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EFFICACY AND SAFETY OF HEMATOLOGICAL OF PHOSPHAZIDE OF HIGHLY ACTIVE ANTIRETROVIRAL THERAPY FOR HIV-INFECTED PATIENTS: 48 WEEKS OF TREATMENT


Background: explore the effectiveness and the hematological safety of the Russian antiretroviral drug Phosphazid (PhAZT, Nikavir) - pro drug zidovudine regimens of HIV- infection.

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5'-Aminocarbonyl Phosphonates as New Zidovudine Depot Forms - Antiviral Properties, Intracellular Transformations, and Pharmacokinetic Parameters


The main disadvantages of 3'~azido~3~deoxythymidine {zidovudine, AZT), the most common anti-HIV drug, are toxicity and a short half- life in the organism. The introduction of an H-phosphonate group into the AZT 5' position resulted in significant improvement of its therapeutic properties and allowed a new anti-HIV drug, Nikavir {AZT H~phosphonate}. In this work, we described a new group of AZT derivatives, namely, AZT 5'-aminocarbonylphosphonates, The synthesized compounds displayed antiviral properties in cell cultures infected with HIV-1 and the capacity to release the active nucleoside in animals {rabbits and dogs) in a dose-dependent manner. The compounds were less toxic in MT-4 and HL-60 cell cultures and experimental animals compared with AZT.

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ANTIVIRAL ACTIVITY AND RESISTANCE PROFILE OF PHOSPHAZID - A NOVEL PRODRUG OF AZT


Both AZT and its novel 5'-hydrogen phosphonate derivative, Phosphazid, possess similar in vitro activity and resistance profiles. Experiments involving AZT- resistant virus isolates revealed a strong correlation between resistance to AZT and crossresistance to Phosphazid. In vitro selection for resistance to Phosphazid yielded viruses that were about 15-fold less sensitive than wild-type virus to this drug. Sequencing of the reverse transcriptase region of seven Phosphazid-selected viruses revealed a single codon mutation, D67N, that is associated with resistance to AZT.

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