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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Enfuvirtide is a member of a new approach to HIV because it blocks the ability of HIV to penetrate cells. No data are published regarding the use of the drug during pregnancy. However, enfuvirtide is an FDA pregnancy risk category B, suggesting it is probably safe for use in pregnancy.
Enfuvirtide
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Juan Ambrosioni, Jose M. Gatell
Enfuvirtide is an antiretroviral drug used in salvage regimens in (usually) highly drug-experienced individuals that suppresses replication of HIV-1 strains with multidrug resistance to reverse transcriptase inhibitors and protease inhibitors. It is used to optimize the response in these individuals to new HIV combination regimens.
Cutaneous Manifestations of Highly Active Antiretroviral Therapy
Published in Clay J. Cockerell, Antoanella Calame, Cutaneous Manifestations of HIV Disease, 2012
Deborah B. Henderson, Clay J. Cockerell
Fusion inhibitors (FIs) are the newest class of antiretrovirals. This group of drugs exerts its effect through specific inhibition of gp41, a CD4+ transmembrane glycoprotein. This action successfully blocks the binding between the host and virus cells, and prevents structural changes necessary for membrane fusion between virus and host. Of this drug class, only enfuvirtide/T-20 is currently approved for use in patients with poor response to other antiretroviral agents. Enfuvirtide is administered via subcutaneous injection and is most commonly associated with injection site reactions. These are characterized by induration, erythema, nodules, cysts, and tenderness at and around the injection site. Up to 98% of patients experienced this complication in Phase III trials.59 Biopsies of involved areas reveal a localized hypersensitivity reaction with changes suggestive of an interstitial granulomatous drug reaction.58 Mixed lymphocytic infiltrates with neutrophils and with or without eosinophils are also seen histologically. Some authors have proposed that rotating injection sites, smaller injection volumes, and specific peptide use may help to minimize the number of enfuvirtide-induced injection reactions.60
Antimicrobial peptides and other peptide-like therapeutics as promising candidates to combat SARS-CoV-2
Published in Expert Review of Anti-infective Therapy, 2021
Masoumeh Sadat Mousavi Maleki, Mosayeb Rostamian, Hamid Madanchi
In addition to natural AVPs, modified and synthetic peptides and other peptide-like structures such as peptidomimetics can also be considered in the fight against COVID-19. Synthetic peptides have various functions such as being antagonists, inhibitors of virus entry into the cell, inhibitors of key enzymes of the virus life cycle, mimics and competitors with receptors for viruses, and immune system modulators. The targets of synthetic peptides are enormously diverse. In the case of coronaviruses, some studies have reported changes in the structure of the S protein to prevent them from entering the cell as the most significant goal of drug design [93,95,96,101]. The entry of coronaviruses, including SARS-CoV-2, into the host cells depends on the binding of coronavirus glycoprotein S (spike) to the receptors. Therefore, factors used by SARS-CoV-2 to enter the cell can be used as therapeutic targets [16]. The receptors of glycoprotein S are ACE2 for SARS-CoV and SARS-CoV-2, CD209L (a type C lectin also called L-SIGN) for SARS-CoV, and DPP4 for MERS-CoV [15]. Madanchi et al. in an in silico study stated that Enfuvirtide, an HIV-1 fusion inhibitor synthetic peptide, can act as a potent SARS-CoV-2 fusion inhibitor [134]. Therefore, their research team strongly recommends a clinical trial on Enfuvirtide as a fusion inhibitor for the treatment of COVID-19.
Evaluating fostemsavir as a therapeutic option for patients with HIV
Published in Expert Opinion on Pharmacotherapy, 2021
Marco Berruti, Rachele Pincino, Lucia Taramasso, Antonio Di Biagio
Entry inhibitors are second-line agents that prevent HIV-1 cellular entry through binding a viral cellular target. Enfuvirtide and maraviroc were the first drugs to use this mechanism of action, as they targeted, respectively, the cellular glycoprotein 41 and the CCR5 receptor. However, these drugs have both been shown to have a lower virologic efficacy or little advantage [13–17] with respect to comparators in more recent years. In addition, the disadvantageous method of administering enfuvirtide, namely subcutaneous administration twice daily while maintaining the cold chain, hampered the diffusion of its use out of the context of strict clinical need. For maraviroc, besides the low efficacy in the naïve and experienced PWH [15,18,19], there was the additional need for tropism testing before prescription, which limited its use. Recently two new drug members of this class are entering the market: ibalizumab and fostemsavir.
Fostemsavir for the treatment of HIV
Published in Expert Review of Anti-infective Therapy, 2021
Nikhil Seval, Cynthia Frank, Michael Kozal
The entry inhibitors are a broad categorization of antiretroviral agents that are often used in drug regimens when the first-line drug classes are limited. Maraviroc, a CCR5 chemokine receptor antagonist, is limited in its indication to those with R5 tropic virus and can be complicated by both hepatotoxicity and drug–drug interactions. Enfuvirtide binds to the gp41 subunit of the HIV viral envelope protein thus preventing fusion and entry into CD4 cells – it is subcutaneous injection whose a twice-a-day administration is often found to be too cumbersome by patients. Ibalizumab is a recombinant monoclonal antibody that was FDA approved in 2018 and functions as a ‘post-attachment’ inhibitor by binding to domain 2 of CD4 cells. It requires an infusion every 2 weeks that may not be feasible for all patients. Fostemsavir represents the addition of a new drug class to the market in an oral formulation with a favorable tolerability profile.