Chemistry:Elsulfavirine

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Short description: Chemical compound
Elsulfavirine
Elsulfavirine.svg
Clinical data
Trade namesElpida
Other namesVM 1500; elpivirine
ATC code
  • None
Legal status
Legal status
  • Rx-only in Russia
Identifiers
CAS Number
PubChem CID
DrugBank
UNII
Chemical and physical data
FormulaC24H17BrCl2FN3O5S
Molar mass629.28 g·mol−1

Elsulfavirine (trade name Elpida; also known as VM 1500) is drug used to treat HIV infection. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI).[1][2][3] Elsulfavirine is a prodrug which is metabolized to the active antiviral agent deselsulfavirine (also known as VM 1500A).[4] It was developed by the Russian company Viriom.[5]

In June 2017, elsulfavirine was approved for use in Russia as an oral formulation for the treatment of HIV-1 infections in combination with other antiretroviral drugs.[4][6] Currently, elsulfavirine is used in antiretroviral therapy regimens in the Russian Federation, which includes the combination elsulfavirine + lamivudine (or emtricitabine) + tenofovir.[7]

Long-acting injectable formulations of eslulfavarinin and deselsulfavarine are under investigation.[8][9]

In addition, Roche is investigating the use of elsulfavirin for the treatment of COVID-19 and it is currently in Phase II clinical trials for this possible indication.[5]

References

  1. "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment". Expert Opinion on Drug Metabolism & Toxicology 15 (10): 813–829. October 2019. doi:10.1080/17425255.2019.1673367. PMID 31556749. 
  2. "Emerging reverse transcriptase inhibitors for HIV-1 infection". Expert Opinion on Emerging Drugs 23 (2): 149–157. June 2018. doi:10.1080/14728214.2018.1474202. PMID 29737220. 
  3. "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment". Expert Opinion on Drug Metabolism & Toxicology 15 (10): 813–829. October 2019. doi:10.1080/17425255.2019.1673367. PMID 31556749. 
  4. 4.0 4.1 "Elsulfavirine: First Global Approval". Drugs 77 (16): 1811–1816. October 2017. doi:10.1007/s40265-017-0820-3. PMID 28940154. 
  5. 5.0 5.1 "Elsulfavirine - Viriom". AdisInsight. https://adisinsight.springer.com/drugs/800031212. 
  6. "Chapter 29: To Market, To Market--2017". 2018 Medicinal Chemistry Reviews 53. https://www.acsmedchem.org/?nd=mcr5329. 
  7. "Elpida (elsulfavirine) becomes the preferred first line therapy for treatment of HIV infection in Russia" (Press release). PRN Newswire. February 2, 2021.
  8. "What's in the Pipeline?". Contagion 4 (3). June 5, 201. https://www.contagionlive.com/view/whats-in-the-pipeline. 
  9. "Pre-clinical pharmacokinetics of elsufavirine/VM1500A long acting injectable formulations". International Antiviral Society-USA. 2017. Poster WEPEA0190.