Dexelvucitabine
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IUPAC name 2′,3′-Didehydro-2′,3′-dideoxy-5-fluorocytidine | |
Systematic IUPAC name 4-Amino-5-fluoro-1-[(2R,5S)-5-(hydroxymethyl)-2,5-dihydrofuran-1-yl]pyrimidin-2(1H)-one | |
Other names Reverset | |
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Properties | |
Chemical formula | C9H10FN3O3 |
Molar mass | 227.195 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). N verify (what is YN ?) Infobox references |
Dexelvucitabine is a failed experimental agent for the management of human immunodeficiency virus infection. It is a cytidine nucleoside analog and nucleoside reverse transcriptase inhibitor.[1] that inhibits HIV-1 replication in vitro. During phase II clinical trials there was some indication of a decreased mean viral load in patients with infected human immunodeficiency virus.[2][3]
On April 3, 2006, Pharmasset and Incyte, the pharmaceutical companies developing dexelvucitabine, announced the decision to cease further trials and development of the drug due to an increased incidence of grade 4 hyperlipasemia (an excess of the pancreatic enzyme lipase in the bloodstream) in a phase II trial.[1][4]
References
- ^ a b PubChem. "Dexelvucitabine". pubchem.ncbi.nlm.nih.gov. Retrieved 2022-04-07.
- ^ Hernandez-Santiago, Brenda I.; Mathew, Judy S.; Rapp, Kim L.; Grier, Jason P.; Schinazi, Raymond F. (June 2007). "Antiviral and Cellular Metabolism Interactions between Dexelvucitabine and Lamivudine". Antimicrobial Agents and Chemotherapy. 51 (6): 2130–2135. doi:10.1128/aac.01543-06. ISSN 0066-4804. PMC 1891415. PMID 17403996.
- ^ Sobieszczyk, Magdalena E; Talley, Angela K; Wilkin, Timothy; Hammer, Scott M (2005-03-01). "Advances in antiretroviral therapy". Topics in HIV Medicine. 13 (1): 24–44. ISSN 2161-5845. PMID 15849370.
- ^ Ryder, Neil S (2007-12-01). "Discontinued drugs in 2006: anti-infectives". Expert Opinion on Investigational Drugs. 16 (12): 1867–1878. doi:10.1517/13543784.16.12.1867. ISSN 1354-3784. PMID 18041997. S2CID 40129603.
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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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