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AIDSinfo Drug Database

AIDSinfo Drug Database

Drugs by class

FDA-approved

Investigational

Astodrimer  Audio icon

Other Names: SPL-7013, VivaGel, astodrimer sodium
Drug Class: Microbicides
Molecular Formula: C583 H641 N63 O287 S64
Registry Number: 137946-42-5 (CAS)
Chemical Name: N2,N6-bis(N2,N6-bis(N2,N6-bis(N2,N6-bis(N2,N6-bis((3,6-disulfonaphthalen-1-yloxy)acetyl)-l-lysyl)-l-lysyl)-l-lysyl)-l-lysyl)-N1-(diphenylmethyl)-l-lysinamide
Chemical Class: Dendrimers
Company: Starpharma
Phase of Development: Phase I/II
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(Compound details obtained from ChemIDplus Advanced1 and NIAID Therapeutics Database2)

What is an investigational drug?

An investigational drug is one that is under study and is not approved by the U.S. Food and Drug Administration (FDA) for sale in the United States. Medical research studies are conducted to evaluate the safety and effectiveness of an investigational drug. These research studies are also called clinical trials. Once an investigational drug has been proven safe and effective in clinical trials, FDA may approve the drug for sale in the United States.

What is astodrimer?

Astodrimer (brand name: VivaGel) is an investigational drug that has been studied to prevent sexual transmission of HIV and herpes simplex virus type 2 (HSV-2).3 It is a type of drug product called a topical microbicide. Topical microbicides are products that are applied to the vagina or rectum (such as gels, films, or creams) or inserted into the vagina (such as vaginal rings) to prevent getting sexually transmitted infections, such as HIV infection.4,5

Astodrimer belongs to a group of drugs called polyanion-based entry inhibitors.6 Polyanion-based entry inhibitors interact through an electrostatic association with the surface of viruses such as HIV. The interaction between the negatively charged surface of a polyanion-based entry inhibitor and HIV’s positively charged surface may prevent HIV from attaching to, entering, or infecting healthy cells.7-9

Astodrimer is currently developed as a gel for vaginal use.3 In addition to being studied for preventing HIV and HSV-2 transmission, astodrimer gel has also been studied for treating bacterial vaginosis. Bacterial vaginosis is an infection that causes unwanted overgrowth of certain bacteria in the vagina. Under the brand name VivaGel® BV, astodrimer was approved in 2015 for marketing in the European Union for treating and managing bacterial vaginosis. Astodrimer gel is currently being studied for preventing recurrent bacterial vaginosis.10-13

How do topical microbicides work?

Topical microbicides can also be referred to as topical pre-exposure prophylaxis (PrEP) products.4,5 PrEP means using a medicine before possible exposure to a virus or bacteria to reduce the risk of becoming infected with the virus or bacteria.

Topical microbicides to prevent HIV infection are designed to work close to where they are applied and near to where HIV might enter the body (through the vagina or rectum).5,14

Early development of microbicides focused on products that used non-antiretroviral (ARV) medicines. These products worked in various ways, such as by inactivating pathogens, strengthening the body’s natural defenses, or blocking virus from getting into healthy cells.15-17

Current microbicide research is mainly focused on testing products that contain ARV medicines. ARV-based microbicides work at a particular step in the HIV life cycle and act almost exclusively against HIV. They may contain more than one ARV medicine to help make the product more effective. ARV-based microbicides might:

  • prevent HIV entry into healthy cells
  • prevent HIV from converting its RNA into DNA, which stops HIV from replicating
  • prevent HIV from inserting its genetic material into the DNA of host cells, which stops HIV from replicating
  • prevent HIV from becoming a mature virus that can infect healthy cells.15,18,19

Astodrimer works by blocking HIV from getting into healthy cells.3,6

How are clinical trials of investigational drugs conducted?

Clinical trials are conducted in phases. Each phase has a different purpose and helps researchers answer different questions.20

  • Phase I trials: Researchers test an investigational drug in a small group of people (20–80) for the first time. The purpose is to evaluate its safety and identify side effects.
  • Phase II trials: The investigational drug is administered to a larger group of people (100–300) to determine its effectiveness and to further evaluate its safety.
  • Phase III trials: The investigational drug is administered to large groups of people (1,000–3,000) to confirm its effectiveness, monitor side effects, compare it with standard or equivalent treatments, and collect information that will allow the investigational drug to be used safely.20

In most cases, an investigational drug must be proven effective and must show continued safety in a Phase III clinical trial to be considered for approval by FDA for sale in the United States. Some drugs go through FDA’s accelerated approval process and are approved before a Phase III clinical trial is complete. After a drug is approved by FDA and made available to the public, researchers track its safety in Phase IV trials to seek more information about the drug’s risks, benefits, and optimal use.20

In what phase of testing is astodrimer?

Astodrimer gel for preventing transmission of HIV and HSV-2 has been studied in Phase I/II clinical trials.2

What are some studies on astodrimer?

Study Name: MTN-004 (SPL7013-006; NCT00442910); ATN 062 (NCT00490152)
Phase: I
Location: United States and Puerto Rico
Participants: Sexually active women not infected with HIV or any other sexually transmitted infection (STI)
Purpose: The purpose of MTN-004 was to look at the safety and acceptability of astodrimer vaginal gel used over 14 days. (In this study, acceptability referred to overall product like or dislike and the likelihood of future gel use.)
Note: While MTN-004 was ongoing, researchers expanded the gel acceptability assessment in women participating in this study by simultaneously conducting a study known as ATN 062. ATN 062 gathered acceptability data by using questionnaires, teleconferences, and an interactive voice reporting system through which women reported their experiences with using the study gels.21-24

For more details on this study, see the Health Professional version.




Study Name: SPL7013-004; NCT00331032
Phase: I
Location: United States and Kenya
Participants: Sexually abstinent (but previously sexually active) women not infected with HIV or any other STI
Purpose: The purpose of this study was to look at the safety of astodrimer gel when used twice a day for 14 days.25-27

For more details on this study, see the Health Professional version.




Study Name: SPL7013-003; NCT00740584
Phase: I/II
Location: Australia
Participants: Women not infected with HIV or any other STI
Purpose:The purpose of this study was to look at the antiviral activity of single doses of astodrimer gel used on five separate occasions that were at least 5 days apart.3,28

For more details on this study, see the Health Professional version.

Additional studies of astodrimer gel have also been completed.

What side effects might astodrimer cause?

In the three studies discussed under the previous question, mild genitourinary side effects associated with astodrimer gel use were common.3,21,26 The most common genitourinary side effects in the MTN-004 (SPL7013-006) study were difficult or painful sexual intercourse, bleeding or spotting between menstrual periods, and genital/vaginal burning or itching.21 Other side effects that have been associated with astodrimer gel use include mild damage to the vaginal/cervical tissue lining, bacterial vaginosis, and vaginal yeast infection.3,27

Information on possible side effects of the drug product is not complete. As testing of astodrimer gel continues, additional information on possible side effects will be gathered.

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

More information about astodrimer-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.

 

I am interested in participating in a clinical trial of astodrimer. How can I find more information about participating in a clinical trial?

Participating in a clinical trial can provide benefits. For example, a volunteer participant can benefit from new research treatments before they are widely available. Participants also receive regular and careful medical attention from a research team that includes doctors and other health professionals. However, clinical trials may also involve risks of varying degrees, such as unpleasant, serious, or even life-threatening side effects from the treatment being studied.20

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

  1. United States National Library of Medicine. ChemIDplus Advanced. Available at: http://chem.sis.nlm.nih.gov/chemidplus/rn/1379746-42-5. Last accessed on May 15, 2016.
  2. National Institute of Allergy and Infectious Diseases (NIAID). NIAID ChemDB, HIV Drugs in Development. Available at: http://chemdb.niaid.nih.gov/DrugDevelopmentHIV.aspx. Last accessed on May 15, 2016.
  3. Price CF, Tyssen D, Sonza S, et al. SPL7013 Gel (VivaGel®) Retains Potent HIV-1 and HSV-2 Inhibitory Activity following Vaginal Administration in Humans. PLoS One. 2011;6(9):e24095. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3174146/. Last accessed on May 15, 2016.
  4. National Institute of Allergy and Infectious Diseases (NIAID). NIAID Research on Microbicides. Available at: http://www.niaid.nih.gov/topics/hivaids/research/prevention/pages/topicalmicrobicides.aspx. Last accessed on May 15, 2016.
  5. Shattock RJ, Rosenberg Z. Microbicides: Topical Prevention against HIV. Cold Spring Harb Perspect Med. 2012 Feb;2(2):a007385. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3281595/. Last accessed on May 15, 2016.
  6. Sonza S, Johnson A, Tyssen D, et al. Enhancement of Human Immunodeficiency Virus Type 1 Replication is Not Intrinsic to All Polyanion-Based Microbicides. Antimicrob Agents Chemother. 2009 Aug;53(8):3565-8. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2715623/. Last accessed on May 15, 2016.
  7. International Partnership for Microbicides (IPM) website. Glossary: Polyanion. Available at: http://www.ipmglobal.org/our-work/glossary/polyanion. Last accessed on May 15, 2016.
  8. Fletcher PS, Wallace GS, Mesquita PM, Shattock RJ. Candidate polyanion microbicides inhibit HIV-1 infection and dissemination pathways in human cervical explants. Retrovirology. 2006 Aug 1;3:46. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1590048/. Last accessed on May 15, 2016.
  9. Garg AB, Nuttall J, Romano J. The future of HIV microbicides: challenges and opportunities. Antivir Chem Chemother. 2009;19(4):143-50. Available at: http://www.intmedpress.com/serveFile.cfm?sUID=a04ed6be-7c85-4bc7-9f9d-b9f5e9290a52. Last accessed on May 15, 2016.
  10. Starpharma: News Release, dated November 28, 2012. VivaGel phase 3 study results. Available at: http://www.starpharma.com/news/139. Last accessed on May 15, 2016.
  11. Starpharma Pty Ltd. A Phase 3, Double-blind, Multicentre, Randomised, Placebo-controlled Study to Determine the Efficacy and Safety of SPL7013 Gel to Prevent the Recurrence of Bacterial Vaginosis. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on September 5, 2014. NLM Identifier: NCT02237950. Available at: https://www.clinicaltrials.gov/ct2/show/NCT02237950. Last accessed on May 15, 2016.
  12. Starpharma Pty Ltd. A Phase 3, Double-blind, Multicentre, Randomised, Placebo-controlled Study to Determine the Efficacy and Safety of SPL7013 Gel to Prevent the Recurrence of Bacterial Vaginosis. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on September 5, 2014. NLM Identifier: NCT02236156. Available at: https://www.clinicaltrials.gov/ct2/show/NCT02236156. Last accessed on May 15, 2016.
  13. Starpharma: News Release, dated September 24, 2015. EU Marketing Approval Granted for VivaGel® BV. Available at: http://www.starpharma.com/news/253. Last accessed on May 15, 2016.
  14. Cranage M, Sharpe S, Herrera C, et al. Prevention of SIV Rectal Transmission and Priming of T Cell Responses in Macaques after Local Pre-exposure Application of Tenofovir Gel. PLoS Med. 2008 Aug 5;5(8):e157; discussion e157. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2494562/. Last accessed on May 15, 2016.
  15. Global Campaign for Microbicides website. About Microbicides—How do they work? Available at: http://www.global-campaign.org/the_science.htm#work. Last accessed on May 15, 2016.
  16. CONRAD website. Microbicide Development. Available at: http://www.conrad.org/microbicides.html. Last accessed on May 15, 2016.
  17. CONRAD website. Microbicide Mechanisms of Action. Available at: http://www.conrad.org/microbicides-research-mechanisms.html. Last accessed on May 15, 2016.
  18. Global Campaign for Microbicides. Antiretroviral (ARV)-Based Microbicides: The Promise and the Puzzle; 2010. Available at: http://www.global-campaign.org/clientfiles/FS-ARV-BasedMicrobicides[E].pdf. Last accessed on May 15, 2016.
  19. International Partnership for Microbicides (IPM) website. How ARV-based Microbicides Work. Available at: http://www.ipmglobal.org/why-microbicides/how-arv-based-microbicides-work. Last accessed on May 15, 2016.
  20. National Institutes of Health (NIH). NIH Clinical Research Trials and You. Available at: http://www.nih.gov/health-information/nih-clinical-research-trials-you. Last accessed on May 15, 2016.
  21. McGowan I, Gomez K, Bruder K, et al. Phase 1 Randomized Trial of the Vaginal Safety and Acceptability of SPL7013 Gel (VivaGel®) in Sexually Active Young Women (MTN-004). AIDS. 2011 May 15;25(8):1057-64. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3103767/. Last accessed on May 15, 2016.
  22. Starpharma Pty Ltd. Phase 1 Study of the Safety and Acceptability of 3% w/w SPL7013 Gel (VivaGel™) Applied Vaginally in Sexually Active Young Women. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on March 2, 2007. NLM Identifier: NCT00442910. Available at: https://www.clinicaltrials.gov/ct2/show/NCT00442910. Last accessed on May 15, 2016.
  23. Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD). Microbicide-Use Adherence, Acceptability, and Attitudes Among Sexually Active Young Women Participating in a Phase I Microbicide Trial (MTN 004) "Tell Juliana". In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on June 21, 2007. NLM Identifier: NCT00490152. Available at: https://www.clinicaltrials.gov/ct2/show/NCT00490152. Last accessed on May 15, 2016.
  24. Carballo-Diéguez A, Giguere R, Dolezal C, et al. "Tell Juliana": Acceptability of the Candidate Microbicide VivaGel® and Two Placebo Gels among Ethnically Diverse, Sexually Active Young Women Participating in a Phase 1 Microbicide Study. AIDS Behav. 2012 Oct;16(7):1761-74. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3272128/. Last accessed on May 15, 2016.
  25. National Institute of Allergy and Infectious Diseases (NIAID). An Expanded Phase I Randomized Placebo Controlled Trial of the Safety and Tolerability of 3 Percent w/w SPL7013 Gel (VivaGel™) in Healthy Young Women When Administered Twice Daily for 14 Days. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on May 25, 2006. NLM Identifier: NCT00331032. Available at: https://www.clinicaltrials.gov/ct2/show/NCT00331032. Last accessed on May 15, 2016.
  26. Cohen CR, Brown J, Moscicki AB, et al. A Phase I Randomized Placebo Controlled Trial of the Safety of 3% SPL7013 Gel (VivaGel®) in Healthy Young Women Administered Twice Daily for 14 Days. PLoS One. 2011 Jan 20;6(1):e16258. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3024437/. Last accessed on May 15, 2016.
  27. Moscicki AB, Kaul R, Ma Y, et al. Measurement of mucosal biomarkers in a phase 1 trial of intravaginal 3% SPL 7013 gel (VivaGel®) to assess expanded safety. J Acquir Immune Defic Syndr. 2012 Feb 1;59(2):134-40. Available at: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3261360/. Last accessed on May 15, 2016.
  28. Starpharma Pty Ltd. Assessment of Local Retention and Duration of Activity of SPL7013 Following Vaginal Application of 3% SPL7013 Gel (VivaGel) in Healthy Volunteers. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on August 21, 2008. NLM Identifier: NCT00740584. Available at: https://www.clinicaltrials.gov/ct2/show/NCT00740584. Last accessed on May 15, 2016.


Last Reviewed: May 15, 2016

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