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Update on Raltegravir and the Development of New Integrase Strand Transfer Inhibitors

Southern Medical Journal, 2012
Raltegravir (RAL) is the first antiretroviral in the integrase strand transfer inhibitors (INSTI) class. The use of RAL has expanded since its approval in October 2007 for multidrug-resistant human immunodeficiency virus type 1 infection in adults.
Caitlin Lee, Shamroe   +3 more
openaire   +2 more sources

The Promise of Dolutegravir: A Novel Second Generation Integrase Strand Transfer Inhibitor

Current Clinical Pharmacology, 2016
Dolutegravir (DTG), a novel integrase strand transfer inhibitor (INSTI), is one of the newest addition to the arsenal of anti-human immunodeficiency virus (HIV) therapeutics. Dolutegravir is the first member of the class of second generation integrase strand transfer inhibitors aimed primarily to address the current unmet need for novel unboosted ...
Ashish Kumar Kakkar
exaly   +3 more sources

Dolutegravir: A new integrase strand transfer inhibitor for the treatment of HIV

Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2013
The first two integrase strand transfer inhibitors ( INSTI s) approved for treatment of patients infected with human immunodeficiency virus ( HIV) were raltegravir and elvitegravir. Both raltegravir and elvitegravir are now guideline‐preferred agents as
Bhavik M, Shah   +2 more
openaire   +2 more sources

HIV-1 Integrase Strand Transfer Inhibitors

2010
Publisher Summary This chapter focuses on a new class of antiretroviral agents called “integrase (IN) strand transfer inhibitors” that exert their pharmacological effect by preventing the incorporation of viral DNA into host chromatin. The evolution of HIV-1IN strand transfer inhibitors has been one of the most significant advances in the field of ...
openaire   +1 more source

Chromone and chromanone derivatives as strand transfer inhibitors of HIV-1 integrase

Archives of Pharmacal Research, 2008
HIV-1 integrase catalyzes terminal cleavage at the 3' end of the proviral DNA, removing a pair of bases and causing strand transfer by joining the 3' end to 5'-phosphates in the target DNA. Several aryl 1,3-diketo acids that can inhibit the strand transfer reaction of HIV-1 IN have been identified.
Jang Hyun, Park   +7 more
openaire   +2 more sources

Integrase strand transfer inhibitor-associated diabetes mellitus: A case report

International Journal of STD & AIDS, 2016
Integrase strand transfer inhibitors (INSTIs) have become integral antiretroviral therapy (ART) agents for treating HIV infection. We report the case of a 44-year-old male with a history of hemophilia A who developed diabetes mellitus four months after switching from abacavir, lamivudine, and efavirenz to abacavir, lamivudine, and raltegravir ...
Peter S, Fong   +3 more
openaire   +2 more sources

Emergent drug resistance with integrase strand transfer inhibitor-based regimens

AIDS, 2017
To estimate the incidence of and risk factors for emergent resistance to integrase strand transfer inhibitor (INSTI) and nucleoside(-tide) reverse transcriptase inhibitors (NRTI) in HIV-1-infected adults receiving an INSTI and two NRTIs.Retrospective cohort study.Persons aged at least 19 years were included if they received their first prescription for
Katherine J, Lepik   +11 more
openaire   +2 more sources

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