Tenofovir Alafenamide for the Treatment of Chronic Hepatitis B Monoinfection

Abstract

Tenofovir alafenamide (TAF) is indicated for adult patients with chronic hepatitis B virus (HBV) infection with compensated liver disease at an oral dose of 25 mg/day. TAF is a more stable prodrug in the plasma than tenofovir disoproxil fumarate (TDF), leading to decreased plasma exposure of tenofovir. Decreased exposure is thought to reduce the risk of long-term TDF toxicities, such as nephrotoxicity and decreased bone mineral density (BMD). TAF, a nucleotide reverse transcriptase inhibitor, has the same mechanism of action as TDF. The results of phase III primary trials and extensions showed that TAF is noninferior to TDF at suppressing the HBV viral load in treatment-naive and treatment-experienced HBeAg-negative and HBeAg-positive patients at 48 weeks, 96 weeks, and 144 weeks of therapy. The most commonly reported adverse events were headache, abdominal pain, fatigue, cough, nausea, and back pain. At all evaluated time points (out to 144 wks of treatment), patients who received TAF had less risk of nephrotoxicity and less of a decline in BMD than the patients who received TDF. TAF appears to be safe in patients with a creatinine clearance (Cl ) above 15 ml/min; however, TAF is not currently recommended in patients with an estimated Cl below this threshold. TAF is safe in patients with mild hepatic impairment but is not currently recommended in patients with moderate or severe hepatic impairment (Child-Pugh class B or C).

Co-crystals, Salts or Mixtures of Both? The Case of Tenofovir Alafenamide Fumarates

“…Tenofovir alafenamide fumarate (known as TAF) [6][7][8] is a novel prodrug derivative of the well-known nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir (TFV) [9][10][11], which was initially developed for the treatment of HIV infection as tenofovir disoproxil fumarate (TDF) in the late 1990s [12][13][14] and marketed under the tradename Viread ® since 2001 [15]. TAF, as a new type of TFV prodrug, was approved as a mono therapy (Vemlidy ® ) in November 2016 for the treatment of chronic hepatitis B virus infection [16][17][18][19][20] in adults with compensated liver disease by the U.S Food & Drug Administration (FDA). Interestingly, therapy (Vemlidy ® ) in November 2016 for the treatment of chronic hepatitis B virus infection [16][17][18][19][20] in adults with compensated liver disease by the U.S Food & Drug Administration (FDA).…”

“…TAF, as a new type of TFV prodrug, was approved as a mono therapy (Vemlidy ® ) in November 2016 for the treatment of chronic hepatitis B virus infection [16][17][18][19][20] in adults with compensated liver disease by the U.S Food & Drug Administration (FDA). Interestingly, therapy (Vemlidy ® ) in November 2016 for the treatment of chronic hepatitis B virus infection [16][17][18][19][20] in adults with compensated liver disease by the U.S Food & Drug Administration (FDA). Interestingly, according to the FDA data, TAF is marketed as a hemifumarate [21].…”

Qualitative Interviews on The Diagnosis Process of Hepatitis B Among 50 Patients in Chongqing, China

“…The most influential recommendations for patients are lifestyle and diet. Other studies have found that most patients in China find themselves in the middle and late stages of the disease when they are suffering from hepatitis B [34]and have symptoms such as nausea and fatigue [35]. Influenced by the environment and other factors [36], they are likely to develop into liver cancer and reduce their quality of life [37].…”

Long-acting implants to treat and prevent HIV infection

“…The prodrug tenofovir alafenamide (TAF) is 10 times more potent than tenofovir disoproxil fumarate (TDF), and has the added advantage that it is taken up into cells from the plasma as the prodrug, which is converted to the parent drug and then to the active intracellular diphosphate inside the cell [9]. In addition, from the perspective of prevention, TAF has activity against both hepatitis B virus (HBV) and HIV, and could potentially prevent both infections, in addition to treating them in those who have already acquired coinfection [10].…”