Emtricitabine/tenofovir explained

Verifiedrevid:447540265
Type:combo
Width:250
Component1:Emtricitabine
Class1:Nucleoside reverse transcriptase inhibitor
Component2:Tenofovir disoproxil
Class2:Nucleotide analogue reverse transcriptase inhibitor
Tradename:Truvada, others
Dailymedid:Truvada
Pregnancy Au:B3
Routes Of Administration:By mouth
Atc Prefix:J05
Atc Suffix:AR03
Legal Au:S4
Legal Au Comment:[1]
Legal Ca:Rx-only
Legal Uk:POM
Legal Us:Rx-only
Legal Eu:Rx-only
Legal Eu Comment:[2]
Legal Status:Rx-only
Cas Number:731772-45-5
Pubchem:11954236
Kegg:D02297
Niaid Chemdb:214126
Synonyms:Emtricitabine/tenofovir disoproxil fumarate

Emtricitabine/tenofovir, sold under the brand name Truvada among others, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS.[3] [4] It contains the antiretroviral medications emtricitabine and tenofovir disoproxil. For treatment, it must be used in combination with other antiretroviral medications.[5] For prevention before exposure, in those who are at high risk, it is recommended along with safer sex practices. It does not cure HIV/AIDS.[3] Emtricitabine/tenofovir is taken by mouth.

Common side effects include headache, tiredness, trouble sleeping, abdominal pain, weight loss, and rash.[3] Serious side effects may include high blood lactate levels and enlargement of the liver. Use of this medication during pregnancy does not appear to harm the fetus, but this has not been well studied.[6]

Emtricitabine/tenofovir was approved for medical use in the United States in 2004.[3] It is on the World Health Organization's List of Essential Medicines.[7] In the United States, emtricitabine/tenofovir was under patent by Gilead until 2020, but is now available as a generic worldwide.[8] In 2020, it was the 278th most commonly prescribed medication in the United States, with more than 1million prescriptions.[9] [10]

Medical uses

Emtricitabine/tenofovir is used both to treat and to prevent HIV/AIDS.[3] The U.S. National Institutes of Health (NIH) recommends antiretroviral therapy (ART) for all people with HIV/AIDS.[11]

HIV prevention

The Centers for Disease Control and Prevention (CDC) recommends the use of emtricitabine/tenofovir for pre-exposure prophylaxis (PrEP) for uninfected, HIV-1 negative individuals that may be at risk for HIV-1 infection.[12] [13] A Cochrane systematic review found a 51% relative risk reduction of contracting HIV with both tenofovir alone and the tenofovir/emtricitabine combination.[14] A JAMA systematic review found a similar relative risk reduction of 54% on average and greater reduction with greater adherence.[15] It was approved for PrEP against HIV infection in the United States in 2012.[16]

The CDC recommends PrEP be considered for the following high-risk groups:[17]

The consideration of utilizing emtricitabine/tenofovir as a reduction strategy involves discussion with a health professional who can help the patient navigate the benefits and risks. Patients are advised to discuss any history of bone issues, kidney issues, or hepatitis B infection with their healthcare provider.[18] Effectiveness of PrEP for prevention of infection is reliant on an individual's ability to take the medication consistently.[19]

Emtricitabine/tenofovir is also used for HIV post-exposure prophylaxis. People who start taking emtricitabine/tenofovir see HIV reduction benefits up to 72 hours after starting, but the medicine must be taken for thirty days after a high-risk sexual event to ensure HIV transmission levels are optimally reduced.[20] [21]

Emtricitabine/tenofovir as PrEP should not be used for individuals who are positive for HIV-1.

HIV treatment

Emtricitabine/tenofovir has been approved in the United States as part of antiretroviral combination therapy for the treatment of HIV-1. The combination therapy is suggested as one of the options for adults who have not received any prior treatment for HIV infection.[22]

Hepatitis B

Both emtricitabine and tenofovir are indicated for the treatment of hepatitis B, with the added benefit that they can target HIV for those with co-infection.[23] Emtricitabine/tenofovir may also be considered for some antiviral resistant hepatitis B infections.[24]

Pregnancy and breastfeeding

In the United States, it is recommended that all pregnant HIV-infected women start antiretroviral therapy (ART) as early in pregnancy as possible to reduce the risk of transmission. ART generally does not increase risk of birth defects with exception of dolutegravir, which is not recommended during first trimester of pregnancy only due to potential risk of neural tube defects.[25]

Emtricitabine/tenofovir is secreted in breast milk.[26] In developed countries, HIV-infected mothers are generally recommended to not breastfeed due to slight risk of mother-to-children HIV transmission.[27] [28] In developing countries, where avoiding breastfeeding may not be an option, the World Health Organization recommends a triple drug regimen of tenofovir, efavirenz, and either lamivudine or emtricitabine.[28]

Side effects

Emtricitabine/tenofovir is generally well tolerated. Some of its side effects include:

Fat redistribution and accumulation (lipodystrophy) has been observed in people receiving antiretroviral therapy, including fat reductions in the face, limbs, and buttocks and increases in visceral fat of the abdomen and accumulations in the upper back. When used as pre-exposure prophylaxis (PrEP) this effect may not be present.[29] Weight changes have however been linked to the medication.[30]

Drug interactions

Drug-drug Interaction!Coadministration
TenofovirDidanosine
  • May increase didanosine concentration and risk of didanosine toxicity (e.g. pancreatitis, neuropathy).
  • Discontinue didanosine if patient develops didanosine-associated adverse events.
  • For patients who weigh more than 60 kg, didanosine dose should be reduced to 250 mg; there is no available data to recommend didanosine dose adjustments in patients who weigh less than 60 kg.
Atazanavir
  • May decrease atazanavir and increase tenofovir concentrations.
  • Atazanavir should only be taken together with emtricitabine/tenofovir with ritonavir.
  • Monitor for tenofovir toxicity.
Lopinavir/ritonavir, atazanavir coadministered with ritonavir & darunavir coadministered with ritonavir
  • May increase tenofovir concentrations.
Ledipasvir/sofosbuvir
  • May increase tenofovir concentrations.
  • Consider alternative Hepatitis C antiviral or antiretroviral therapy.
  • Monitor for tenofovir toxicity.
Emtricitabine/tenofovirP-glycoprotein and breast cancer resistance protein (BCRP) transporters inhibitors
  • May increase absorption of emtricitabine/tenofovir.
Drugs may decrease renal function (e.g. acyclovir, adefovir, dipivoxil, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides, etc.)
  • May increase emtricitabine and/or tenofovir concentrations.
High-dose or multiple NSAIDs
Orlistat
  • May inhibit the absorption of emtricitabine/tenofovir and result in loss of viral control.[31]
  • Monitor HIV viral load frequently while the patient is taking orlistat.
  • Discontinue orlistat if HIV viral load increases.
Other drugs with adverse reactions include dabigatran etexilate, lamivudine, and vincristine. Dabigatran etexilate used with p-glycoprotein inducers requires monitoring of decreased levels and effects of dabigatran. Lamivudine may increase the adverse or toxic effect of emtricitabine. Vincristine used with P-glycoprotein/ABCB1 inducers can decrease the serum concentration of vincristine.[32]

Society and culture

The patent for the drug combination is owned by Gilead Sciences in some regions. The European patent EP0915894B1[33] expired in July 2018, Gilead Sciences wished the patent to be extended, however "four rival labs—Teva, Accord Healthcare, Lupin and Mylan—had sought to have that overturned in the courts in Britain", the High Court of England and Wales invalidated Gilead's patent,[34] however the company appealed [35] and the UK referred the case to the European Court of Justice who refused to extend the patent.[36] An Irish court rejected an injunction request to prevent the launch of generic Emtricitabine/tenofovir prior to the resolution of the case.[37] [38] Despite the expiration of the Gilead Sciences patent, as of 2021, there are still widespread challenges to the availability and uptake of generic PrEP throughout Europe. [39]

In 2019, Gilead Sciences challenged the validity of patents granted to the United States after 2015 for using the drug combination for HIV PrEP and post-exposure prophylaxis (PEP).[40] [41] [42] . In July 2024, The Biden administration appealed the jury finding that ruled in favor of Gilead Sciences verdict that the U.S. government’s patents are invalid.[43]

In the United States, most healthcare plans are required to cover PrEP without any copay or other cost sharing. This is due to a United States Preventive Services Task Force recommendation that gave PrEP a grade A rating. Under the Affordable Care Act, this recommendation requires all non-grandfathered private health plans to cover PrEP without cost sharing.[44] [45]

In the United Kingdom, PrEP is widely available to all at-risk groups following the Department for Health and Social Care's decision to make it available across England in 2020. Wales, Scotland, and Northern Ireland made it available in 2017 and 2018. [46] [47] [48]

Notes and References

  1. Web site: Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017 . Therapeutic Goods Administration (TGA) . 21 June 2022 . 30 March 2024.
  2. Web site: Truvada EPAR . European Medicines Agency . 21 February 2005 . 13 June 2024.
  3. Web site: Truvada. Drugs.com. 12 December 2016. live. https://web.archive.org/web/20161220233315/https://www.drugs.com/truvada.html. 20 December 2016.
  4. Web site: UK label Truvada film-coated tablets. Electronic Medicines Compendium. August 2016. live. https://web.archive.org/web/20161220171148/https://www.medicines.org.uk/emc/medicine/15826. 20 December 2016.
  5. Book: WHO Model Formulary 2008 . 2009 . 9789241547659 . ((World Health Organization)) . Stuart MC, Kouimtzi M, Hill SR . 10665/44053 . World Health Organization . World Health Organization . 160 .
  6. Web site: Emtricitabine / tenofovir Pregnancy and Breastfeeding Warnings . Drugs.com . 1 August 2018 . https://web.archive.org/web/20191010041222/https://www.drugs.com/pregnancy/emtricitabine-tenofovir.html . 10 October 2019 . live . 10 October 2019.
  7. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 21st list 2019 . 2019 . 10665/325771 . World Health Organization . World Health Organization . Geneva . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO . free .
  8. Web site: AOC asks pharma CEO why $2,000 HIV drug costs just $8 in Australia . The Independent . 15 November 2019 . en . 17 May 2019.
  9. Web site: The Top 300 of 2020 . ClinCalc . 7 October 2022.
  10. Web site: Emtricitabine; Tenofovir Disoproxil - Drug Usage Statistics . ClinCalc . 7 October 2022.
  11. Web site: Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV. July 2019. AIDSinfo Clinical Guidelines. 30 October 2019. 4 December 2016. https://web.archive.org/web/20161204180634/https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf. dead.
  12. Web site: PrEP . Centers for Disease Control and Prevention (CDC) . 17 October 2019 . https://web.archive.org/web/20191031230000/https://www.cdc.gov/hiv/basics/prep.html . 31 October 2019 . live . 31 October 2019.
  13. Web site: Truvada- emtricitabine and tenofovir disoproxil fumarate tablet, film coated label . DailyMed . 18 May 2018 . https://web.archive.org/web/20191031230542/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=54e82b13-a037-49ed-b4b3-030b37c0ecdd . 31 October 2019 . live . 31 October 2019.
  14. Okwundu CI, Uthman OA, Okoromah CA. 35672491 . Antiretroviral pre-exposure prophylaxis (PrEP) for preventing HIV in high-risk individuals . Cochrane Database Syst Rev . 7. 7 . CD007189 . 2012 . 10.1002/14651858.CD007189.pub3 . 22786505 . 11324012 .
  15. Chou R, Evans C, Hoverman A, Sun C, Dana T, Bougatsos C, Grusing S, Korthuis PT . 11 June 2019 . Preexposure Prophylaxis for the Prevention of HIV Infection: Evidence Report and Systematic Review for the US Preventive Services Task Force . JAMA . 321 . 22 . 2214–2230 . 10.1001/jama.2019.2591 . 31184746 . 184485546 . 0098-7484. free .
  16. News: 16 July 2012 . FDA approves first pill to help prevent HIV . Perrone . Matthew . . live . https://web.archive.org/web/20120719082458/http://seattletimes.nwsource.com/html/businesstechnology/2018699860_apushivdrugfda.html . 19 July 2012 . Associated Press .
  17. Web site: Pre-Exposure Prophylaxis (PrEP) . 4 June 2015. https://web.archive.org/web/20150605164822/http://www.cdc.gov/hiv/prevention/research/prep/. 5 June 2015.
  18. Web site: Administration of pre-exposure prophylaxis against HIV infection . UpToDate . 31 October 2019 . 1 November 2019 . https://web.archive.org/web/20191101012946/https://www.uptodate.com/contents/administration-of-pre-exposure-prophylaxis-against-hiv-infection . dead .
  19. Web site: Pre-exposure prophylaxis of HIV in adults at high risk: Truvada (emtricitabine/tenofovir disoproxil). 5 October 2016 .
  20. Panlilio AL, Cardo DM, Grohskopf LA, Heneine W, Ross CS . Updated U.S. Public Health Service guidelines for the management of occupational exposures to HIV and recommendations for postexposure prophylaxis . MMWR Recomm Rep . 54 . RR-9 . 1–17 . September 2005 . 16195697 .
  21. Kuhar DT, Henderson DK, Struble KA, Heneine W, Thomas V, Cheever LW, Gomaa A, Panlilio AL . Updated US Public Health Service guidelines for the management of occupational exposures to human immunodeficiency virus and recommendations for postexposure prophylaxis . Infection Control and Hospital Epidemiology . September 2013 . 34 . 9 . 875–92 . 10.1086/672271 . 23917901 . 17032413 . 20711 .
  22. Web site: Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV. 30 October 2019. 4 December 2016. https://web.archive.org/web/20161204180634/https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf. dead.
  23. Web site: Update on Prevention, Diagnosis, and Treatment of Chronic Hepatitis B: AASLD 2018 Hepatitis B Guidance. 20 November 2019. 25 January 2020. https://web.archive.org/web/20200125221107/https://www.aasld.org/sites/default/files/2019-06/HBVGuidance_Terrault_et_al-2018-Hepatology.pdf. dead.
  24. Web site: Emtricitabine and Tenofovir Disoproxil Fumarate (Professional Patient Advice) . Drugs.com . 31 October 2019 .
  25. Web site: Brief What's New in the Guidelines Perinatal. AIDSinfo. 23 October 2019. 23 October 2019. https://web.archive.org/web/20191023125908/https://aidsinfo.nih.gov/guidelines/brief-html/3/perinatal/224/whats-new-in-the-guidelines. dead.
  26. Web site: Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. National Institutes of Health (NIH) . 21 October 2014. live. https://web.archive.org/web/20140412004422/http://aidsinfo.nih.gov/contentfiles/lvguidelines/perinatalgl.pdf. 12 April 2014.
  27. Web site: Emtricitabine / tenofovir Use During Pregnancy . Drugs.com . 23 October 2019 .
  28. Tenofovir . Drugs and Lactation Database (LactMed) . National Library of Medicine (US) . 23 October 2019 . 2006. 30000609 .
  29. News: PrEP does not raise lipids or alter body fat, safety study finds. 16 February 2018.
  30. Glidden DV, Mulligan K, McMahan V, Anderson PL, Guanira J, Chariyalertsak S, Buchbinder SP, Bekker LG, Schechter M, Grinsztejn B, Grant RM . Metabolic Effects of Preexposure Prophylaxis With Coformulated Tenofovir Disoproxil Fumarate and Emtricitabine . Clin. Infect. Dis. . 67 . 3 . 411–419 . July 2018 . 29415175 . 6051460 . 10.1093/cid/ciy083 .
  31. Web site: DailyMed - XENICAL- orlistat capsule. dailymed.nlm.nih.gov. 30 October 2019.
  32. Ramanathan S, Shen G, Cheng A, Kearney BP. July 2007. Pharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137. J. Acquir. Immune Defic. Syndr.. 45. 3. 274–9. 10.1097/QAI.0b013e318050d88c. 17414929. 31756102. free.
  33. Web site: EP0915894B1 - NUCLEOTIDE ANALOGS. Espacenet. 13 December 2017.
  34. Web site: U.K. Court invalidates Gilead's Truvada patent extension, allowing PrEP generics. 19 September 2018 .
  35. Web site: Truvada ruling could allow cheap HIV prevention in the UK -. 19 September 2018.
  36. Web site: EU door opens for generic version of AIDS medicine Truvada.
  37. News: Gilead loss of generic HIV drug battle a boost for gay community. The Irish Times. 18 May 2018.
  38. News: Gilead in row with generics manufacturers over HIV drug in Ireland. The Irish Times. 30 October 2017.
  39. Web site: European PrEP programs face two big issues: How to get more people coming forward, and how to serve them if they do. 27 January 2021 .
  40. News: Rowland . Christopher . Gilead defied a government HIV patent. The Justice Department has opened a review. . . 24 April 2019 . https://web.archive.org/web/20191101010542/https://www.washingtonpost.com/business/economy/gilead-defied-a-government-hiv-patent-the-justice-department-has-opened-a-review/2019/04/24/16e4e20e-62bc-11e9-bfad-36a7eb36cb60_story.html . 1 November 2019 . live . 31 October 2019 .
  41. News: Rowland . Christopher . Gilead files challenge to government patents for HIV prevention pill . . 21 August 2019 . https://web.archive.org/web/20191101011634/https://www.washingtonpost.com/business/economy/gilead-files-challenge-to-government-patents-for-hiv-prevention-pill/2019/08/21/43baa61e-c43d-11e9-b5e4-54aa56d5b7ce_story.html . 1 November 2019 . live . 29 October 2019 .
  42. Petitions to US Patent and Trademark Office on HIV PrEP Patents . . 21 August 2019 . https://web.archive.org/web/20191030023128/https://www.gilead.com/news-and-press/company-statements/petitions-to-us-patent-and-trademark-office-on-hiv-prep-patents . 30 October 2019 . live . 29 October 2019.
  43. News: Silverman . Ed . Biden administration appeals jury finding in battle over patents for HIV prevention pills . 8 July 2024 . STAT News . 8 July 2024.
  44. New Guidance On PrEP: Support Services Must Be Covered Without Cost-Sharing Health Affairs Forefront . 4 August 2022 . Health Affairs Forefront . 2021 . en . 10.1377/forefront.20210728.333084. Keith . Katie .
  45. Web site: 19 July 2021 . FAQS ABOUT AFFORDABLE CARE ACT IMPLEMENTATION PART 47 . 4 August 2022 . Centers for Medicare & Medicaid Services.
  46. Web site: HIV drug PrEP to be available across England.
  47. Web site: Free PrEP on the NHS.
  48. https://pharmacy-xl.org/order-sovaldi-online-en.html Generic Sovaldi

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