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Evaluation of the effect of dabrafenib and metabolites on QTc interval in patients with BRAF V600-mutant tumours.

Nebot N, Arkenau HT, Infante JR, Chandler JC, Weickhardt A, Lickliter JD, Sarantopoulos J, Gordon MS, Mak G, St-Pierre A, Tang L, Mookerjee B, Carson SW, Hayes S, Grossmann KF.

Br J Clin Pharmacol. 2018 Apr;84(4):764-775. doi: 10.1111/bcp.13488. Epub 2018 Jan 23.


Dose selection, pharmacokinetics, and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436).

Falchook GS, Long GV, Kurzrock R, Kim KB, Arkenau HT, Brown MP, Hamid O, Infante JR, Millward M, Pavlick A, Chin MT, O'Day SJ, Blackman SC, Curtis CM, Lebowitz P, Ma B, Ouellet D, Kefford RF.

Clin Cancer Res. 2014 Sep 1;20(17):4449-58. doi: 10.1158/1078-0432.CCR-14-0887. Epub 2014 Jun 23.


Evaluation of the Effect of Selumetinib on Cardiac Repolarization: A Randomized, Placebo- and Positive-controlled Crossover QT/QTc Study in Healthy Subjects.

Zhou D, So K, Dymond AW, Vik T, Al-Huniti N, Mariani G, Zorenyi G, Huang Y, Holmes V, Severin P, Rasmussen S, Martin P.

Clin Ther. 2016 Dec;38(12):2555-2566. doi: 10.1016/j.clinthera.2016.10.004. Epub 2016 Nov 9.


Olaparib does not cause clinically relevant QT/QTc interval prolongation in patients with advanced solid tumours: results from two phase I studies.

Swaisland H, Plummer R, So K, Garnett S, Bannister W, Fabre MA, Dota C, Fielding A.

Cancer Chemother Pharmacol. 2016 Oct;78(4):775-84. doi: 10.1007/s00280-016-3124-5. Epub 2016 Aug 23.


Intravenous Dosing as an Alternate Approach to Safely Achieve Supratherapeutic Exposure for Assessments of Cardiac Repolarization: A Randomized Clinical Trial with Mavoglurant (AFQ056).

Ufer M, Sagkriotis A, Salunke A, Ganesan S, Tisserant A, Dodman A, Voltz E, Woessner R, Jordaan P, Legangneux E.

Clin Ther. 2016 Dec;38(12):2589-2597. doi: 10.1016/j.clinthera.2016.10.007. Epub 2016 Nov 4.


Ipragliflozin does not prolong QTc interval in healthy male and female subjects: a phase I study.

Zhang W, Smulders R, Abeyratne A, Dietz A, Krauwinkel W, Kadokura T, Keirns J.

Clin Ther. 2013 Aug;35(8):1150-1161.e3. doi: 10.1016/j.clinthera.2013.06.009. Epub 2013 Aug 2.


Preladenant, a selective adenosine A₂A receptor antagonist, is not associated with QT/QTc prolongation.

Wang Z, Xuan F, Lin WH, Troyer MD, Tendolkar A, Cutler DL.

Eur J Clin Pharmacol. 2013 Oct;69(10):1761-7. doi: 10.1007/s00228-013-1541-5. Epub 2013 Jul 16.


Lack of effect of perampanel on QT interval duration: Results from a thorough QT analysis and pooled partial seizure Phase III clinical trials.

Yang H, Laurenza A, Williams B, Patten A, Hussein Z, Ferry J.

Epilepsy Res. 2015 Aug;114:122-30. doi: 10.1016/j.eplepsyres.2015.04.010. Epub 2015 May 1.


Dabrafenib plus trametinib in patients with BRAFV600-mutant melanoma brain metastases (COMBI-MB): a multicentre, multicohort, open-label, phase 2 trial.

Davies MA, Saiag P, Robert C, Grob JJ, Flaherty KT, Arance A, Chiarion-Sileni V, Thomas L, Lesimple T, Mortier L, Moschos SJ, Hogg D, Márquez-Rodas I, Del Vecchio M, Lebbé C, Meyer N, Zhang Y, Huang Y, Mookerjee B, Long GV.

Lancet Oncol. 2017 Jul;18(7):863-873. doi: 10.1016/S1470-2045(17)30429-1. Epub 2017 Jun 4.


Effects of Therapeutic and Supratherapeutic Doses of Siponimod (BAF312) on Cardiac Repolarization in Healthy Subjects.

Shakeri-Nejad K, Aslanis V, Veldandi UK, Mooney L, Pezous N, Brendani B, Juan A, Allison M, Perry R, Legangneux E.

Clin Ther. 2015 Nov 1;37(11):2489-2505.e2. doi: 10.1016/j.clinthera.2015.09.006. Epub 2015 Oct 27.


Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers.

Peeters M, Janssen K, Kakuda TN, Schöller-Gyüre M, Lachaert R, Hoetelmans RM, Woodfall B, De Smedt G.

Ann Pharmacother. 2008 Jun;42(6):757-65. doi: 10.1345/aph.1K681. Epub 2008 Apr 29.


Safety, tolerability, and pharmacokinetic profile of dabrafenib in Japanese patients with BRAF V600 mutation-positive solid tumors: a phase 1 study.

Fujiwara Y, Yamazaki N, Kiyohara Y, Yoshikawa S, Yamamoto N, Tsutsumida A, Nokihara H, Namikawa K, Mukaiyama A, Zhang F, Tamura T.

Invest New Drugs. 2018 Apr;36(2):259-268. doi: 10.1007/s10637-017-0502-8. Epub 2017 Sep 7.


Evaluation of the effects of bitopertin (RG1678) on cardiac repolarization: a thorough corrected QT study in healthy male volunteers.

Hofmann C, Banken L, Hahn M, Swearingen D, Nagel S, Martin-Facklam M.

Clin Ther. 2012 Oct;34(10):2061-71. doi: 10.1016/j.clinthera.2012.08.010. Epub 2012 Sep 12.


Phase 1 study to evaluate the effect of the MEK inhibitor trametinib on cardiac repolarization in patients with solid tumours.

Patnaik A, Tolcher A, Papadopoulos KP, Beeram M, Rasco D, Werner TL, Bauman JW, Scheuber A, Cox DS, Patel BR, Zhou Y, Hamid M, Schramek D, Sharma S.

Cancer Chemother Pharmacol. 2016 Sep;78(3):491-500. doi: 10.1007/s00280-016-3090-y. Epub 2016 Jul 8.


A Randomized Trial to Assess the Effect of Doravirine on the QTc Interval Using a Single Supratherapeutic Dose in Healthy Adult Volunteers.

Khalilieh SG, Yee KL, Fan L, Liu R, Heber W, Dunzo E, Triantafyllou I, Hussaini A, Iwamoto M.

Clin Drug Investig. 2017 Oct;37(10):975-984. doi: 10.1007/s40261-017-0552-x.


Population pharmacokinetics of dabrafenib, a BRAF inhibitor: effect of dose, time, covariates, and relationship with its metabolites.

Ouellet D, Gibiansky E, Leonowens C, O'Hagan A, Haney P, Switzky J, Goodman VL.

J Clin Pharmacol. 2014 Jun;54(6):696-706. doi: 10.1002/jcph.263. Epub 2014 Jan 17.


Effect of a single supratherapeutic dose of dolutegravir on cardiac repolarization.

Chen S, Min SS, Peppercorn A, Borland J, Lou Y, Song I, Fujiwara T, Piscitelli SC.

Pharmacotherapy. 2012 Apr;32(4):333-9. doi: 10.1002/j.1875-9114.2012.01033.x. Epub 2012 Mar 15.


A single supratherapeutic dose of vorinostat does not prolong the QTc interval in patients with advanced cancer.

Munster PN, Rubin EH, Van Belle S, Friedman E, Patterson JK, Van Dyck K, Li X, Comisar W, Chodakewitz JA, Wagner JA, Iwamoto M.

Clin Cancer Res. 2009 Nov 15;15(22):7077-84. doi: 10.1158/1078-0432.CCR-09-1214. Epub 2009 Nov 3.

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