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Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer.
TLDR
The combination of dabrafenib plus trametinib has activity in a subset of patients with BRAF V600-mutant mCRC, and mutational analysis revealed that the patient achieving a complete response and two of three evaluable patients achieving a partial response had PIK3CA mutations. Expand
Bacterial redox protein azurin, tumor suppressor protein p53, and regression of cancer
TLDR
The use of a purified bacterial redox protein, azurin, that enters human cancer (melanoma UISO-Mel-2) cells and induces apoptosis is reported and has been shown to allow regression of human U ISO- Mel-2 tumors xenotransplanted in nude mice and may potentially be used in cancer treatment. Expand
Bacterial cupredoxin azurin as an inducer of apoptosis and regression in human breast cancer
TLDR
In conclusion, azurin blocks breast cancer cell proliferation and induces apoptosis through the mitochondrial pathway both in vitro and in vivo, thereby suggesting a potential chemotherapeutic application of this bacterial cupredoxin for the treatment of breast cancer. Expand
Combined BRAF (Dabrafenib) and MEK inhibition (Trametinib) in patients with BRAFV600-mutant melanoma experiencing progression with single-agent BRAF inhibitor.
TLDR
Dabrafenib plus trametinib has modest clinical efficacy in patients with BRAF inhibitor-resistant melanoma and may be a therapeutic strategy for patients who previously benefited from BRAF inhibitors monotherapy but demonstrates minimal efficacy after rapid progression with BRAf inhibitor therapy. Expand
Updated overall survival (OS) for BRF113220, a phase 1-2 study of dabrafenib (D) alone versus combined dabrafenib and trametinib (D+T) in pts with BRAF V600 mutation-positive (+) metastatic melanoma
TLDR
Safety and efficacy of D+T were evaluated in this Phase 1-2 study, and primary endpoints were progression free survival (PFS), response rate (RR), duration of response (DoR), and safety. Expand
Overall Survival and Durable Responses in Patients With BRAF V600-Mutant Metastatic Melanoma Receiving Dabrafenib Combined With Trametinib.
TLDR
Dabrafenib plus trametinib results in a median OS of more than 2 years in BRAF inhibitor-naive patients with BRAF V600 mutation-positive metastatic melanoma, and approximately 20% were progression free at 3 years. Expand
First‐Time‐in‐Human Study With GSK249320, a Myelin‐Associated Glycoprotein Inhibitor, in Healthy Volunteers
TLDR
GSK249320, a monoclonal antibody directed against myelin‐associated glycoprotein (MAG), is being developed for the enhancement of recovery of function poststroke and was well tolerated at all doses, with AUC showing dose linearity. Expand
Phase 1-2 trial of the BRAF inhibitor dabrafenib (D) plus MEK inhibitor trametinib (T) in BRAF V600 mutant colorectal cancer (CRC): Updated efficacy and biomarker analysis.
TLDR
Preclinical data suggest that improved MAPK pathway suppression with combined inhibition of BRAF and MEK may improve efficacy in BRAF mutant CRC, and this work is likely to be a first step in this direction. Expand
Disposition and Metabolism of GSK2251052 in Humans: A Novel Boron-Containing Antibiotic
TLDR
A combination of in vitro metabolism experiments and a pharmacokinetic study in monkeys with the inhibitor 4-methylpyrazole provided strong evidence that alcohol dehydrogenase, potentially in association with aldehyde dehydrogen enzyme, is the primary enzyme involved in the formation of the M3 metabolite. Expand
A phase I/II dose escalation and expansion study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK525762 in combination with fulvestrant in subjects with ER+
TLDR
Preclinical data suggest that reducing expression of the estrogen receptor (ER) as well as other ER-responsive genes may provide therapeutic benefit for women for whom endocrine therapy alone has proven inadequate. Expand
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