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Elsulfavirine

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Elsulfavirine
Clinical data

Trade names	Elpida
Other names	VM 1500; elpivirine
ATC code	None
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

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 (oremtricitabine) + 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[edit]

^ 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.

^ 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.

^ 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.

^ ^a ^b 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.

^ ^a ^b "Elsulfavirine - Viriom". AdisInsight.

^ 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.

^ "Elpida (elsulfavirine) becomes the preferred first line therapy for treatment of HIV infection in Russia" (Press release). PRN Newswire. February 2, 2021.

^ Akram R, DeSimone Jr J (June 5, 201). "What's in the Pipeline?". Contagion. 4 (3).

^ Bichko V, Rogovoy B, Koryakova A (2017). "Pre-clinical pharmacokinetics of elsufavirine/VM1500A long acting injectable formulations". International Antiviral Society-USA. Poster WEPEA0190.

Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)

Capsid inhibitors

Lenacapavir (LEN)

Entry/fusion inhibitors
(Discovery and development)

gp41 (Enfuvirtide (ENF, T-20))^◊
CCR5 (Maraviroc (MVC)
Vicriviroc^†, Cenicriviroc^†, Leronlimab^†)
CD4 (Ibalizumab (IBA), Semzuvolimab^§)
gp120 (Fostemsavir (FTR))

Integrase inhibitors
(Integrase strand transfer inhibitors (INSTI))

Maturation inhibitors

Protease Inhibitors (PI)
(Discovery and development)

1^st generation

2^nd generation

Reverse-transcriptase
inhibitors (RTIs)

Nucleoside and
nucleotide (NRTI)

Nucleoside analogues/NRTIs: Abacavir (ABC)^#
Didanosine (ddI)^◊
Emtricitabine (FTC)
Lamivudine (3TC)^#
Stavudine (d4T)^◊
Zalcitabine (ddC)^‡
Zidovudine (AZT, ZDV)^#
Amdoxovir^†
Apricitabine^†
Censavudine^†
Elvucitabine^†
Islatravir (EFdA, ISL)^§
Racivir^†
Stampidine^†

Non-nucleoside (NNRTI)
(Discovery and development)

1^st generation

2^nd generation

Combined formulations

Pharmacokinetic boosters

Experimental agents

Uncoating inhibitors	TRIM5alpha (gene)
Transcription inhibitors	Tat antagonists
Translation inhibitors	Trichosanthin
BNAbs	Elipovimab
Other	Abzyme BIT225^† Calanolide A Ceragenin Cyanovirin-N Diarylpyrimidines Epigallocatechin gallate (EGCG) Foscarnet Fosdevirine^† Griffithsin Hydroxycarbamide KP-1461^† Miltefosine Portmanteau inhibitors Scytovirin Seliciclib^† Synergistic enhancers Tre recombinase Zinc finger protein transcription factor
Failed agents	Aplaviroc Atevirdine Brecanavir Capravirine Dexelvucitabine Droxinavir Lasinavir Emivirine Lersivirine Lodenosine Loviride Mozenavir Palinavir Telinavir

^#WHO-EM

^‡Withdrawn from market

Clinical trials:

^†Phase III
^§Never to phase III

°DHHS recommended initial regimen options. ^◊Formerly or rarely used agent.

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Retrieved from "https://en.wikipedia.org/w/index.php?title=Elsulfavirine&oldid=1204660734" Categories: ●Drugs not assigned an ATC code ●Non-nucleoside reverse transcriptase inhibitors ●Prodrugs ●Benzonitriles ●Diphenyl ethers ●Sulfonamides ●Organic compound stubs Hidden categories: ●Articles with short description ●Short description matches Wikidata ●Drugs with non-standard legal status ●Articles without EBI source ●Chemical pages without ChemSpiderID ●Articles without KEGG source ●Articles containing unverified chemical infoboxes ●All stub articles ●This page was last edited on 7 February 2024, at 16:46 (UTC). ●Text is available under the Creative Commons Attribution-ShareAlike License 4.0; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization. ●Privacy policy ●About Wikipedia ●Disclaimers ●Contact Wikipedia ●Code of Conduct ●Developers ●Statistics ●Cookie statement ●Mobile view