Concomitant oral and intravenous pharmacokinetics of dabrafenib, a BRAF inhibitor, in patients with BRAF V600 mutation‐positive solid tumors
CL Denton, E Minthorn, SW Carson… - 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 …
BRAF and CRAF kinases as well as mutant forms of BRAF kinase. The aim of this phase 1 …
Dose selection, pharmacokinetics, and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436)
GS Falchook, GV Long, R Kurzrock, KB Kim… - Clinical Cancer …, 2014 - AACR
Purpose: Dabrafenib is a selective, potent ATP-competitive inhibitor of the BRAF V600-
mutant kinase that has demonstrated efficacy in clinical trials. We report the rationale for …
mutant kinase that has demonstrated efficacy in clinical trials. We report the rationale for …
Population pharmacokinetics of dabrafenib, a BRAF inhibitor: effect of dose, time, covariates, and relationship with its metabolites
D Ouellet, E Gibiansky, C Leonowens… - The Journal of …, 2014 - Wiley Online Library
Dabrafenib is a BRAF kinase inhibitor indicated for the treatment of BRAF V600E mutation‐
positive melanoma. The population pharmacokinetics of dabrafenib, including changes over …
positive melanoma. The population pharmacokinetics of dabrafenib, including changes over …
Effects of particle size, food, and capsule shell composition on the oral bioavailability of dabrafenib, a BRAF inhibitor, in patients with BRAF mutation‐positive tumors
D Ouellet, KF Grossmann, G Limentani… - Journal of …, 2013 - Wiley Online Library
Dabrafenib is a small‐molecule inhibitor of BRAF kinase activity that is currently being
developed for the treatment of BRAF V600 mutation‐positive melanoma. This clinical, open …
developed for the treatment of BRAF V600 mutation‐positive melanoma. This clinical, open …
Clinical pharmacokinetics and pharmacodynamics of dabrafenib
A Puszkiel, G Noé, A Bellesoeur, N Kramkimel… - Clinical …, 2019 - Springer
Dabrafenib is a potent and selective inhibitor of BRAF-mutant kinase that is approved, as
monotherapy or in combination with trametinib (mitogen-activated protein kinase (MAPK) …
monotherapy or in combination with trametinib (mitogen-activated protein kinase (MAPK) …
BRAF inhibitors: from the laboratory to clinical trials
MA Rahman, A Salajegheh, RA Smith… - Critical reviews in …, 2014 - Elsevier
BRAF is one of the most commonly mutated proto-oncogenes and plays a significant role in
the development of numerous cancers of high clinical impact. Due to the commonality of …
the development of numerous cancers of high clinical impact. Due to the commonality of …
Dabrafenib: first global approval
AD Ballantyne, KP Garnock-Jones - Drugs, 2013 - Springer
Dabrafenib (Tafinlar®), a mutant-BRAF kinase inhibitor, emerged from GlaxoSmithKline's
research programme for the discovery of selective inhibitors of mutant BRAF kinase activity …
research programme for the discovery of selective inhibitors of mutant BRAF kinase activity …
BRAF inhibitors in cancer therapy
CH Johansson, SE Brage - Pharmacology & therapeutics, 2014 - Elsevier
Activating BRAF mutations, leading to constitutive activation of the MAPK signaling pathway,
are common in a variety of human cancers. Several small molecule BRAF inhibitors have …
are common in a variety of human cancers. Several small molecule BRAF inhibitors have …
A next-generation BRAF inhibitor overcomes resistance to BRAF inhibition in patients with BRAF-mutant cancers using pharmacokinetics-informed dose escalation
R Yaeger, MA McKean, R Haq, JT Beck, MH Taylor… - Cancer Discovery, 2024 - AACR
RAF inhibitors have transformed treatment for BRAF V600-mutant cancer patients, but
clinical benefit is limited by adaptive induction of ERK signaling, genetic alterations that …
clinical benefit is limited by adaptive induction of ERK signaling, genetic alterations that …
Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial
GS Falchook, GV Long, R Kurzrock, KB Kim… - The Lancet, 2012 - thelancet.com
Background Dabrafenib is an inhibitor of BRAF kinase that is selective for mutant BRAF. We
aimed to assess its safety and tolerability and to establish a recommended phase 2 dose in …
aimed to assess its safety and tolerability and to establish a recommended phase 2 dose in …
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