Effects of fostemsavir: A Synthesis of Findings from 24 Studies

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Original Abstract of the Article

Major Research Findings

Fostemsavir is a novel antiretroviral drug that belongs to a new class of drugs called attachment inhibitors. These drugs block the entry of HIV into CD4+ T-lymphocytes by preventing conformational changes in gp120, a protein on the surface of the virus that is necessary for attachment to host cells 8 . This new drug class is especially important for patients who have been treated with multiple antiretroviral therapies but have not found a regimen that works for them, which is a growing problem worldwide 8 9 .

Fostemsavir is the first attachment inhibitor approved by the Food and Drug Administration and European Medicines Agency for the treatment of HIV-1 infection 11 . Fostemsavir has shown promise as part of a drug combination therapy in highly treatment-experienced HIV-1 infected patients 20 . In a phase 3 study called BRIGHTE, fostemsavir was shown to be more effective than a placebo at suppressing viral replication in patients with multidrug-resistant HIV-1 2 . After 96 weeks, fostemsavir was found to be generally well-tolerated and led to sustained virologic and immunologic responses in patients. In fact, fostemsavir-based treatment regimens have shown comparable or superior efficacy and safety to other antiretroviral therapies in heavily treatment-experienced patients with multidrug-resistant HIV-1 4 .

Benefits and Risks

Benefit Summary

Fostemsavir offers a new treatment option for patients with multidrug-resistant HIV-1 21 . Fostemsavir is effective and safe for patients who have not found a successful antiretroviral regimen 4 .

Risk Summary

Fostemsavir is generally well tolerated 22 14 . However, fostemsavir’s blood concentration increases when administered concurrently with CYP3A4 inhibitors, such as ritonavir and atazanavir 22 . Therefore, dose adjustments may be required when fostemsavir is administered with ritonavir or atazanavir 22 . The potential for QTc prolongation with fostemsavir has also been studied 1 . While fostemsavir 1200 mg b.i.d. did not result in a clinically meaningful QTc prolongation, a supratherapeutic dose of 2400 mg b.i.d. did show a clinically significant prolongation 1 . Further research into the effects of fostemsavir on the QTc interval is necessary 1 .

Comparison between Studies

Similarities

Fostemsavir is a new class of antiretroviral drug that shows efficacy and safety in heavily treatment-experienced patients with multidrug-resistant HIV-1 21 2 4 .

Differences

Some studies have evaluated the effects of fostemsavir monotherapy 23 . Others have evaluated fostemsavir in combination with other antiretroviral drugs 2 4 .

Consistency and Discrepancies

Fostemsavir is a new class of antiretroviral drug that shows efficacy and safety in heavily treatment-experienced patients with multidrug-resistant HIV-1 21 2 4 . However, the effectiveness of fostemsavir monotherapy can vary between studies 23 . Further research is needed on fostemsavir combination therapies 4 .

Considerations for Real-World Application

Fostemsavir may offer a new treatment option for patients with multidrug-resistant HIV-1 21 . However, when fostemsavir is administered with CYP3A4 inhibitors, such as ritonavir and atazanavir, dose adjustments may be required 22 . Healthcare providers must carefully consider drug interactions and side effects before prescribing fostemsavir, taking into account individual patient circumstances 21 .

Limitations of Current Research

Research on fostemsavir is still limited 21 4 . Further research is needed on the long-term effects and safety of fostemsavir 21 4 .

Future Research Directions

Research is needed to evaluate the long-term efficacy and safety of fostemsavir, as well as the efficacy of fostemsavir in combination with other antiretroviral drugs 21 4 .

Conclusion

Fostemsavir may offer a new treatment option for patients with multidrug-resistant HIV-1 21 2 4 . Fostemsavir is effective and safe for patients who have not found a successful antiretroviral regimen 4 . However, research on fostemsavir is still limited 21 4 . Further research is needed to evaluate the long-term effects and safety of fostemsavir 21 4 .

Literature analysis of 24 papers
Positive Content
24
Neutral Content
0
Negative Content
0
Article Type
8
0
1
5
23
1.

Effects of Temsavir, Active Moiety of Antiretroviral Agent Fostemsavir, on QT Interval: Results From a Phase I Study and an Exposure-Response Analysis.

Author: LagishettyChakradhar, MooreKaty, AckermanPeter, LlamosoCyril, MageeMindy

HIV-1 treatment
Arrhythmia
QTc prolongation

Fostemsavir, a prodrug of temsavir, was found to be safe for treating multidrug-resistant HIV infection at therapeutic doses. However, supratherapeutic doses showed a potential for QTc prolongation.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

2.

Safety and efficacy of the HIV-1 attachment inhibitor prodrug fostemsavir in heavily treatment-experienced individuals: week 96 results of the phase 3 BRIGHTE study.

Author: LatailladeMax, LalezariJacob P, KozalMichael, AbergJudith A, PialouxGilles, CahnPedro, ThompsonMelanie, MolinaJean-Michel, MorenoSantiago, GrinsztejnBeatriz, DiazRicardo S, CastagnaAntonella, KumarPrincy N, LatiffGulam H, De JesusEdwin, WangMarcia, ChabriaShiven, GartlandMargaret, PierceAmy, AckermanPeter, LlamosoCyril

HIV-1 treatment
Superior efficacy

This study reports interim analyses through week 96 of the BRIGHTE study, which evaluated the efficacy of fostemsavir versus placebo in heavily treatment-experienced individuals with multidrug-resistant HIV-1. Fostemsavir demonstrated superior efficacy compared to placebo after 8-day functional monotherapy.

Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

3.

Viral Drug Resistance Through 48 Weeks, in a Phase 2b, Randomized, Controlled Trial of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir.

Author: LatailladeMax, ZhouNannan, JoshiSamit R, LeeSangil, StockDavid A, HannaGeorge J, KrystalMark,

HIV-1 treatment

Fostemsavir, a prodrug of temsavir, demonstrated safety, efficacy, and a dose-response relationship when compared to ritonavir-boosted atazanavir in treatment-experienced, HIV-1-infected subjects in a phase 2b trial.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Comparative Efficacy and Safety of Fostemsavir in Heavily Treatment-Experienced People With HIV-1.

Author: AndersonSarah-Jane, van DoornewaardAlexander, TurnerMatthew, JacobIan, ClarkAndrew, BrowningDominy, SchroederMelanie

Treat HIV-1

This analysis indirectly compares the efficacy and safety of fostemsavir, a new attachment inhibitor for multidrug-resistant HIV-1, with other antiretroviral regimens. Fostemsavir demonstrated sustained virologic and immunologic responses in heavily treatment-experienced patients over 96 weeks.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

6.

Lenacapavir with Fostemsavir in a Multidrug-Resistant HIV-Infected Hemodialysis Patient.

Author: BigirimanaFerdinand, Van den WijngaertSigi, FossoChristelle, StoffelsKarolien, MartinCharlotte, MaillartEvelyne, ClevenberghPhilippe

MDR HIV treatment
Renal safety
None mentioned

A patient with end-stage renal disease and multidrug-resistant (MDR) HIV infection successfully maintained viral suppression for over a year after switching to a combination of fostemsavir and lenacapavir plus lamivudine. This combination shows promise for treating MDR HIV in patients with renal impairment.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

7.

Safety and efficacy of the HIV-1 attachment inhibitor prodrug BMS-663068 in treatment-experienced individuals: 24 week results of AI438011, a phase 2b, randomised controlled trial.

Author: LalezariJacob P, LatiffGulam H, BrinsonCynthia, EchevarríaJuan, Treviño-PérezSandra, BognerJohannes R, ThompsonMelanie, FourieJan, Sussmann PenaOtto A, Mendo UrbinaFernando C, MartinsMarcelo, DiaconescuIulian G, StockDavid A, JoshiSamit R, HannaGeorge J, LatailladeMax,

HIV-1 infection treatment

This study presents the results of the primary analysis of AI438011, an ongoing trial investigating the efficacy, safety, and dose-response of BMS-663068 in treatment-experienced, HIV-1-infected patients. BMS-663068 is an oral prodrug of BMS-626529, an attachment inhibitor that binds to HIV-1 gp120, blocking viral attachment to host CD4 cells.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Fostemsavir: a new CD4 attachment inhibitor.

Author: CahnPedro, FinkValeria, PattersonPatricia

Drug resistance prevention
HIV treatment
ARV failure
Drug resistance

This study addresses the ongoing challenge of antiretroviral (ARV) failure and drug resistance despite the availability of modern HAART. The authors emphasize the need for new classes of ARVs with different mechanisms of action to overcome this challenge and highlight the lack of new ARV classes introduced since the launch of integrase inhibitors more than a decade ago.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

10.

[The newest developments of the study on anti-HIV drugs].

Author: ZhangXing-quan

Less toxicity
Potent antiretroviral activity
Reverse latent HIV infections

This review focuses on investigational antiretroviral agents currently in phase 2-3 clinical trial, including tenofoviralafenamidefumarate (TAF), doravirine, and GSK744. It also discusses novel drug candidates with different mechanisms, such as histone deacetylase inhibitors and other agents targeting HIV latency.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : Chinese

12.

Prevalence of gp160 polymorphisms known to be related to decreased susceptibility to temsavir in different subtypes of HIV-1 in the Los Alamos National Laboratory HIV Sequence Database.

Author: GartlandMargaret, ArnoultEric, FoleyBrian T, LatailladeMax, AckermanPeter, LlamosoCyril, KrystalMark

Analysis of the LANL HIV Sequence Database found a low prevalence of gp160 amino acid polymorphisms associated with reduced temsavir susceptibility.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

13.

Impact of natural polymorphisms of HIV-1 non-group M on genotypic susceptibility to the attachment inhibitor fostemsavir.

Author: Alessandri-GradtElodie, CharpentierCharlotte, LeozMarie, MourezThomas, DescampsDiane, PlantierJean-Christophe

HIV-1 entry inhibition
Natural resistance

Fostemsavir, a promising attachment inhibitor (AI) for HIV treatment, has been shown to be effective against most HIV-1 groups. However, previous studies indicated potential resistance in divergent HIV-1 group O. This study aims to investigate the susceptibility of other divergent groups, N and P, to fostemsavir.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

15.

Compartmental absorption modeling and site of absorption studies to determine feasibility of an extended-release formulation of an HIV-1 attachment inhibitor phosphate ester prodrug.

Author: BrownJonathan, ChienCaly, TimminsPeter, DennisAndrew, DollWalter, SandeferErik, PageRichard, NettlesRichard E, ZhuLi, GraselaDennis

Compartmental absorption modeling was used to predict the potential feasibility of extended-release (ER) delivery for BMS-663068, a prodrug for the treatment of HIV/AIDS. The model was successfully used to guide the development of ER tablet formulations.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

16.

Effects of Temsavir, Active Moiety of Antiretroviral Agent Fostemsavir, on QT Interval: Results From a Phase I Study and an Exposure-Response Analysis.

Author: LagishettyChakradhar, MooreKaty, AckermanPeter, LlamosoCyril, MageeMindy

HIV-1 treatment
Arrhythmia
QTc prolongation

Fostemsavir, a prodrug of temsavir, was found to be safe for treating multidrug-resistant HIV infection at therapeutic doses. However, supratherapeutic doses showed a potential for QTc prolongation.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

17.

Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects.

Author: NettlesRichard E, SchürmannDirk, ZhuLi, StonierMichele, HuangShu-Pang, ChangIh, ChienCaly, KrystalMark, Wind-RotoloMegan, RayNeelanjana, HannaGeorge J, BertzRichard, GraselaDennis

Reduced viral load

BMS-663068 is a prodrug that inhibits HIV-1 infection. In a study of 50 HIV-1-infected subjects, BMS-663068 was administered with or without ritonavir for 8 days. All regimens resulted in substantial decreases in plasma HIV-1 RNA levels and were generally well tolerated. Further clinical trials of BMS-663068 as part of combination antiretroviral therapy are warranted.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

18.

Fostemsavir in Adults with Multidrug-Resistant HIV-1 Infection.

Author: KozalMichael, AbergJudith, PialouxGilles, CahnPedro, ThompsonMelanie, MolinaJean-Michel, GrinsztejnBeatriz, DiazRicardo, CastagnaAntonella, KumarPrincy, LatiffGulam, DeJesusEdwin, GummelMark, GartlandMargaret, PierceAmy, AckermanPeter, LlamosoCyril, LatailladeMax,

HIV-1 inhibition

Fostemsavir is the prodrug of temsavir, a first-in-class investigational HIV-1 attachment inhibitor. Fostemsavir may be a promising treatment option for patients with HIV-1 infection who have limited treatment options.

Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

20.

Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.

Author: WangTao, UedaYasu, ZhangZhongxing, YinZhiwei, MatiskellaJohn, PearceBradley C, YangZheng, ZhengMing, ParkerDawn D, YamanakaGregory A, GongYi-Fei, HoHsu-Tso, ColonnoRichard J, LangleyDavid R, LinPin-Fang, MeanwellNicholas A, KadowJohn F

Antiviral potency

Temsavir (BMS-626529), an HIV-1 attachment inhibitor, demonstrated promising antiviral potency and pharmacokinetic properties. However, its physical properties limited plasma exposure at higher doses, leading to the development of the phosphonooxymethyl prodrug fostemsavir (BMS-663068).

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

21.

The Genesis and Future Prospects of Small Molecule HIV-1 Attachment Inhibitors.

Author: WangTao, KadowJohn F, MeanwellNicholas A, KrystalMark

HIV-1 attachment inhibition
Improved treatment options
None reported

Fostemsavir is a first-in-class HIV-1 attachment inhibitor recently approved for use in highly treatment experienced (HTE) patients with multidrug resistant HIV-1. It binds to gp120, a critical viral protein, and inhibits HIV-1 entry and infection.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

22.

Pharmacokinetic interactions between BMS-626529, the active moiety of the HIV-1 attachment inhibitor prodrug BMS-663068, and ritonavir or ritonavir-boosted atazanavir in healthy subjects.

Author: ZhuLi, HruskaMatthew, HwangCarey, ShahVaishali, FurlongMichael, HannaGeorge J, BertzRichard, LandryIshani Savant

HIV-1 attachment inhibition
Drug-drug interactions

BMS-663068, a prodrug of BMS-626529, an HIV-1 attachment inhibitor, showed moderate increases in systemic exposure when coadministered with ritonavir or atazanavir/ritonavir. However, the combination was well tolerated, with no adverse events leading to discontinuation or death.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

23.

Prediction of virological response and assessment of resistance emergence to the HIV-1 attachment inhibitor BMS-626529 during 8-day monotherapy with its prodrug BMS-663068.

Author: RayNeelanjana, HwangCarey, HealyMatthew D, WhitcombJeannette, LatailladeMax, Wind-RotoloMegan, KrystalMark, HannaGeorge J

HIV-1 treatment

BMS-663068 is a drug being developed for HIV-1 infection. This study investigated the effectiveness of BMS-663068 in HIV-1 infected subjects, finding variable responses.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

24.

Synthesis of the 6-azaindole containing HIV-1 attachment inhibitor pro-drug, BMS-663068.

Author: ChenKe, RisattiChristina, BultmanMichael, SoumeillantMaxime, SimpsonJames, ZhengBin, FanfairDayne, MahoneyMichelle, MudrykBoguslaw, FoxRichard J, HsaioYi, MurugesanSaravanababu, ConlonDavid A, BuonoFrederic G, EastgateMartin D

Synthesis efficiency

This study describes a short and efficient synthesis of a complex 6-azaindole, BMS-663068. The synthesis involves a series of reactions, including a regioselective Friedel-Crafts acylation, Pictet-Spengler cyclization, and a radical-mediated aromatization, resulting in an efficient 11-step linear synthesis of this complex clinical candidate.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

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