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Elsulfavirine

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From Wikipedia, the free encyclopedia

Chemical compound

Pharmaceutical compound

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
PubChemCID	11527519
DrugBank	14929
UNII	ZC4CGO0RUG
KEGG	D13018
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 nameElpida; also known asVM 1500) is drug used to treatHIV infection. It is anon-nucleoside reverse transcriptase inhibitor (NNRTI).^[1]^[2]^[3] Elsulfavirine is aprodrug which is metabolized to the active antiviral agentdeselsulfavirine (also known as VM 1500A).^[4] It wasdeveloped 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 ^bAl-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 againstHIV (primarilyJ05)

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	Amprenavir (APV)^‡ Fosamprenavir (FPV) Indinavir (IDV)^◊ Lopinavir (LPV) Nelfinavir (NFV)^◊ Ritonavir (RTV)^# Saquinavir (SQV)^◊
2^nd generation	Atazanavir (ATV)°^# Darunavir (DRV)°^# Tipranavir (TPV)^◊ TMC-310911^§

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	Efavirenz (EFV)^# Nevirapine (NVP)^# Delavirdine (DLV)^‡
2^nd generation	diarylpyrimidines Dapivirine (DPV) Etravirine (ETR) Rilpivirine (RPV) Doravirine (DOR) Elsulfavirine (ESV)

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

°DHHSrecommendedinitial regimen options.^◊Formerly or rarely used agent.

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