|Pronunciation||del a' vir deen|
|Other names||Delavirdine mesylate|
|Drug class||Non-nucleoside reverse transcriptase inhibitor (NNRTI)|
|Side effects||Tiredness, dizziness, headache, rash|
|Typical dose||400 mg TID|
|Metabolism||Liver (CYP3A4- and CYP2D6-mediated)|
|Elimination half-life||5.8 hours|
|Excretion||Kidney (51%) and fecal (44%)|
|Chemical and physical data|
|Molar mass||456.57 g·mol−1|
|3D model (JSmol)|
Delavirdine (DLV), sold under the brand name Rescriptor, is a medication used to treat HIV/AIDS. It is used together with other HIV medicines; though is not a preferred treatment. It is taken by mouth, three times per day.
Common side effects include tiredness, dizziness, headache, and rash. Other symptoms may include Stevens-Johnson syndrome, central obesity, and immune reconstitution syndrome. Safety in pregnancy is unclear. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
The risk of cross-resistance across the NNRTI class, as well as its complex set of drug interactions, make the place of delavirdine in second-line and salvage therapy unclear, and it is currently rarely used.
The recommended dosage is 400 mg, three times a day.
The most common side event is moderate to severe rash, which occurs in up to 20% of patients. Other common adverse events include fatigue, headache and nausea. Liver toxicity has also been reported.
Like ritonavir, delavirdine is an inhibitor of cytochrome P450 isozyme CYP3A4, and interacts with many medications. It should not be administered with a wide range of drugs, including amprenavir, fosamprenavir, simvastatin, lovastatin, rifampin, rifabutin, rifapentine, St John's wort, astemizole, midazolam, triazolam, ergot medications, and several medications for acid reflux.
Modification of the scheme that was done for ateviridine q.v. by performing the reductive alkylation with acetone gives 2 after removal of the protecting group. Acylation of this amine with the imidazolide from 5-Methylsulfonaminoindole-2-carboxylic acid (1) affords the amide, reverse transcriptase inhibitor, atevirdine.
- "Delavirdine". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Retrieved 23 December 2021.
- "Delavirdine Mesylate Monograph for Professionals". Drugs.com. Retrieved 23 December 2021.
- DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download from AIDSInfo Archived 2006-05-06 at the Wayback Machine)
- "RESCRIPTOR brand of delavirdine mesylate tablets. Product information" (PDF). Archived from the original (PDF) on 2006-04-15. Retrieved 2006-05-18.
- WO 9109849, Romero DL, Mitchell MA, Thomas RC, Palmer JR, Tarpley WG, Aristoff PA, Smith HW, "Diaromatic Substituted Anti-AIDS Compounds", published 11 July 1991, assigned to Upjohn Company
- US 5563142, Palmer JR, Romero DL, Aristoff PA, Thomas RC, Smith HW, "Diaromatic substituted compounds as anti-HIV-1 agents", published 8 October 1996, assigned to Upjohn Company
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