Fosdevirine
Chemical compound
- None
- 5-Chloro-3-[[3-[(E)-2-cyanoethenyl]-5-methylphenyl]-methoxyphosphoryl]-1H-indole-2-carboxamide
- 1018450-26-4
- 44232529
- 28529638
- Z4I0C281BJ
- D09906
- ChEMBL2104968
- Interactive image
- CC1=CC(=CC(=C1)/C=C/C#N)[P@](=O)(C2=C(NC3=C2C=C(C=C3)Cl)C(=O)N)OC
InChI
- InChI=1S/C20H17ClN3O3P/c1-12-8-13(4-3-7-22)10-15(9-12)28(26,27-2)19-16-11-14(21)5-6-17(16)24-18(19)20(23)25/h3-6,8-11,24H,1-2H3,(H2,23,25)/b4-3+/t28-/m1/s1
- Key:CGBYTKOSZYQOPV-ASSBYYIWSA-N
Fosdevirine is an experimental antiviral agent of the non-nucleoside reverse transcriptase inhibitor class that was studied for potential use in the treatment of HIV-AIDS.[1][2]
It was discovered by Idenix Pharmaceuticals and was being developed by GlaxoSmithKline and ViiV Healthcare, but it has now been discontinued[3][4] due to unexpected side effects.[5]
References
- ^ Dousson C, Alexandre FR, Amador A, Bonaric S, Bot S, Caillet C, et al. (March 2016). "Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor". Journal of Medicinal Chemistry. 59 (5): 1891–8. doi:10.1021/acs.jmedchem.5b01430. PMID 26804933.
- ^ "Fosdevirine". AIDSinfo. U.S. National Library of Medicine, U.S. Department of Health and Human Services. Archived from the original on 2019-08-11. Retrieved 2018-08-14.
- ^ "Fosdevirine". Adis Insight. Springer Nature Switzerland AG.
Highest Development Phases: Discontinued, HIV-1 infections
- ^ "Fosdevirine". MedKoo Biosciences.
GSK2248761 is no longer in clinical development.
- ^ Margolis DA, Eron JJ, DeJesus E, White S, Wannamaker P, Stancil B, Johnson M (2013). "Unexpected finding of delayed-onset seizures in HIV-positive, treatment-experienced subjects in the Phase IIb evaluation of fosdevirine (GSK2248761)". Antiviral Therapy. 19 (1): 69–78. doi:10.3851/IMP2689. PMID 24158593. S2CID 6147197.
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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
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