Pharmacokinetics and pharmacogenetics of the MEK1/2 inhibitor, selumetinib, in Asian and Western healthy subjects: a pooled analysis
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DOI: 10.1007/s00228-017-2217-3
Abstract: PurposeEmerging data on selumetinib, a MEK1/2 inhibitor in clinical development, suggest a possible difference in pharmacokinetics (PK) between Japanese and Western patients. This pooled analysis sought to assess the effect of ethnicity on selumetinib exposure… read more here.
Keywords: selumetinib; analysis; mek1 inhibitor; asian subjects ... See more keywords
Clinical Pharmacokinetics and Pharmacodynamics of Selumetinib
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DOI: 10.1007/s40262-020-00967-y
Abstract: Selumetinib, a highly specific mitogen-activated protein kinase 1/2 inhibitor, is approved for children older than 2 years of age with neurofibromatosis 1 who have inoperable plexiform neurofibromas. By selectively binding to mitogen-activated protein kinase 1/2… read more here.
Keywords: selumetinib; clinical pharmacokinetics; activated protein; protein kinase ... See more keywords
Safety and tolerability of selumetinib as a monotherapy, or in combination with docetaxel as second-line therapy, in Japanese patients with advanced solid malignancies or non-small cell lung cancer
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DOI: 10.1093/jjco/hyx144
Abstract: Objective This Phase I study (NCT01605916) investigated the safety, tolerability and pharmacokinetic profile of selumetinib plus docetaxel as second-line therapy in Japanese patients with locally advanced or metastatic non-small cell lung cancer (NSCLC), or selumetinib… read more here.
Keywords: selumetinib; combination; safety tolerability; japanese patients ... See more keywords
Selumetinib in Children with Neurofibromatosis Type 1 and Asymptomatic Inoperable Plexiform Neurofibroma At Risk for Developing Tumor-Related Morbidity.
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DOI: 10.1093/neuonc/noac109
Abstract: BACKGROUND Selumetinib was recently approved for treatment of inoperable symptomatic plexiform neurofibromas (PNs) in children with neurofibromatosis type 1 (NF1). This parallel phase II study determined the response rate to selumetinib in children with NF1… read more here.
Keywords: selumetinib; neurofibromatosis type; children neurofibromatosis; selumetinib children ... See more keywords
A phase I trial of the MEK inhibitor selumetinib (AZD6244) in pediatric patients with recurrent or refractory low-grade glioma: a Pediatric Brain Tumor Consortium (PBTC) study
Sign Up to like & getrecommendations! Published in 2017 at "Neuro-Oncology"
DOI: 10.1093/neuonc/now282
Abstract: Background Activation of the mitogen-activated protein kinase pathway is important for growth of pediatric low-grade gliomas (LGGs). The aim of this study was to determine the recommended phase II dose (RP2D) and the dose-limiting toxicities… read more here.
Keywords: selumetinib; mek inhibitor; grade; study ... See more keywords
Effect of food on capsule and granule formulations of selumetinib.
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DOI: 10.1111/cts.13209
Abstract: Selumetinib is an oral, potent, and highly selective allosteric MEK1/2 inhibitor approved for the treatment of pediatric patients (aged ≤2 years) with neurofibromatosis type 1 who have symptomatic, inoperable plexiform neurofibromas. A granule formulation of selumetinib… read more here.
Keywords: effect food; granule formulations; capsule granule; selumetinib ... See more keywords
Selumetinib in combination with dexamethasone for the treatment of relapsed/refractory RAS-pathway mutated paediatric and adult acute lymphoblastic leukaemia (SeluDex): study protocol for an international, parallel-group, dose-finding with expansion phase I/II trial
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DOI: 10.1136/bmjopen-2021-059872
Abstract: Introduction Event-free survival rates at 15 years for paediatric patients with relapsed/refractory acute lymphoblastic leukaemia (ALL) are 30%–50%, with 5-year survival for adult patients only 20%. Many patients with newly diagnosed and relapsed ALL harbour… read more here.
Keywords: phase; combination; relapsed refractory; adult ... See more keywords
Phase Ib Results of the Rational Combination of Selumetinib and Cyclosporin A in Advanced Solid Tumors with an Expansion Cohort in Metastatic Colorectal Cancer.
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DOI: 10.1158/0008-5472.can-18-0316
Abstract: MEK inhibition is of interest in cancer drug development, but clinical activity in metastatic colorectal cancer (mCRC) has been limited. Preclinical studies demonstrated Wnt pathway overexpression in KRAS-mutant cell lines resistant to the MEK inhibitor,… read more here.
Keywords: selumetinib; selumetinib cyclosporin; combination selumetinib; cancer ... See more keywords
Abstract 3648: MSU-42011, alone and in combination with selumetinib, reduces pERK levels in NF1 cancer cells and decreases CCL2 expression in THP-1 macrophages
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DOI: 10.1158/1538-7445.am2023-3648
Abstract: Neurofibromatosis type 1 (NF1) is a common genetic disease that predisposes approximately 50% of affected individuals to develop plexiform neurofibromas (PNFs), which can progress to highly aggressive malignant peripheral nerve sheath tumors (MPNSTs) in approximately… read more here.
Keywords: selumetinib; combination; expression; msu 42011 ... See more keywords
Efficacy and Safety of Selumetinib in Pediatric Patients With Neurofibromatosis Type 1
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DOI: 10.1212/wnl.0000000000013296
Abstract: Background and Objectives Although the recent approval of selumetinib is expected to transform the management of children with neurofibromatosis type 1 (NF1), particularly those with symptomatic and inoperable plexiform neurofibromas, no systematic review has summarized… read more here.
Keywords: efficacy safety; selumetinib; safety selumetinib; neurofibromatosis type ... See more keywords
Targeting the mitogen‑activated protein kinase kinase and protein kinase A pathways overcomes acquired resistance to Selumetinib in low‑grade glioma cells.
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DOI: 10.3892/or.2020.7867
Abstract: The Ras/Raf/MEK/MAPK signaling cascade is frequently activated in human cancer and serves a crucial role in the oncogenesis of pediatric low‑grade gliomas (PLGGs). Therefore, drugs targeting kinases among the mitogen‑activated protein kinase (MAPK) effectors of receptor tyrosine… read more here.
Keywords: selumetinib; kinase; resistance; protein kinase ... See more keywords