Nevirapine (Viramune, Boehringer Ingelheim Ltd) is the first marketed non-nucleoside reverse transcriptase inhibitor. As with any antiretroviral drug, nevirapine should always be used as part of a fully suppressive regimen. Clinical studies have shown that nevirapine-containing regimens may accomplish durable virological and immunological responses in approximately half of all antiretroviral-naive patients. It can also be successfully used as a component of salvage therapies and as a part of a strategy to simplify protease inhibitor-containing regimens. Nevirapine has a beneficial effect on the lipid profile in both treatment-naive and -experienced patients. Nevirapine also has an important role in preventing mother-to-child transmission of HIV. It is usually well-tolerated with rash and liver toxicity being the most frequently reported adverse events. Nevirapine interacts with cytochrome P450 enzymes both as a substrate and as an inducer. For this reason, therapeutic drug monitoring should be recommended whenever nevirapine is used with protease inhibitors, methadone (Methadose, Rosemont Pharmaceuticals Ltd), oral contraceptives, rifampicin (Rifadin, Aventis Pharma) and other potentially interacting drugs. Nevirapine-resistant mutations are common to the non-nucleoside reverse transcriptase inhibitor family and they include K103N, V106A, Y181C, Y188C and G190A. A better understanding of the nevirapine profile will certainly contribute to ensuring that its clinical application becomes more effective and beneficial.