Drugs

Fostemsavir

Fostemsavir

Other Names: BMS-663068, FTR, GSK3684934, fostemsavir tromethamine, prodrug of BMS-626529, prodrug of GSK2616713, prodrug of temsavir Drug Class: gp120 Attachment Inhibitor Molecular Formula: C25 H26 N7 O8 P Registry Number: 864953-29-7 (CAS) Chemical Name: Piperazine, 1-benzoyl-4-((4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-((phosphonooxy)methyl)-1H-pyrrolo(2,3-c)pyridin-3-yl)oxoacetyl)- Chemical Class: Pyridines and derivatives Organization: ViiV Healthcare Phase of Development: Fostemsavir is in Phase 3 development for HIV treatment.

(Compound details obtained from ChemIDplus Advanced,1 NIAID Therapeutics Database,2 DrugBank,3 and HIV Treatment Bulletin article4)

What is fostemsavir?

What is fostemsavir?

Fostemsavir (GSK3684934) is an investigational drug that is being studied to treat HIV infection.5

Fostemsavir belongs to a group of HIV drugs called gp120 attachment inhibitors.4 By attaching to the gp120 protein on the outer surface of HIV, fostemsavir blocks HIV from getting into and infecting the immune cells.6

Fostemsavir is a prodrug, which means that it is an inactive drug. Once taken, a prodrug does not work until the body converts it into an active form. In the body, fostemsavir is converted to temsavir (GSK2616713).5–7

To learn about how investigational drugs are tested during clinical trials, read the AIDSinfo What is an Investigational HIV Drug? and HIV/AIDS Clinical Trials fact sheets.

Which clinical trials are studying fostemsavir?

Which clinical trials are studying fostemsavir?

Study Names: AI438-006; NCT01009814
Phase: 2a
Status: This study has been completed.
Location: Germany
Purpose: The purpose of this study was to evaluate the safety and effectiveness of fostemsavir, given with and without the HIV medicine ritonavir (brand name: Norvir).8

Study Names: AI438-011; NCT01384734
Phase: 2b
Status: This study has been completed.
Locations: Multiple countries, including United States
Purpose: The purpose of this study was to evaluate the safety and effectiveness of four different doses of fostemsavir and to compare fostemsavir to the FDA-approved protease inhibitor atazanavir (brand name: Reyataz) boosted with ritonavir.9

Study Names: BRIGHTE; AI438-047; NCT02362503
Phase: 3
Status: This study is ongoing, but not recruiting participants.
Locations: North America, South America, Europe, Asia, Africa, and Australia
Purpose: The purpose of this study is to evaluate the safety and effectiveness of fostemsavir.10

For more details on the studies listed above, see the Health Professional version of this drug summary.

What side effects might fostemsavir cause?

What side effects might fostemsavir cause?

One goal of HIV research is to identify new drugs that have fewer side effects. The following side effects were observed in the studies of fostemsavir listed above.

AI438-006 study (NCT01009814):
In this Phase 2a study, the most common side effects were headache, rash, and urinary urgency. Most instances of these side effects were mild.6,8

AI438-011 study (NCT01384734):
In this Phase 2b study, mild headache and nausea were the most common side effects. Treatment-related serious side effects occurred in one participant receiving fostemsavir. There were no cases of fostemsavir-related side effects that led to participants dropping out of the study.11

BRIGHTE (NCT02362503):
A safety analysis at Week 96 found that 94% of participants experienced at least one side effect during this Phase 3 study, though most were mild in severity. Moderate to severe side effects occurred in 21% of participants and included nausea, diarrhea, headache, immune reconstitution inflammatory syndrome (IRIS), vomiting, fatigue, and weakness or lack of energy. Twelve participants had serious side effects that were related to treatment with fostemsavir, and seven percent of participants had side effects that caused them to leave the study.12

 Because fostemsavir is still being studied, information on possible side effects of the drug is not complete. As testing of fostemsavir continues, additional information on possible side effects will be gathered.

Where can I get more information about clinical trials studying fostemsavir?

Where can I get more information about clinical trials studying fostemsavir?

More information about fostemsavir-related research studies is available from the AIDSinfo database of ClinicalTrials.gov study summaries. Click on the title of any trial in the list to see the ClinicalTrials.gov trial summary and more information about the study.

Some clinical trials may be looking for volunteer participants. Your health care provider can help you decide whether participating in a clinical trial is right for you. For more information, visit NIH Clinical Research Trials and You.

References

References

  1. United States National Library of Medicine. ChemIDplus Advanced: Fostemsavir. https://chem.nlm.nih.gov/chemidplus/rn/864953-29-7. Accessed November 6, 2019
  2. National Institute of Allergy and Infectious Diseases (NIAID). NIAID ChemDB, HIV Drugs in Development. https://chemdb.niaid.nih.gov/DrugDevelopmentHIV.aspx. Accessed November 6, 2019
  3. DrugBank. Fostemsavir. https://www.drugbank.ca/drugs/DB11796. Accessed November 6, 2019
  4. Collins S and Clayden P, eds. HIV pipeline 2019: new drugs in development. HIV Treatment Bulletin. 2019 Jul; 20(1) Suppl: 1-10. HIV Treatment Bulletin. http://i-base.info/htb/wp-content/uploads/2019/07/PIPELINE-2019-FINAL-full-version.pdf. Accessed November 6, 2019
  5. Llamoso C, Bogner JR, Afonina L, et al. HIV-1 attachment inhibitor prodrug BMS-663068 in antiretroviral-experienced subjects: Week 96 safety analysis. International Congress of Drug Therapy in HIV Infection (HIV Glasgow); October 23-26, 2016; Glasgow, UK. http://natap.org/2016/GLASGOW/GLASGOW_32.htm. Accessed November 6, 2019
  6. Nettles RE, Schürmann D, Zhu L, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012;206(7). https://academic.oup.com/jid/article/206/7/1002/805849. Accessed November 6, 2019
  7. United States National Library of Medicine. ChemIDplus Advanced: Temsavir. https://chem.nlm.nih.gov/chemidplus/rn/701213-36-7. Accessed November 6, 2019
  8. ViiV Healthcare. Randomized, open label, multiple-dose study to evaluate the pharmacodynamics, safety and pharmacokinetics of BMS-663068 in HIV-1 infected subjects. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on November 6, 2009. NLM Identifier: NCT01009814. https://clinicaltrials.gov/ct2/show/NCT01009814. Accessed November 6, 2019
  9. ViiV Healthcare. A Phase IIb randomized, controlled, partially-blinded trial to investigate safety, efficacy and dose-response of BMS-663068 in treatment-experienced HIV-1 subjects, followed by an open-label period on the recommended dose. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on June 23, 2011. NLM Identifier: NCT01384734. https://clinicaltrials.gov/ct2/show/NCT01384734. Accessed November 6, 2019
  10. ViiV Healthcare. A multi-arm Phase 3 randomized placebo controlled double blind clinical trial to investigate the efficacy and safety of BMS-663068 in heavily treatment experienced subjects infected with multi-drug resistant HIV-1. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on February 9, 2015. NLM Identifier: NCT02362503. https://clinicaltrials.gov/ct2/show/NCT02362503. Accessed November 6, 2019
  11. Thompson M, Urbina FM, Latiff G, et al. Long-term safety and efficacy of fostemsavir in treatment-experienced participants living with HIV-1. Poster presented at: Conference on Retroviruses and Opportunistic Infections (CROI); March 4-7, 2019; Seattle, WA. Poster 483. https://www.croiconference.org/sites/default/files/posters-2019/1430_Thompson_0483.pdf. Accessed November 6, 2019
  12. Lataillade M, Lalezari J, Aberg J, et al. Week 96 safety and efficacy of the novel HIV-1 attachment inhibitor prodrug fostemsavir in heavily treatment-experienced participants infected with multi-drug-resistant HIV-1 (BRIGHTE study). Slides presented at: International AIDS Society (IAS) Conference on HIV Science; July 21-24, 2019; Mexico City, Mexico. http://programme.ias2019.org/PAGMaterial/PPT/1166_3381/IAS%20Brighte%20Week%2096%20oral_with%20link%20for%20sharing.pptx. Accessed November 6, 2019

Last Reviewed: November 6, 2019

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