Effects of etravirine: A Synthesis of Findings from 26 Studies

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Original Abstract of the Article

Main Research Findings

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been shown to be effective against HIV-1 infection. 13 examined the susceptibility of Human Endogenous Retrovirus Type K (HK2) to reverse transcriptase inhibitors. This study found that etravirine is effective at inhibiting HK2 replication. 11 studied the suppression of Zika Virus infection in the brain using the antiretroviral drug rilpivirine. It showed that rilpivirine, along with other NNRTIs like etravirine and efavirenz, can suppress ZIKV infection and replication in human brain cells. 9 explored the design and synthesis of novel oxime-biphenyl-DAPYs as potential HIV-1 treatments. While efavirenz and etravirine were compared in this study, the focus was on a new compound, 7d, with promising activity against HIV-1. 20 investigated the prevalence of rilpivirine resistance in people starting antiretroviral treatment in Argentina. This research indicated a concern about resistance to newer NNRTIs in this population. 21 examined the potential of antiretrovirals for HIV prophylaxis, including etravirine. This study found that etravirine could potentially be more effective than existing PrEP regimens. 22 explored the potential of repurposing approved drugs for triple-negative breast cancer treatment. This research identified etravirine as a promising candidate for targeting CK2 alpha kinase, a key modulator of TNBC. 4 explored the design of novel diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles with high potency against HIV-1. This study compared the activity of these compounds to the marketed drug Etravirine. 2 examined the use of therapeutic drug monitoring (TDM) in treatment-experienced HIV-infected patients receiving darunavir-based salvage therapy. While this study did not focus on etravirine, it highlights the importance of monitoring drug levels in HIV treatment. 16 assessed the emergence of uncommon HIV-1 non-B subtypes and circulating recombinant forms in Marseille, France, including the prevalence of antiretroviral drug resistance. This study found that etravirine/rilpivirine-associated RAM prevalence was 4.3% in this population. 18 investigated the pharmacokinetics of temsavir, the active moiety of the HIV-1 attachment inhibitor prodrug, fostemsavir, in combination with other antiretrovirals, including etravirine. This study explored potential drug-drug interactions and found that etravirine decreased temsavir concentrations. 8 explored the discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs. This research compared the activity of these compounds to etravirine and other NNRTIs. 24 investigated the discovery of novel dihydrothiopyrano[4,3-d]pyrimidine derivatives as potent HIV-1 NNRTIs with improved resistance profiles. This study compared the activity of these compounds to etravirine and rilpivirine. 14 explored the discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs. This research compared the activity of these compounds to etravirine and rilpivirine, as well as efavirenz. 1 studied the effects of hepatic impairment on the steady-state pharmacokinetics of etravirine. This study showed that etravirine can be safely administered in patients with impaired liver function. 15 investigated the structure-based optimization of thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs. This research compared the activity of these compounds to etravirine. explored the potential of repurposing FDA-approved antiviral drugs for the treatment of COVID-19. This study included etravirine as a potential drug candidate. 6 investigated the prevalence of rilpivirine resistance-associated mutations in the USA and their effects on phenotypic susceptibility to rilpivirine and etravirine. 12 assessed the endothelial, inflammatory, coagulation, metabolic effects and safety of etravirine in HIV-uninfected volunteers. This study showed that etravirine was generally well tolerated. 25 examined the evolution of HIV-1 drug resistance in patients receiving antiretroviral therapy in Yunnan Province, China. 19 described the prevalence of transmitted drug resistance in children recently diagnosed with HIV-1 infection in France. 23 evaluated the characteristics of treatment-experienced HIV-infected African children and adolescents initiating darunavir and/or etravirine-based antiretroviral treatment. 10 investigated the bioactivation of etravirine to reactive metabolites. 26 investigated the prevalence of rilpivirine and etravirine resistance mutations in HIV-1 Subtype C-infected patients in Botswana.

Benefits and Risks

Benefits Summary

Etravirine is a promising drug that has been shown to be effective in treating HIV-1 infection and has been explored as a potential treatment for other conditions. Research has shown that etravirine is effective against both wild-type HIV and viruses harboring NNRTI resistance and is generally well tolerated. It may also have potential for use in HIV prevention and as a treatment for other viral infections like Zika virus. The drug has also been explored as a potential treatment for triple-negative breast cancer.

Risks Summary

While etravirine has shown promise in research, it's important to consider its potential risks. A major concern is the increasing prevalence of etravirine resistance. This resistance can develop in patients who have been treated with etravirine, and it can also be transmitted from person to person. Another risk is that etravirine can interact with other medications, potentially causing side effects. Additionally, etravirine has been associated with adverse events like skin rashes and hypersensitivity reactions.

Comparison of Studies

Commonalities

These studies all investigated the effectiveness of etravirine or other NNRTIs in treating HIV-1 infection and explored its potential for other uses. They also highlight the growing concern about the development of drug resistance to these therapies.

Differences

The studies varied in their focus, methodology, and the populations they examined. Some focused specifically on etravirine, while others compared it to other NNRTIs or investigated its potential for other applications. Some studies focused on specific populations, like those with liver impairment or children, while others investigated broader patient populations.

Consistency and Contradictions in Results

Overall, the results of these studies demonstrate that etravirine is a potentially valuable tool for treating HIV-1 infection, but they also highlight the importance of understanding and addressing the growing issue of drug resistance. It's important to note that the emergence of resistance is a complex issue that requires ongoing monitoring and research. While some studies have suggested that etravirine may be effective in preventing HIV infection, further research is needed to confirm this.

Implications for Everyday Life

The research on etravirine and other NNRTIs provides valuable insights for individuals living with HIV and their healthcare providers. These findings emphasize the importance of adherence to treatment regimens, regular monitoring for drug resistance, and the ongoing need for research and development of new therapies to combat this evolving virus.

Limitations of Current Research

While these studies offer valuable insights, they also have limitations. The focus on specific populations and drug combinations does not necessarily reflect the broad spectrum of HIV-1 infection and treatment approaches. Further research is needed to explore the long-term effects of etravirine and other NNRTIs, particularly in diverse populations.

Future Research Directions

Future research should focus on developing new strategies to prevent and overcome drug resistance. This could include the development of new drugs that target different parts of the HIV-1 lifecycle, or the development of combination therapies that reduce the likelihood of resistance developing. Additional research is also needed to investigate the potential of repurposing existing drugs for the treatment of other infections, including Zika virus.

Conclusion

Etravirine is a promising NNRTI that has shown effectiveness in treating HIV-1 infection. However, the emergence of drug resistance is a significant challenge that requires ongoing monitoring and research. Efforts to develop new therapies and strategies to prevent and overcome resistance are essential. Individuals living with HIV should work closely with their healthcare providers to ensure they receive appropriate treatment and monitoring. It's vital to continue researching this evolving virus to improve treatment options and find ways to combat this significant global health issue.

Literature analysis of 26 papers
Positive Content
22
Neutral Content
1
Negative Content
3
Article Type
0
0
0
0
26
1.

Effects of hepatic impairment on the steady-state pharmacokinetics of etravirine 200 mg BID: an open-label, multiple-dose, controlled Phase I study in adults.

Author: Schöller-GyüreMonika, KakudaThomas N, De SmedtGoedele, WoodfallBrian, BerckmansCindy, PeetersMonika, HoetelmansRichard M W

No dose adjustment
Well tolerated
Cardiac arrhythmia
Fatigue
Headache
Nausea

No clinically relevant differences were observed between patients with mild or moderate hepatic impairment and healthy matched subjects with regard to the pharmacokinetics of etravirine. No dose adjustment of etravirine appears to be necessary in patients with mild or moderate hepatic impairment.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
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

2.

Therapeutic drug monitoring in treatment-experienced HIV-infected patients receiving darunavir-based salvage regimens: A case series.

Author: LandrySébastien, ChenChi-Nan, PatelNimish, TsengAlice, LalondeRichard G, ThibeaultDenis, SancheSteven, SheehanNancy L

Virologic response

This study examined the clinical value of therapeutic drug monitoring (TDM) in treatment-experienced HIV-1 patients initiating darunavir-based salvage therapy. While the study found that most patients achieved viral suppression, a single patient with the lowest instantaneous inhibitory potential had persistent viral load. Further research is needed to evaluate the predictive value of TDM and the utility of instantaneous inhibitory potential in predicting virologic outcome in this population.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
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

3.

HIV Drug Resistance Mutations in Non-B Subtypes After Prolonged Virological Failure on NNRTI-Based First-Line Regimens in Sub-Saharan Africa.

Author: KityoCissy, ThompsonJennifer, NankyaImmaculate, HoppeAnne, NdashimyeEmmanuel, WarambwaColin, MambuleIvan, van OosterhoutJoep J, Wools-KaloustianKara, BertagnolioSilvia, EasterbrookPhilippa J, MugyenyiPeter, WalkerA Sarah, PatonNicholas I,

HIV treatment
Drug resistance

This study determined drug resistance mutation (DRM) patterns in a large cohort of patients failing nonnucleoside reverse transcriptase inhibitor (NNRTI)-based first-line antiretroviral therapy regimens in programs without routine viral load (VL) monitoring. The study found that non-B subtypes differ in DRMs at first-line failure, which impacts on residual nucleoside reverse transcriptase inhibitor and NNRTI 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

6.

Prevalence in the USA of rilpivirine resistance-associated mutations in clinical samples and effects on phenotypic susceptibility to rilpivirine and etravirine.

Author: PicchioGaston R, RimskyLaurence T, Van EygenVeerle, HaddadMojgan, NapolitanoLaura A, VingerhoetsJohan

Rilpivirine resistance

The prevalence of most known rilpivirine RAMs in the USA, apart from Y181C, was low. Rilpivirine RAMs were often associated with reduced rilpivirine phenotypic 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

9.

Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1.

Author: YangYang, PannecouqueChristophe, ClercqErik De, ZhuangChunlin, ChenFen-Er

Anti-HIV-1 activity

A novel series of oxime-biphenyl-DAPYs were designed and synthesized as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) against HIV-1. Compound 7d demonstrated significant activity against both wild-type and mutant strains, with a higher selectivity index than existing FDA-approved drugs.

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

11.

Suppression of Zika Virus Infection in the Brain by the Antiretroviral Drug Rilpivirine.

Author: SariyerIlker Kudret, GordonJennifer, BurdoTricia H, WolleboHassen S, GiantiEleonora, DonadoniMartina, BellizziAnna, CicaleseStephanie, LoomisRegina, RobinsonJake A, CarnevaleVincenzo, SteinerJoseph, OzdenerMehmet H, MillerAndrew D, AminiShohreh, KleinMichael L, KhaliliKamel

Zika treatment
None

This study demonstrated that rilpivirine (RPV), a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for HIV-1 treatment, inhibits the enzymatic activity of Zika virus (ZIKV) NS5, suppresses ZIKV infection in human astrocytes, and improves clinical outcome in ZIKV-infected mice.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, U.S. Gov't, Non-P.H.S.Research funding provided by US government agencies other than the Public Health Service.

Language : English

12.

Endothelial, inflammatory, coagulation, metabolic effects and safety of etravirine in HIV-uninfected volunteers.

Author: GuptaSamir K, MiDeming, LiuZiyue, SahaChandan

HIV PEP safety
Rash

A pilot study of etravirine in healthy volunteers was conducted to assess its proatherosclerotic properties.

Evaluation StudyResearch that systematically evaluates the effectiveness of a particular program or policy. It measures its outcomes and provides important information for future decision-making.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

13.

Susceptibility of Human Endogenous Retrovirus Type K to Reverse Transcriptase Inhibitors.

Author: Contreras-GalindoRafael, DubeDerek, FujinagaKoh, KaplanMark H, MarkovitzDavid M

HK2 replication inhibition

This study investigated the efficacy of commercially available reverse transcriptase inhibitors (RTIs) in inhibiting the activity of human endogenous retroviruses (HERVs), specifically the HERV type K (HERV-K) HML-2 (HK2) family. The results demonstrated that several nucleoside analogue RTIs effectively blocked HK2 replication, suggesting their potential for suppressing HK2 activity in diseases associated with these viruses.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

14.

Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored "hydrophobic channel".

Author: ZhouZhongxia, LiuTao, KangDongwei, HuoZhipeng, WuGaochan, DaelemansDirk, De ClercqErik, PannecouqueChristophe, ZhanPeng, LiuXinyong

HIV-1 NNRTI activity

A new series of diarylpyrimidines (DAPYs) were synthesized and evaluated as novel HIV-1 NNRTIs. They were active against the HIV-1 wild-type (WT) strain with EC50 values ranging from 3 nM to 63 nM and displayed significantly reduced cytotoxicity.

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

Language : English

15.

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Author: KangDongwei, FangZengjun, HuangBoshi, LuXueyi, ZhangHeng, XuHaoran, HuoZhipeng, ZhouZhongxia, YuZhao, MengQing, WuGaochan, DingXiao, TianYe, DaelemansDirk, De ClercqErik, PannecouqueChristophe, ZhanPeng, LiuXinyong

Antiviral potency
HIV-1 inhibition
Promising drug candidate

This study designed, synthesized, and biologically tested new derivatives of piperidine-substituted thiophene[3,2-d]pyrimidine HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTI). Some of the synthesized compounds displayed single-digit nanomolar anti-HIV potencies. Compound 25a was exceptionally potent against a panel of NNRTI-resistant mutant viruses.

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.

Emergence of uncommon HIV-1 non-B subtypes and circulating recombinant forms and trends in transmission of antiretroviral drug resistance in patients with primary infection during the 2013-2015 period in Marseille, Southeastern France.

Author: TamaletCatherine, Tissot-DupontHervé, MotteAnne, TourrèsChristian, DhiverCatherine, RavauxIsabelle, Poizot-MartinIsabelle, DiengThérèse, TomeiChristelle, BregigeonSylvie, Zaegel-FaucherOlivia, LarocheHélène, AherfiSarah, MokhtariSaadia, ChaudetHervé, MénardAmelie, BrouquiPhilippe, SteinAndreas, ColsonPhilippe

Drug resistance

This study assessed the prevalence of non-B HIV-1 subtypes and antiretroviral resistance-associated mutations (RAMs) among patients with primary HIV-1 infections (PHI) in Southeastern France. The proportion of non-B subtypes increased significantly, particularly in 2011-2013. The prevalence of protease, nucleos(t)ide reverse transcriptase, and first-generation nonnucleoside reverse transcriptase inhibitors-associated RAMs was 1.7%, 5.2%, and 5.2%, respectively. Men who have sex with men (MSM) were more frequently infected with drug-resistant viruses than other patients. These findings suggest that prevention strategies and therapies should consider the recent increase in rare HIV-1 strains and the spread of drug-resistant HIV-1.

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

20.

Prevalence of rilpivirine resistance in people starting antiretroviral treatment in Argentina.

Author: BissioEmiliano, BarbásMaria G, KademiánSilvia, BouzasMaria B, SalomónHoracio, CudoláAnalia, GiulianoSilvina Fernández, FalistoccoCarlos

NNRTI resistance

This study analyzes the prevalence of resistance mutations to newer generation non-nucleoside reverse transcriptase inhibitors (NNRTIs) in HIV-infected patients starting antiretroviral therapy (ART) in Argentina.

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

Language : English

22.

Exploring the potential of approved drugs for triple-negative breast cancer treatment by targeting casein kinase 2: Insights from computational studies.

Author: ShoaibTagyedeen H, IbraheemWalaa, AbdelrahmanMohammed, OsmanWadah, SherifAsmaa E, AshourAhmed, IbrahimSabrin R M, GhazawiKholoud F, MiskiSamar F, AlmadaniSara A, ALsiyudDuaa Fahad, MohamedGamal A, AlzainAbdulrahim A

Anti-tumor agent

This study evaluated the potential of seven approved drugs as therapeutic agents against human ck2 alpha kinase, a key driver of triple-negative breast cancer (TNBC) metastasis and invasiveness. In silico analysis identified etravirine, an FDA-approved antiviral drug, as the most promising candidate. Molecular docking and simulations indicated a stable and reliable binding mode with the protein, suggesting potential antitumor activity. Further investigation into the use of etravirine, potentially through gold nanocarriers, is warranted.

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

23.

Characteristics of Treatment-experienced HIV-infected African Children and Adolescents Initiating Darunavir and/or Etravirine-based Antiretroviral Treatment.

Author: CorriganBethany, MukuiIrene, MulengaLloyd, MthethwaNobuhle, LetsieMosilinyane, BrunoStephanie, RakhmaninaNatella

Drug donation program
Pediatric ART

This study evaluated characteristics of African pediatric patients initiated on darunavir (DRV) and/or etravirine (ETR) for the treatment of HIV/AIDS.

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

24.

Discovery of Novel Dihydrothiopyrano[4,3-<i>d</i>]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles.

Author: WangZhao, ZalloumWaleed A, WangWenbo, JiangXiangyi, De ClercqErik, PannecouqueChristophe, KangDongwei, ZhanPeng, LiuXinyong

HIV-1 treatment
antiviral activity
dihydrothiopyrano[4
3-d]pyrimidine

This study designed a novel series of dihydrothiopyrano[4,3-d]pyrimidine derivatives as potential anti-HIV-1 agents. Compound 20a exhibited potent antiviral activity against various HIV-1 strains, improved resistance profiles, reduced cytotoxicity, and favorable drug-like properties.

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

25.

Drug resistance evolution in patients with human immunodeficiency virus-1 under long-term antiretroviral treatment-failure in Yunnan Province, China.

Author: LiJianjian, XuYawen, LiuJiafa, YangBihui, YangCuixian, ZhangMi, DongXingqi

HIV-1 treatment
Drug resistance

This study analyzes the prevalence and evolution of HIV-1 drug resistance (DR) in Yunnan, China, to provide insight into the occurrence and development of resistance and inform strategies to delay resistance and achieve successful individualized treatment.

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

26.

Prevalence of Rilpivirine and Etravirine Resistance Mutations in HIV-1 Subtype C-Infected Patients Failing Nevirapine or Efavirenz-Based Combination Antiretroviral Therapy in Botswana.

Author: DiphokoThabo, GaseitsiweSimani, KasvosveIshmael, MoyoSikhulile, OkatchHarriet, MusondaRosemary, WainbergMark, MakhemaJoseph, MarlinkRichard, NovitskyVladimir, EssexMax

Cross-resistance risk
HIV drug resistance

This study investigated the prevalence of HIV-1 drug resistance mutations (DRMs) to rilpivirine (RPV) and etravirine (ETR) in Botswana. High prevalence of RPV and ETR DRMs was found even though these drugs have not been used in Botswana. This highlights the importance of genotyping patients with prior exposure to nevirapine or efavirenz before prescribing RPV- or ETR-containing therapies.

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

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