Biomaterial Database

Enfuvirtide: the first HIV fusion inhibitor. 2005

Adriano Lazzarin

Vita Salute San Raffaele University, Clinic of Infectious Diseases, via Stamira d'Ancona 20, 20127 Milano, Italy. lazzarin.adriano@hsr.it

Highly active antiretroviral therapy, a combination of antiretrovirals to treat HIV-infected individuals, may fail for a number of reasons, including the selection of genetic mutations which confer resistance to the antiretroviral drugs, and poor adherence or treatment discontinuation resulting from drug toxicity. Treatment-experienced patients, who have failed therapy owing to the emergence of drug-resistant virus, have a significant unmet medical need. Enfuvirtide (T-20), the first of a new class of antiretroviral agents known as HIV fusion inhibitors, has a unique mechanism of action involving disruption of HIV entry at the stage of membrane fusion. The potent antiviral activity and favourable safety and tolerability profile of enfuvirtide has been demonstrated in combination with other agents. Its novel mechanism of action offers a low potential for cross-resistance with conventional classes of antiretrovirals, and its extracellular distribution means that drug interactions and intracellular metabolic disturbances are unlikely. Targeting viral fusion or entry will hopefully provide respite for patients who have limited treatment options following the emergence of multi-drug resistance.

UI	MeSH Term	Description	Entries
D008969	Molecular Sequence Data	Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.	Sequence Data, Molecular,Molecular Sequencing Data,Data, Molecular Sequence,Data, Molecular Sequencing,Sequencing Data, Molecular
D010446	Peptide Fragments	Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.	Peptide Fragment,Fragment, Peptide,Fragments, Peptide
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
D000077560	Enfuvirtide	A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.	DP 178,DP-178,DP178,Fuzeon,Pentafuside,Peptide T20,T20 Peptide,T20, Peptide
D000595	Amino Acid Sequence	The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.	Protein Structure, Primary,Amino Acid Sequences,Sequence, Amino Acid,Sequences, Amino Acid,Primary Protein Structure,Primary Protein Structures,Protein Structures, Primary,Structure, Primary Protein,Structures, Primary Protein
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
D015700	HIV Envelope Protein gp41	Transmembrane envelope protein of the HUMAN IMMUNODEFICIENCY VIRUS which is encoded by the HIV env gene. It has a molecular weight of 41,000 and is glycosylated. The N-terminal part of gp41 is thought to be involved in CELL FUSION with the CD4 ANTIGENS of T4 LYMPHOCYTES, leading to syncytial formation. Gp41 is one of the most common HIV antigens detected by IMMUNOBLOTTING.	Envelope Protein gp41, HIV,HIV Transmembrane Protein gp41,HTLV-III gp41,env Protein gp41, HIV,gp41(HIV),gp41 Envelope Protein, HIV
D018791	CD4 Lymphocyte Count	The number of CD4-POSITIVE T-LYMPHOCYTES per unit volume of BLOOD. Determination requires the use of a fluorescence-activated flow cytometer.	Lymphocyte Count, CD4,T4 Lymphocyte Count,CD4 Cell Counts,CD4 Counts,CD4+ Cell Counts,CD4+ Counts,CD4 Cell Count,CD4 Count,CD4 Lymphocyte Counts,CD4+ Cell Count,CD4+ Count,Count, T4 Lymphocyte,Counts, T4 Lymphocyte,Lymphocyte Count, T4,Lymphocyte Counts, CD4,Lymphocyte Counts, T4,T4 Lymphocyte Counts