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| Systematic (IUPAC) name | |
| (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one | |
| Clinical data | |
| Trade names | Sustiva, Stocrin etc. |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a699004 |
| Pregnancy cat. | D (U.S.) |
| Legal status | POM (UK), ℞-only (U.S.) |
| Routes | Oral |
| Pharmacokinetic data | |
| Protein binding | 99.5-99.75% |
| Metabolism | Hepatic (CYP3A4 and CYP2B6-mediated) |
| Half-life | 40-55 hours |
| Excretion | Renal and fecal |
| Identifiers | |
| CAS number | 154598-52-4 |
| ATC code | J05AG03 |
| PubChem | CID 64139 |
| DrugBank | DB00625 |
| ChemSpider | 57715 |
| UNII | JE6H2O27P8 |
| KEGG | D00896 |
| ChEBI | CHEBI:119486 |
| ChEMBL | CHEMBL223228 |
| NIAID ChemDB | 032934 |
| Chemical data | |
| Formula | C14H9ClF3NO2 |
| Mol. mass | 315.675 g/mol |
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InChI=1S/C14H9ClF3NO2/c15-9-3-4-11-10(7-9)13(14(16,17)18,21-12(20)19-11)6-5-8-1-2-8/h3-4,7-8H,1-2H2,(H,19,20)/t13-/m0/s1 |
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 (what is this?) (verify) |
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Efavirenz (EFV, brand names Sustiva, Stocrin, Efavir etc.) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.
For HIV infection that has not previously been treated, the United States Department of Health and Human Services Panel on Antiretroviral Guidelines currently recommends the use of efavirenz in combination with tenofovir/emtricitabine (Truvada) as one of the preferred NNRTI-based regimens in adults and adolescents .
Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to reduce the risk of HIV infection in people exposed to a significant risk (e.g. needlestick injuries, certain types of unprotected sex etc.).
The usual adult dose is 600 mg once a day. It is usually taken on an empty stomach at bedtime to reduce neurological and psychiatric adverse effects.
Efavirenz was combined with the popular HIV medication Truvada, which consists of tenofovir and emtricitabine, all of which are reverse transcriptase inhibitors. This combination of three medications approved by the U.S. Food and Drug Administration (FDA) in July 2006 under the brand name Atripla, provides HAART in a single tablet taken once a day. It results in a simplified drug regimen for many patients.
Efavirenz was approved by the FDA on September 21, 1998, making it the 14th approved antiretroviral drug.
Efavirenz is used to treat HIV infection. It is never used alone and is always given in combination with other drugs. The decision on when to start treatment should take into account CD4 count, HIV viral load, treatment history, resistance profiles and patient preference.
Since the preliminary publication of the results of the ACTG 5142 trial in 2006 which compared efavirenz against lopinavir, efavirenz has been used as first line treatment in preference to the protease inhibitors. The ACTG 5095 trial showed that the potency of efavirenz is maintained at all CD4 counts and HIV viral loads.
Efavirenz falls in the NNRTI class of antiretrovirals. Both nucleoside and non-nucleoside RTIs inhibit the same target, the reverse transcriptase enzyme, an essential viral enzyme which transcribes viral RNA into DNA. Unlike nucleoside RTIs, which bind at the enzyme's active site, NNRTIs act allosterically by binding to a distinct site away from the active site known as the NNRTI pocket.
Efavirenz is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.
As most NNRTIs bind within the same pocket, viral strains which are resistant to efavirenz are usually also resistant to the other NNRTIs, nevirapine and delavirdine. The most common mutation observed after efavirenz treatment is K103N, which is also observed with other NNRTIs.
The usual adult dose of efavirenz is 600 mg per day (usually given at bedtime); or 800 mg daily when given concurrently with rifampicin as part of treatment of co-infection with tuberculosis.
As with most HIV treatments, efavirenz is quite expensive. A one month supply of 600 mg tablets costed approximately $550 in April 2008. Some emerging countries have opted to purchase Indian generics such as Efavir by Cipla Ltd for a fraction of the cost. In Thailand, one month supply of Efavirenz + Truvada, as of June 2012, costs THB 2900 ($90), there's also a social program for poorer patients who can't afford even this price. In South Africa, a license has been granted to generics giant Aspen Pharmacare to manufacture, and distribute to Sub-Saharan Africa, a cost-effective antiretroviral drug.
Generic brands India:
Efavirenz is chemically described as (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Its empirical formula is C14H9ClF3NO2. Efavirenz is a white to slightly pink crystalline powder with a molecular mass of 315.68 g/mol. It is practically insoluble in water (<10 µg/mL).
15. Sütterlin, S., Vögele, C., & Gauggel, S. (2010). Neuropsychiatric complications of Efavirenz therapy: suggestions for a new research paradigm. The Journal of Neuropsychiatry and Clinical Neurosciences, 22(4), 361-369.
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