Assessment of the drug interaction potential and single‐and repeat‐dose pharmacokinetics of the BRAF inhibitor dabrafenib
…, D Ouellet, LE Richards‐Peterson… - The Journal of …, 2015 - Wiley Online Library
The induction of CYP2C9 by dabrafenib using S‐warfarin as a probe and the effects of a
CYP3A inhibitor (ketoconazole) and a CYP2C8 inhibitor (gemfibrozil) on dabrafenib …
CYP3A inhibitor (ketoconazole) and a CYP2C8 inhibitor (gemfibrozil) on dabrafenib …
Metabolism and disposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following …
…, DM Knecht, PD Gorycki, LE Richards-Peterson - Drug Metabolism and …, 2013 - ASPET
A phase I study was conducted to assess the metabolism and excretion of [ 14 C]dabrafenib
(GSK2118436; N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-…
(GSK2118436; N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-…
Concomitant oral and intravenous pharmacokinetics of dabrafenib, a BRAF inhibitor, in patients with BRAF V600 mutation‐positive solid tumors
…, GC Young, LE Richards‐Peterson… - The Journal of …, 2013 - Wiley Online Library
Dabrafenib is an orally bioavailable, potent, and selective inhibitor of human wild‐type BRAF
and CRAF kinases as well as mutant forms of BRAF kinase. The aim of this phase 1, single‐…
and CRAF kinases as well as mutant forms of BRAF kinase. The aim of this phase 1, single‐…
Prediction of the transporter-mediated drug-drug interaction potential of dabrafenib and its major circulating metabolites
…, C Watson, L Chen, LE Richards-Peterson - Drug Metabolism and …, 2017 - ASPET
The BRAF inhibitor dabrafenib was recently approved for the treatment of certain BRAF
V600 mutation-positive tumors, either alone or in combination therapy with the mitogen-activated …
V600 mutation-positive tumors, either alone or in combination therapy with the mitogen-activated …
Absolute bioavailability of BRAF inhibitor GSK2118436: Use of a microtracer study in patients with cancer
…, SW Carson, GC Young, LE Richards-Peterson… - Cancer Research, 2012 - AACR
Background. Absolute bioavailability (BA) studies in oncology are logistically and technically
challenging. Use of an intravenous (IV) microtracer offers an attractive alternative to …
challenging. Use of an intravenous (IV) microtracer offers an attractive alternative to …
Pharmacokinetic and pharmacodynamic analysis of preoperative therapy with dabrafenib alone and in combination with trametinib in patients with BRAF mutation …
…, RA Scolyer, S Mahmood, LE Richards-Peterson… - 2014 - ascopubs.org
TPS9112 Background: Dabrafenib (D) has clinical activity in patients (pts) with BRAF V600E/K
mutation–positive melanoma brain metastases (MBM). The combination of D and …
mutation–positive melanoma brain metastases (MBM). The combination of D and …
Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK 1 inhibitor GSK 2982772 in healthy volunteers
…, T Rudo, L Richards‐Peterson… - Pharmacology …, 2017 - Wiley Online Library
GSK 2982772 is a highly selective inhibitor of receptor‐interacting protein kinase 1 ( RIPK 1)
being developed to treat chronic inflammatory diseases. This first‐in‐human study …
being developed to treat chronic inflammatory diseases. This first‐in‐human study …
The metabolic drug-drug interaction profile of Dabrafenib: in vitro investigations and quantitative extrapolation of the P450-mediated DDI risk
…, D Nguyen, C Bowen, L Richards-Peterson… - Drug Metabolism and …, 2014 - ASPET
Dabrafenib is a potent ATP-competitive inhibitor for the V600 mutant b-rapidly accelerated
fibrosarcoma (b-raf) kinase currently approved in the United States for the treatment of …
fibrosarcoma (b-raf) kinase currently approved in the United States for the treatment of …
Quantification of the next-generation oral anti-tumor drugs dabrafenib, trametinib, vemurafenib, cobimetinib, pazopanib, regorafenib and two metabolites in human …
E Cardoso, T Mercier, AD Wagner, K Homicsko… - … of chromatography B, 2018 - Elsevier
A sensitive and selective method of high performance liquid chromatography (HPLC)
coupled to tandem mass spectrometry (MS/MS) has been developed for the simultaneous …
coupled to tandem mass spectrometry (MS/MS) has been developed for the simultaneous …
MM-PBSA and the importance of the dielectric constant for kinase drug design
M Schneider, G Labesse - 2020 - chemrxiv.org
… Gorycki, and Lauren E. RichardsPeterson. Metabolism and disposition of oral dabrafenib in
cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via …
cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via …