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Emtricitabine
drug data and news
Emtricitabine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Emtricitabine | ||
| Brand Names/Synonyms | 524W91; BW 1592; BW 524W91; Coviracil; DRG-0208; Dotfc; Emtricitabine; Emtriva; FTC; Racivir; Truvada | ||
| Indication | For the treatment of HIV-1 infection in adults. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Emtricitabine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. | ||
| Mechanism Of Action | Emtricitabine, a synthetic nucleoside analogue of cytidine, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine substrate deoxycytidine 5'-triphosphate and by incorporating into nascent viral DNA, which results in chain termination. Emtricitabine 5'-triphosphate is a weak inhibitor of mammalian DNA polymerases alpha, beta, and epsilon and of mitochondrial DNA polymerase gamma. Emtricitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. | ||
| Emtricitabine News (When available) |
Advances in First-Line and "Switch" Antiretroviral Strategies for ... Feb 2, 2006 A Potential HIV Prophylactic? Feb 7, 2006 Simplified treatment regimens show promise in HIV-infected ... Feb 6, 2006 Anti-Retrovirals in Africa, not a distant dream Feb 9, 2006 AIDS drug cocktail can block HIV transmission: study Feb 7, 2006 CROI: AZT, 3TC and FTC achieve good concentrations in the female ... Feb 17, 2006 Management of HIV/HBV Coinfection Feb 8, 2006 Anti-Retrovirals in Africa, not a distant dream 09 Feb 2006 Advances in First-Line and "Switch" Antiretroviral Strategies for ... Feb 2, 2006 Study Sets New Gold Standard For Initial Antiretroviral Treatment ... Jan 25, 2006 A Potential HIV Prophylactic? Feb 7, 2006 Management of HIV/HBV Coinfection Feb 8, 2006 Simplified treatment regimens show promise in HIV-infected ... Feb 6, 2006 AIDS drug cocktail can block HIV transmission: study Feb 7, 2006 Study Sets New Gold Standard for Antiretroviral HIV Treatment Jan 23, 2006 Gilead Sciences Announces Fourth Quarter and Full Year 2005 ... Jan 30, 2006 Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006 Companies Anticipate Filing New Drug Application in Second Quarter ... Jan 9, 2006 Study compares HIV treatment options Jan 31, 2006 Health Beat Jan 26, 2006 Researchers find better HIV medication Jan 18, 2006 Data Comparing Viread(R) and Emtriva(R) to Combivir(R) as Part of ... Jan 18, 2006 Better Treatment for HIV Jan 18, 2006 Study gives high marks to new drugs Jan 19, 2006 US stops trial of interrupted HIV treatment Jan 18, 2006 Gilead HIV drug combo beats GSK rival in phase III trial Jan 20, 2006 One AIDS treatment study proves promising, another harmful Jan 20, 2006 Drug price reduction makes Aids manageable Jan 25, 2006 Intermittent AIDS-treatment study is halted Jan 19, 2006 New HIV Drug Regimen More Effective Than Existing Therapy Jan 18, 2006 Stress at work stresses heart Jan 20, 2006 New HIV Regimen Outperforms Gold Standard Jan 19, 2006 Gilead and BMS to seek regulatory approval for efavirenz, Truvada ... Jan 10, 2006 ICAAC: Switching from Combivir to Truvada has benefits for ... Jan 11, 2006 Fat loss associated with Combivir but not Truvada Jan 23, 2006 NEWS RELEASE Jan 19, 2006 Pharmasset Announces Five Clevudine Presentations at AASLD Nov 11, 2005 Preliminary 24-Week Data Evaluating the Impact of Switching from ... Nov 17, 2005 Switching from twice-daily Combivir to once-daily Truvada in ... Nov 23, 2005 Ranbaxy announces new co-packaged triple ART combinations Dec 2, 2005 FDA Safety Labeling Changes: Emtriva, FazaClo, Climara/Climara Pro Sep 14, 2005 Emtriva: New Formulation and Labeling Changes Sep 29, 2005 GB AIDS Drugs Plant “Pivotal� Sep 7, 2005 New drug cocktail beats standard HIV therapy Sep 2, 2005 Gilead Reduces Prices for Viread and Truvada in the Developing ... Aug 29, 2005 *vwd/BUSINESS WIRE: Gilead gibt aktuellen Entwicklungsstand zur ... Aug 10, 2005 Gilead reports problems putting tenofovir, FTC and efavirenz into ... Aug 10, 2005 Gilead Reduces Prices for Viread® and Truvada® in the Developing ... Aug 30, 2005 HIV: An Ever-changing Epidemic Aug 11, 2005 Another Thing You'd Think Would Be Simple Aug 10, 2005 | ||
| Dosage Forms | TABLETS | ||
| Drug_Category | Anti-HIV Agents; ATC:J05AF09 | ||
| Absorption | Rapidly absorbed (93%) | ||
| Interactions |
-->Interactions for Emtricitabine: The potential for drug interactions with EMTRIVA has been studied in combination with indinavir, stavudine, famciclovir, and tenofovir disoproxil fumarate. There were no clinically significant drug interactions for any of these drugs. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical IUPAC Name | 4-amino-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-pyrimidin-2-one | ||
| Chemical Formula | C8H10FN3O3S | ||
| Molecular Weight | 247.248 g/mol | ||
| Smiles String | C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F | ||
| Melting Point | 136-140 °C | ||
| Water Solubility | 112 mg/mL | ||
| State | Solid | ||
| LogP/Hphobicity | -0.43 | ||
| Isoelectric Point | 2.65 | ||
| Biotransformation | Minimally transformed (13%), most appears unchanged in urine (86%). The biotransformation of emtricitabine includes oxidation of the thiol moiety to form the 3’-sulfoxide diastereomers (~ 9% of dose) and conjugation with glucuronic acid to form 2’-O-glucuronide (~ 4% of dose). | ||
| Half Life | 10 hours | ||
| Protein Binding [%] | <4% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Emtricitabine.html http://www.rxlist.com/cgi/generic3/emtriva.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00226 | ||
| CAS Registry Number | 143491-57-0 | ||
| KEGG Compound ID | C12599 | ||
| PubChem ID | SID:207107 | ||
| PharmGKB ID | PA10069 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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