Elsulfavirine
- None
- Rx-only in Russia
- N-[4-[[2-[4-Bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl]amino]-3-chlorophenyl]sulfonylpropanamide
- 868046-19-9
- 11527519
- 14929
- ZC4CGO0RUG
- 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
- ^ 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.
- v
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(Discovery and development)
(Integrase strand transfer inhibitors (INSTI))
(Discovery and development)
1st generation | |
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2nd generation |
inhibitors (RTIs)
Nucleoside and nucleotide (NRTI) | |||||
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Non-nucleoside (NNRTI) (Discovery and development) |
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- Abacavir/lamivudine#
- Abacavir/dolutegravir/lamivudine°
- Abacavir/lamivudine/zidovudine
- Atazanavir/cobicistat
- Bictegravir/emtricitabine/tenofovir alafenamide°
- Cabotegravir/rilpivirine
- Darunavir/cobicistat
- Darunavir/cobicistat/emtricitabine/tenofovir alafenamide°
- Dolutegravir/emtricitabine/tenofovir alafenamide
- Dolutegravir/lamivudine°
- Dolutegravir/lamivudine/tenofovir alafenamide°
- Dolutegravir/lamivudine/tenofovir disoproxil°#
- Dolutegravir/rilpivirine
- Doravirine/lamivudine/tenofovir disoproxil
- Efavirenz/emtricitabine/tenofovir disoproxil#
- Efavirenz/lamivudine/tenofovir disoproxil#
- Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
- Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
- Emtricitabine/tenofovir alafenamide
- Emtricitabine/rilpivirine/tenofovir alafenamide
- Emtricitabine/rilpivirine/tenofovir disoproxil
- Emtricitabine/tenofovir disoproxil#
- Lamivudine/nevirapine/stavudine
- Lamivudine/nevirapine/zidovudine
- Lamivudine/raltegravir
- Lamivudine/tenofovir disoproxil#
- Lamivudine/zidovudine#
- Lopinavir/ritonavir#
Uncoating inhibitors |
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Transcription inhibitors |
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Translation inhibitors | |
BNAbs | |
Other | |
Failed agents |
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III