Elsulfavirine

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]

Elsulfavirine

Clinical data
Trade names	Elpida
Other names	VM 1500; elpivirine
ATC code	J05AG07 (WHO)
Legal status
Legal status	Rx-only in Russia
Identifiers
IUPAC name N-[4-[[2-[4-Bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl]amino]-3-chlorophenyl]sulfonylpropanamide
CAS Number	868046-19-9
PubChem CID	11527519
DrugBank	14929
UNII	ZC4CGO0RUG
Chemical and physical data
Formula	C24H17BrCl2FN3O5S
Molar mass	629.28 g·mol−1
InChI 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

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. 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. "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.