scholarly journals Polymeric Nanoparticles Containing Combination Antiretroviral Drugs for HIV Type 1 Treatment

2013 ◽  
Vol 29 (5) ◽  
pp. 746-754 ◽  
Author(s):  
Annemarie Shibata ◽  
Emily McMullen ◽  
Alex Pham ◽  
Michael Belshan ◽  
Bridget Sanford ◽  
...  
Keyword(s):  
Polymeric Nanoparticles ◽  
Antiretroviral Drugs ◽  
Hiv Type 1

Characterization of Mutations in HIV Type 1 Isolates from 144 Cambodian Recently Infected Patients and Pregnant Women Naive to Antiretroviral Drugs

2005 ◽  
Vol 21 (11) ◽  
pp. 971-976 ◽  
Author(s):  
Nary Ly ◽  
Patricia Recordon-Pinson ◽  
Viseth Phoung ◽  
Chanthan Srey ◽  
Leang Sim Kruy ◽  
...  
Keyword(s):  
Pregnant Women ◽  
Antiretroviral Drugs ◽  
Hiv Type 1

Increasing HIV Type 1 Polymorphic Diversity But No Resistance to Antiretroviral Drugs in Untreated Patients from Central African Republic: A 2005 Study

2006 ◽  
Vol 22 (10) ◽  
pp. 1036-1044 ◽  
Author(s):  
Valerie Marechal ◽  
Valerie Jauvin ◽  
Benjamin Selekon ◽  
Josianne Leal ◽  
Pulcherie Pelembi ◽  
...  
Keyword(s):  
Central African Republic ◽  
Antiretroviral Drugs ◽  
Hiv Type 1

Current Peptide HIV Type-1 Fusion Inhibitors

2009 ◽  
Vol 20 (1) ◽  
pp. 1-18 ◽  
Author(s):  
Wei Pang ◽  
Siu-Cheung Tam ◽  
Yong-Tang Zheng
Keyword(s):  
Antiviral Agents ◽  
Antiretroviral Drugs ◽  
Host Cells ◽  
Fixed Dose ◽  
Clinical Use ◽  
The Past ◽  
Fusion Inhibitors ◽  
Hiv Type 1 ◽  
Hiv 1

There are now 26 antiretroviral drugs and 6 fixed-dose combinations, including reverse transcriptase inhibitors, protease inhibitors, integrase inhibitors and fusion (or entry) inhibitors, approved by the US Food and Drug Administration for clinical use. Although they are clinically effective when used in combination, none of the existing drugs are considered ideal because of toxic side effects and the ascendance of inducing drug-resistant mutants. Development of new antiviral agents is essential. In the past decades, there has been great progress in understanding the structure of HIV type-1 (HIV-1) gp41 and the mechanism of HIV-1 entry into host cells. This opened up a promising avenue for rationally designed agents to interfere with this process. A number of fusion inhibitors have been developed to block HIV-1 replication. Enfuvirtide (T20) was one of those approved for clinical use. This signalled a new era in AIDS therapeutics. It is a synthetic polypeptide with potent inhibitory activity against HIV-1 infection. However, it is sensitive to proteolytic digestion and resistant virus strains are easily induced with multiple clinical use. One of the directions in designing new fusion inhibitors is to overcome these shortages. In the past years, large numbers of promising fusion inhibitory peptides have emerged. The antiviral activities are more potent or they can act differently from that of T20. Some of these new compounds have great potential to be further developed as therapeutic agents. This article reviewed some recent developments of these peptides and the possible role in anti-HIV-1 therapy.

scholarly journals Combinations of the First and Next Generations of Human Immunodeficiency Virus (HIV) Fusion Inhibitors Exhibit a Highly Potent Synergistic Effect against Enfuvirtide- Sensitive and -Resistant HIV Type 1 Strains

2009 ◽  
Vol 83 (16) ◽  
pp. 7862-7872 ◽  
Author(s):  
Chungen Pan ◽  
Lifeng Cai ◽  
Hong Lu ◽  
Zhi Qi ◽  
Shibo Jiang
Keyword(s):  
Human Immunodeficiency Virus ◽  
Synergistic Effect ◽  
First Generation ◽  
Antiretroviral Drugs ◽  
Synergistic Activity ◽  
Fusion Inhibitors ◽  
Immunodeficiency Virus ◽  
Hiv Type 1 ◽  
Hiv 1

ABSTRACT T20 (generic name, enfuvirtide; brand name, Fuzeon) is a first-generation human immunodeficiency virus (HIV) fusion inhibitor approved for salvage therapy of HIV-infected patients refractory to current antiretroviral drugs. However, its clinical use is limited because of rapid emergence of T20-resistant viruses in T20-treated patients. Therefore, T1249 and T1144 are being developed as the second- and third-generation HIV fusion inhibitors, respectively, with improved efficacy and drug resistance profiles. Here, we found that combinations of T20 with T1249 and/or T1144 resulted in exceptionally potent synergism (combination index, <0.01) against HIV-1-mediated membrane fusion by 2 to 3 orders of magnitude in dose reduction. Highly potent synergistic antiviral efficacy was also achieved against infection by laboratory-adapted and primary HIV-1 strains, including T20-resistant variants. The mechanism underlying the synergistic effect could be attributed to the fact that T20, T1249, and T1144 all contain different functional domains and have different primary binding sites in gp41. As such, they may work cooperatively to inhibit gp41 six-helix bundle core formation, thereby suppressing virus-cell fusion. Therefore, these findings strongly imply that, rather than replacing T20, combining it with HIV fusion inhibitors of different generations might produce synergistic activity against both T20-sensitive and -resistant HIV-1 strains, suggesting a new therapeutic strategy for the treatment of HIV-1 infection/AIDS.

Genotypic Resistance of Antiretroviral Drugs among Drug-Naive HIV Type 1 Patients with the Background of Long-Term Access-Easy Zidovudine Therapy

2003 ◽  
Vol 19 (11) ◽  
pp. 1039-1043 ◽  
Author(s):  
Sang Won Park ◽  
Hong Bin Kim ◽  
Young Ju Choi ◽  
Nam Jung Kim ◽  
Myoung Don Oh ◽  
...  
Keyword(s):  
Antiretroviral Drugs ◽  
Zidovudine Therapy ◽  
Genotypic Resistance ◽  
Drug Naïve ◽  
Hiv Type 1

Genotypic Resistance to Antiretroviral Drugs in Patients Infected with Several HIV Type 1 Genetic Forms in Cuba

2007 ◽  
Vol 23 (3) ◽  
pp. 407-414 ◽  
Author(s):  
Lissette Pérez ◽  
Lucía Pérez Álvarez ◽  
Rocío Carmona ◽  
Carlos Aragonés ◽  
Elena Delgado ◽  
...  
Keyword(s):  
Antiretroviral Drugs ◽  
Genotypic Resistance ◽  
Hiv Type 1

Molecular Characterization of HIV Type 1 in Brazzaville, Republic of Congo, and First Data on Resistance to Antiretroviral Drugs

2012 ◽  
Vol 28 (12) ◽  
pp. 1798-1802 ◽  
Author(s):  
Mathilde Pircher ◽  
Merlin Diafouka ◽  
Jennifer Papuchon ◽  
Patricia Recordon-Pinson ◽  
Dominique Nsonde Mahambou ◽  
...  
Keyword(s):  
Molecular Characterization ◽  
Antiretroviral Drugs ◽  
Republic Of Congo ◽  
Hiv Type 1
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