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Etravirine PK Fact Sheet Reviewed March 2016 Page 1 of 2 for Personal Use Only

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Etravirine PK Fact Sheet Reviewed March 2016 Page 1 of 2 for Personal Use Only www.hiv-druginteractions.org Etravirine PK Fact Sheet Reviewed March 2016 Page 1 of 2 For personal use only. Not for distribution. For personal use only. Not for distribution. For personal use only. Not for distribution. Details Generic Name Etravirine (TMC125) Trade Name Intelence® Class Non‐Nucleoside Reverse Transcriptase Inhibitor Molecular Weight 435.28 Structure CN CN O NNH N Br NH2 Summary of Key Pharmacokinetic Parameters Plasma half life 41 h Cmax No data Cmin* 297 ± 391 ng/ml (geometric mean ± sd); 298.8 (2‐4852) ng/ml (median range) AUC* 4522 ± 4710 ng/ml.h (geometric mean ± sd); 4380 (458‐59084) ng/ml.h, (median, range) *Data are from a clinical trial where patients received darunavir/ritonavir 600/100 mg bd as part of their background regimen. Pharmacokinetic estimates account for reduction in parameters due to co‐administration. Bioavailability Absolute oral bioavailability is unknown Absorption The systemic exposure (AUC) to etravirine was decreased by about 50% when etravirine was administered under fasting conditions, as compared to administration following a meal. Therefore, etravirine should be taken following a meal. Protein Binding 99.9% Volume of Distribution No data CSF:Plasma ratio Not determined in humans Semen:Plasma ratio Not determined in humans Renal Clearance <1.2% Renal Impairment A decrease in clearance is not expected in patients with renal impairment. Hepatic Impairment No dose adjustment is required in patients with mild (Child‐Pugh Class A) or moderate (Child‐ Pugh Class B) hepatic impairment. Pharmacokinetics have not been evaluated in severe hepatic impairment (Child‐Pugh Class C). © Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law. www.hiv-druginteractions.org Etravirine PK Fact Sheet Reviewed March 2016 Page 2 of 2 For personal use only. Not for distribution. For personal use only. Not for distribution. For personal use only. Not for distribution. Metabolism and Distribution Metabolised by CYP3A4, CYP2C9, CYP2C19 Inducer of CYP3A4 Inhibitor of CYP2C9, CYP2C19 Transported by Unknown References Unless otherwise stated (see below), information is from: Intelence® Summary of Product Characteristics, Janssen‐Cilag Ltd. Intelence® US Prescribing Information, Janssen Pharmaceuticals Inc. © Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law. .
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