the review, a thorough insight in raltegravir pharmacokinetics and pharmacology will be obtained, as well as an up-to-date overview of all published drug-drug interaction studies. Furthermore, one should be able to make an evidence-based opinion on the drug's clinical efficacy and tolerability. CONCLUSIONS Raltegravir is a welcome addition to the antiretroviral drug armamentarium due to its good tolerability, low potential for drug-drug interactions and good clinical efficacy in both treatment-naive and -experienced patients.

UI	MeSH Term	Description	Entries
D011760	Pyrrolidinones	A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)	Pyrrolidinone,Pyrrolidone,Pyrrolidones
D002460	Cell Line	Established cell cultures that have the potential to propagate indefinitely.	Cell Lines,Line, Cell,Lines, Cell
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
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
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000068898	Raltegravir Potassium	A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.	Isentress,MK 0518,MK-0518,MK0518,Raltegravir,0518, MK,Potassium, Raltegravir
D015497	HIV-1	The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.	Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D015658	HIV Infections	Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	HTLV-III Infections,HTLV-III-LAV Infections,T-Lymphotropic Virus Type III Infections, Human,HIV Coinfection,Coinfection, HIV,Coinfections, HIV,HIV Coinfections,HIV Infection,HTLV III Infections,HTLV III LAV Infections,HTLV-III Infection,HTLV-III-LAV Infection,Infection, HIV,Infection, HTLV-III,Infection, HTLV-III-LAV,Infections, HIV,Infections, HTLV-III,Infections, HTLV-III-LAV,T Lymphotropic Virus Type III Infections, Human
D019428	HIV Integrase Inhibitors	Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA.	Integrase Inhibitors, HIV,Inhibitors, HIV Integrase
D024882	Drug Resistance, Viral	The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.	Antiviral Drug Resistance,Antiviral Drug Resistances,Drug Resistances, Viral