Ponatinib is a potent TKI that can overcome several resistance mechanisms in previously treated patients with CML and Ph+ ALL. Ponatinib should be reserved for patients who have failed first-line therapy, have the T315I mutation, or have progressed.
I n the era of potentantiretrovira1 (ARV) therapy(ART), Hlv-I infection has become a chronicdiseaserather than a terminal illness, allowing those whoaretreated with ART to have normal life ex-pectancies} Complications, mortality, and viral transmission of Hlv-I have significantly decreased with the adventof new ARVs.2.7 Long-term adverse effects of olderARVs include dysglycemia, dyslipidemia, lipodystrophy, and gastrointestinal discomfort'If nonadherence occurs in patients on ART, Hlv-l drugresistance may develop,limiting the effectiveness of future therapy. Hence, it is crucial to choose regimens that are not only effective against Hl'V-l , but alsominimize adverse events andmaximize adherence. Raltegravir,formerly known as MK-0518, is the first integrase strandtransfer inhibitor (INSTI) to be approved by the Food and Drug Administration (FDA). It works by preventing the formation of a functional integrated proviral DNA.s First approved in October 2007 for salvage therapy in ARV-experienced patients, raltegravir is active against multiclass-resistant HIV-I and both CCR5tropic and CXCR4-tropic HIV_I.s-lo In December 2011, the FDA extended the Author information providedat end of text. OBJECTIVE: To review the literature concerning the role of raltegravir in the treatment of HIV•1 in antiretroviral (ARV)-experienced and ARV-na"ive patients. DATA SOURCES: A PubMed search was conducted for published data through March 2012 using the search terms raltegravir, MK-0518, and integrase strand transfer inhibitor. An additional search of International Pharmaceutical Abstracts for unpublished data, including data from the Infectious Diseases Society of America, the Conference on Retroviruses and Opportunistic Infections, the International AIDS Society. and the Interscience Conference on Antimicrobial Agents and Chemotherapy, was conducted using similar search terms. STUDY SELECT10N AM) DATA EXmACTlON: In vitroand in vivo Phase2, Phase 3 , and postmarketing studies availableIn English, evaluating antiretroviral regimens that containrattegravir for the treatment of HIV•1 infection in both ARV•naive andARV• experienced patients, were evaluated. Studies assessing raltegravirpharrnacokineticsand pharmacodynamics were included for review. DATA SYNTliESlS: The nucleoside-based regimen of raltegravir with tenofovir/emtri• citabine provides an effective first•line treatment option. However, nucleoside• sparing regimens appear unfavorable in ARV•naive subjects and should be reserved for patients with limited treatment options. Raltegravir used with optimized background therapy provides an a1temative regimen for ARV-experienced patients. This review describesthe available in vitro and in vivo data on raltegravir potency, defined as the abilityto achieve undetectable viral load, and safety profile, as well as comparison to standardHIV•1 therapies. CONCLUSIONS: Raltegravir has demonstrated potent antiretroviral activity against HIV•1 in both ARV•naive and ARV-experienced subjects, with the benefits of a favorable adverse effect profile ...
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. RAL is now a guideline-preferred treatment option for antiretroviral-naïve patients, indicated for treatment in adolescents, and is being studied as an integral part of nucleoside sparing regimens. The development of resistance and the need for a once-daily dosing option has led to the development of new INSTIs, including elvitegravir and dolutegravir. Elvitegravir is being studied in a promising once-daily single-tablet regimen with tenofovir, emtricitabine, and the investigational pharmacoenhancer cobicistat. The development of cobicistat and the new once-daily INSTIs may revolutionize the treatment of human immunodeficiency virus type 1 infection. This article reviews the current literature on raltegravir and new developments in the INSTI class.
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