TY - JOUR T1 - Factors Contributing to the Antiviral Effectiveness of Tenofovir JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther DO - 10.1124/jpet.117.243139 SP - jpet.117.243139 AU - Rachel Ann Murphy AU - Monica Ann Valentovic Y1 - 2017/01/01 UR - http://jpet.aspetjournals.org/content/early/2017/08/31/jpet.117.243139.abstract N2 - Over 1 million people in the United States are living with Human Immunodeficiency Virus (HIV) which may progress to Acquired Immunodeficiency Disease. The use of antiviral therapy has successfully controlled the rate of viral growth in patients. Antiviral agents improve the quality of life and reduce the potential for spreading HIV; HIV is currently considered a chronic disease provided patients are compliant with their antiviral medications. Tenofovir is a nucleoside transcriptase inhibitor that prevents viral replication and is approved for treatment of HIV and chronic hepatitis B infection. Tenofovir is an antiretroviral drug used alone and in combination with other nucleoside reverse transcriptase inhibitor agents to lower viral load in HIV patients. Tenofovir is administered as a prodrug in order to increase bioavailability. The prodrug forms of tenofovir are tenofovir disoproxil fumarate approved in 2001 and tenofovir alafenamide approved in 2016. Tenofovir is extensively used in controlling HIV as it is administered once daily allowing for good compliance. This minireview discusses the changes in dosing that are needed in the presence of renal impairment which is a common occurrence with HIV chronic disease progression. The impact of food, age and drug transporters on tenofovir absorption and clearance will be discussed. The potential special conditions occurring with fixed combination doses containing tenofovir will also be reviewed including the use of cobicistat, a cytochrome P450 3 inhibitor. The short review also addresses some newer preparations using niosomes to improve tenofovir absorption and delivery to the target cells. ER -