Elsulfavirine Explained

Width:325
Tradename:Elpida
Synonyms:VM 1500; elpivirine
Atc Prefix:None
Legal Status:Rx-only in Russia
Cas Number:868046-19-9
Pubchem:11527519
Unii:ZC4CGO0RUG
Drugbank:14929
Iupac Name:N-[4-[[2-[4-Bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl]amino]-3-chlorophenyl]sulfonylpropanamide
C:24
H:17
Br:1
Cl:2
F:1
N:3
O:5
S:1
Stdinchi: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)
Stdinchikey: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]

Notes and References

  1. Wang Y, De Clercq E, Li G . 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 . 31556749 . 10.1080/17425255.2019.1673367 . 203439476 .
  2. Rai MA, Pannek S, Fichtenbaum CJ . Emerging reverse transcriptase inhibitors for HIV-1 infection . Expert Opinion on Emerging Drugs . 23 . 2 . 149–157 . June 2018 . 29737220 . 6158299 . 10.1080/14728214.2018.1474202 .
  3. Wang Y, De Clercq E, Li G . 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 . 31556749 . 10.1080/17425255.2019.1673367 . 203439476 .
  4. Al-Salama ZT . Elsulfavirine: First Global Approval . Drugs . 77 . 16 . 1811–1816 . October 2017 . 28940154 . 10.1007/s40265-017-0820-3 . 25316512 .
  5. Web site: Elsulfavirine - Viriom . AdisInsight .
  6. 2018 Medicinal Chemistry Reviews . 53 . Chapter 29: To Market, To Market--2017 . Bolger CA, Carpenter JE, Dhar TG, Pashine A, Dragovich PS, Cook JH, Gillis EP, Peese KM, Merritt JR .
  7. Elpida (elsulfavirine) becomes the preferred first line therapy for treatment of HIV infection in Russia . PRN Newswire . February 2, 2021 .
  8. What's in the Pipeline? . June 5, 201 . Akram R, DeSimone Jr J . Contagion . 4 . 3 .
  9. Bichko V, Rogovoy B, Koryakova A . Pre-clinical pharmacokinetics of elsufavirine/VM1500A long acting injectable formulations . International Antiviral Society-USA . 2017 . Poster WEPEA0190 .