Elsulfavirine

Last updated
Elsulfavirine
Elsulfavirine.svg
Clinical data
Trade names Elpida
Other namesVM 1500; elpivirine
ATC code
Legal status
Legal status
  • Rx-only in Russia
Identifiers
  • N-[4-{{#parsoidfragment:1}}2-[4-Bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl]amino]-3-chlorophenyl]sulfonylpropanamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C24H17BrCl2FN3O5S
Molar mass 629.28 g·mol−1
3D model (JSmol)
  • CCC(=O)NS(=O)(=O)C1=CC(=C(C=C1)NC(=O)CC2=C(C(=C(C=C2)Br)OC3=CC(=CC(=C3)C#N)Cl)F)Cl
  • InChI=1S/C24H17BrCl2FN3O5S/c1-2-21(32)31-37(34,35)17-4-6-20(19(27)11-17)30-22(33)9-14-3-5-18(25)24(23(14)28)36-16-8-13(12-29)7-15(26)10-16/h3-8,10-11H,2,9H2,1H3,(H,30,33)(H,31,32)
  • Key:ULTDEARCBRNRGR-UHFFFAOYSA-N

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. ↑ Wang Y, De Clercq E, Li G (October 2019). "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment". Expert Opinion on Drug Metabolism & Toxicology. 15 (10): 813–829. doi:10.1080/17425255.2019.1673367. PMID   31556749. S2CID   203439476.
  2. ↑ Rai MA, Pannek S, Fichtenbaum CJ (June 2018). "Emerging reverse transcriptase inhibitors for HIV-1 infection". Expert Opinion on Emerging Drugs. 23 (2): 149–157. doi:10.1080/14728214.2018.1474202. PMC   6158299 . PMID   29737220.
  3. ↑ Wang Y, De Clercq E, Li G (October 2019). "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment". Expert Opinion on Drug Metabolism & Toxicology. 15 (10): 813–829. doi:10.1080/17425255.2019.1673367. PMID   31556749. S2CID   203439476.
  4. 1 2 Al-Salama ZT (October 2017). "Elsulfavirine: First Global Approval". Drugs. 77 (16): 1811–1816. doi:10.1007/s40265-017-0820-3. PMID   28940154. S2CID   25316512.
  5. 1 2 "Elsulfavirine - Viriom". AdisInsight.
  6. ↑ Bolger CA, Carpenter JE, Dhar TG, Pashine A, Dragovich PS, Cook JH, Gillis EP, Peese KM, Merritt JR. "Chapter 29: To Market, To Market--2017". 2018 Medicinal Chemistry Reviews. 53.
  7. ↑ "Elpida (elsulfavirine) becomes the preferred first line therapy for treatment of HIV infection in Russia" (Press release). PRN Newswire. February 2, 2021.
  8. ↑ Akram R, DeSimone Jr J (June 5, 201). "What's in the Pipeline?". Contagion. 4 (3).
  9. ↑ Bichko V, Rogovoy B, Koryakova A (2017). "Pre-clinical pharmacokinetics of elsufavirine/VM1500A long acting injectable formulations". International Antiviral Society-USA. Poster WEPEA0190.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.