RESUMO
Raltegravir is the first integrase strand transfer inhibitor approved for the treatment of HIV-1 infection. As the first agent in this new class of antiretroviral therapies, raltegravir has demonstrated safety and efficacy in treatment-naive as well as heavily pretreated HIV-infected patients failing therapy with multidrug-resistant virus. Raltegravir has a favorable drug interaction profile that permits both administration to a wide, demographically diverse patient population and coadministration with many other therapeutic agents, including antiretroviral agents and supportive medications, without restrictions or dose adjustment. Data through 96 weeks of follow-up in three phase III studies, protocol 021 (STARTMRK) in treatment-naive patients, and protocols 018 (BENCHMRK-1) and 019 (BENCHMRK-2) in treatment-experienced patients, demonstrated the potent and durable antiretroviral and immunologic effects and the favorable long-term safety profile of raltegravir in both treatment-naive and treatment-experienced patients. Raltegravir represents an important addition to the current armamentarium for the treatment of HIV infection.
Assuntos
Fármacos Anti-HIV/uso terapêutico , Infecções por HIV/tratamento farmacológico , Inibidores de Integrase de HIV/uso terapêutico , Pirrolidinonas/uso terapêutico , Fármacos Anti-HIV/administração & dosagem , Fármacos Anti-HIV/síntese química , Antirretrovirais/administração & dosagem , Antirretrovirais/uso terapêutico , Ensaios Clínicos Fase III como Assunto , Integrase de HIV/metabolismo , Inibidores de Integrase de HIV/administração & dosagem , Inibidores de Integrase de HIV/síntese química , HIV-1/efeitos dos fármacos , HIV-1/fisiologia , Humanos , Pirrolidinonas/administração & dosagem , Pirrolidinonas/efeitos adversos , Pirrolidinonas/síntese química , Raltegravir Potássico , Resultado do TratamentoRESUMO
FK-463 (micafungin) represents the latest development candidate in a novel chemical class of echinocandin lipopeptide antifungal compounds. This agent has potent in vitro and experimental in vivo activity against a variety of pathogenic Candida species (yeasts) and Aspergillus fumigatus (filamentous fungus). This compound has favorable pharmacokinetics and a unique mode of action that makes it active against fungal isolates resistant to established antifungal agents, particularly the triazole agent fluconazole. Single- and multiple-dose phase I studies in normal human volunteers and phase II clinical trials in patients have been completed, with the compound being generally well tolerated and efficacious against infections caused by Candida and Aspergillus species. Published information on the in vitro and experimental in vivo activity, experimental and human pharmacokinetics, and clinical trial data of this new antifungal, echinocandin-like lipopeptide are summarized in this monograph.
