Nikavir in Chemoprevention Regimens of Vertical HIV Transmission

Optimal Choice of Antiretroviral Therapy Regimen Including Phospha

“…We had also studied its safety and low toxicity in the schemes of perinatal chemoprophylaxis of motherto-child HIV transmission, treatment of infection and prevention of parenteral infection of medical workers in the course of their duties earlier. [11][12][13][14]. As a result, ART regimens with the least number of undesirable side reactions (ADR) from organs and systems were identified -this is a combination of 2 NRTIs + AI -tenofovir + phosphazide + dolutegravir (73 (11.8%) of 617 ADR), while the combination of abacavir + phosphazide + dolutegravir potentially causes only 8 (1.3%) ADR, which are the same for all three drugs.…”

AZT 5’-Phosphonates: Achievements and Trends in the Treatment and Prevention of HIV Infection

“…AZT from phosphazide is capable of efficiently penetrating the placenta; thus, equal AZT concentrations are maintained in the mother’s umbilical cord and blood. The use of Nikavir during a pregnancy (combined with Retrovir or Nevirapine during childbirth and the postnatal period) efficiently prevents vertical transmission of HIV [29, 30]. In some cases, Retrovir can be substituted by Nikavir because of a low hemoglobin level in the blood of a pregnant woman.…”

Design, Synthesis, and Antiviral Evaluation of Chimeric Inhibitors of HIV Reverse Transcriptase

“…37 A recent study suggests that although AZT H-phosphonate is structurally similar to AZT-monophosphate (AZTMP), it might be more resistant to extra and/or intracellular dephosphorylation and could penetrate through cellular membranes due to its less polar nature by possessing only a single negative charge unlike a monophosphate group with two negative charges. 38 Overall, the chimeric inhibitors 9 and 10 have exhibited potencies 16-to 30-fold higher than d4T with a selectivity index of 18 and 27, respectively.…”

“…Moreover, it must be noted here that 5′-H-phosphonate derivative of an NRTI, 5′-H-phosphonate-3′-azido-3′-deoxythymidine (AZT H-phosphonate, Nikavir), has been approved by the Russian Ministry of Health for the prevention and treatment of HIV-infected patients as a consequence of lower toxicity profile and a longer half-life than AZT while inducing much slower selection of drug-resistant viruses. 37 A recent study suggests that although AZT H-phosphonate is structurally similar to AZT-monophosphate (AZTMP), it might be more resistant to extra and/or intracellular dephosphorylation and could penetrate through cellular membranes due to its less polar nature by possessing only a single negative charge unlike a monophosphate group with two negative charges. 38 Overall, the chimeric inhibitors 9 and 10 have exhibited potencies 16-to 30fold higher than d4T with a selectivity index of 18 and 27, respectively.…”