Fostemsavir for the treatment of HIV

Seval, Nikhil; Frank, Cynthia; Kozal, Michael J.

doi:10.1080/14787210.2021.1865801

Cited by 22 publications

(15 citation statements)

References 18 publications

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“…Similarly, to what others have found [34][35][36], we recommend that boosted darunavir should be included as part of a salvage regimen amongst treatment-experienced individuals iden-tified to have multiclass HIV DRMs. For individuals with multi-class DRM who are not virologically suppressed, optimizing ART regimens to include newer ARVs such as the attachment inhibitor-fostemsavir and/or anti-CD-4 antibody-ibalizumab might suffice and avert death [37,38]. In the era of mass roll-out of DTG based regimens, there is a need for continued surveillance for INSTI DRMs and determining the clinical significance of these mutations in HIV-1C infections.…”

Section: Discussionmentioning

confidence: 99%

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

Seatla

Maruapula

Choga

et al. 2021

Viruses

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There are limited real-world mutational and virological outcomes data of treatment-experienced persons diagnosed with HIV-1 subtype C (HIV-1 C) who are failing Integrase Strand Transfer Inhibitor-based regimens. Requisition forms sent for HIV-1 genotypic resistance testing (GRT) between May 2015 and September 2019 were reviewed and participants experiencing virologic failure while on dolutegravir (DTG) or raltegravir (RAL) cART at sampling recruited. Sanger sequencing of the HIV-1 Pol gene was performed from residual plasma samples and drug resistance mutational (DRM) analysis performed using the Stanford University HIV drug resistance database. 40 HIV-1C integrase sequences were generated from 34 individuals, 24 of whom were on DTG cART, three on RAL cART and seven on an unknown (DTG or RAL)-anchored cART at time of GRT. 11/34 (32%) individuals had DRMs to DTG and other integrase inhibitors. 7/11 (64%) patients had exposure to a RAL-based cART at the time of sampling. Out of the 11 individuals with DRMs, one (9%) had 2-class, 6 (55%) had 3-class, and 4 (36%) had 4-class multidrug-resistant HIV-1C. 7/11 individuals (64%) are currently virologically suppressed. Of the four individuals not virologically suppressed, three had extensive DRMs involving 4-classes of ARV drugs and one individual has demised. Resistance to DTG occurs more often in patients exposed to RAL cART. Individuals with 4-class DRMs plus integrase T97 and E157Q mutations appear to have worse outcomes. There is a need for frequent VL monitoring and GRT amongst treatment-experienced HIV-1C diagnosed individuals.

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Section: Discussionmentioning

confidence: 99%

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

Seatla

Maruapula

Choga

et al. 2021

Viruses

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“…It truly demonstrates that Fostemsavir is available to HTE populations regardless of viral tropism. Finally, clinical study data indicate that HTE HIV-infected patients have a virological and significant immunological response in combination with OBT [21]. In summary, the results of the efficacy and safety studies show that the drug has unique potential for MDR HIV-infected patients in need of new treatment options.…”

Section: Limitation and Future Developmentmentioning

confidence: 94%

The treatment of Rukobia in AIDS: from lead compound to clinical trial

Ma¹,

Chen²

2023

Second International Conference on Biological Engineering and Medical Science (ICBioMed 2022)

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Every year, few novel drugs were approved by FDA, getting the chance to go public. Their treatment on different diseases interested the authors to find the reason why a certain drug can apply on the treatment from the initial state to the finished medicines and the efforts scientists took for the therapy of diseases. The Rukobia is a good option approved by FDA in 2020 as a novel HIV-1 treatment drug which can help the treatment for multi-drug resistance patients. With the rapidly increasing HIV patients, developing countries need to control and cure the patients with HIV and the treatment for those multi-drug resistance patients can effectively prolong their lives. Present drug therapy can't satisfy the necessary of AIDS patients and the usual treatment cocktail therapy bring patients high drug resistance of first line drugs which means the patients will have no excellent alternative treatment after the cocktail therapy, finishing their lives with no hope. Although the HIV can be treated by the specific gene treatment but it can't be applied on most of patients and the completely curative patients are only 4 until now, as a result, the drug treatment is still important for HIV therapy. Rukobia can't cure the AIDS because the high replication rate of the HIV can't be completely killed in the short time so the drug resistance will also produce after a period of treatment but the novel active site make it different from the known antiviral drugs. The authors want to explore the mechanism of Rukobia and the relationship between the drug development and treatment so Rukobia is a good option which applied the new standard and new methods so it has strong reference meaning for this review. In the future, scientists including the authors can apply the mentioned researching method the development and treatment of the new drugs for other diseases and the Rukobia treatment is summarized more clearly in this review.

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“…Fostemsavir is converted to temsavir by alkaline phosphatase in the gastrointestinal lumen. Thus, the drug can rapidly be absorbed due to its efficient membrane permeability, and the NH group on the pyrrolopyridine ring is free to take part in the key interactions with the gp120 [36]. The crystal structure of the gp120-temsavir complex (PDB code: 5u7o) shows that temsavir binds to a surface-accessible cavity interface between the inner and outer domains of the glycoprotein under the β20-21 loop, interacting with the C terminus of the α1-helix (Figure 3A) [30].…”

Section: Pyrrole-based Entry Inhibitors Of the Hiv-1mentioning

confidence: 99%

Section: Pyrrole-based Entry Inhibitors Of the Hiv-1mentioning

confidence: 99%

Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors

et al. 2021

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Acquired immunodeficiency syndrome (AIDS) is caused by human immunodeficiency virus (HIV) and remains a global health problem four decades after the report of its first case. Despite success in viral load suppression and the increase in patient survival due to combined antiretroviral therapy (cART), the development of new drugs has become imperative due to strains that have become resistant to antiretrovirals. In this context, there has been a continuous search for new anti-HIV agents based on several chemical scaffolds, including nitrogenated heterocyclic pyrrole rings, which have been included in several compounds with antiretroviral activity. Thus, this review aims to describe pyrrole-based compounds with anti-HIV activity as a new potential treatment against AIDS, covering the period between 2015 and 2020. Our research allowed us to conclude that pyrrole derivatives are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle and act with an innovative mechanism.

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Fostemsavir for the treatment of HIV

Cited by 22 publications

References 18 publications

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

The treatment of Rukobia in AIDS: from lead compound to clinical trial

Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors

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