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Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
TLDR
It is concluded that the affinities of topoisomerase I drugs for BCRP are, in decreasing order: SN-38 > topotecan > 9-aminocamptothecin > CPT-11 > NX211 > DX8951f > BNP1350 • GF120918. Expand
The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein
TLDR
It is shown that imatinib is efficiently transported by mouse Bcrp1 in transfected Madin-Darby canine kidney strain II (MDCKII) monolayers and the hypothesis that P-gp and BCRP inhibitors, such as elacridar and pantoprazole, improve the brain penetration of imatinIB is tested. Expand
Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line.
TLDR
It is reported for the first time that BCRP/MXR/ABCP can also be up-regulated upon exposure of tumor cells to the clinically important drug topotecan, and that B CRP-mediated efflux of topOTecan is very efficient. Expand
Mechanism of the Pharmacokinetic Interaction between Methotrexate and Benzimidazoles
TLDR
Benzimidazoles differentially affect transport of MTX mediated by BCRP and MRP2, two transporters known to transport MTX and located in apical membranes of epithelia involved in drug disposition. Expand
A Phase I and Pharmacological Study with Imidazolium-trans-DMSO-imidazole-tetrachlororuthenate, a Novel Ruthenium Anticancer Agent
TLDR
The maximum-tolerated dose (MTD), profile of adverse events, and dose-limiting toxicity of NAMI-A in patients with solid tumors were determined and the ruthenium pharmacokinetic analysis revealed a linear relationship between dose and area under the concentration-time curve (AUC) of total and unbound rUThenium. Expand
The Effect of Low pH on Breast Cancer Resistance Protein (ABCG2)-Mediated Transport of Methotrexate, 7-Hydroxymethotrexate, Methotrexate Diglutamate, Folic Acid, Mitoxantrone, Topotecan, and
TLDR
It is concluded that BCRP transports substrate drugs more efficiently at low pH, independent of the dissociation status of the substrate. Expand
Phase II Study of WEE1 Inhibitor AZD1775 Plus Carboplatin in Patients With TP53-Mutated Ovarian Cancer Refractory or Resistant to First-Line Therapy Within 3 Months.
TLDR
This is the first report providing clinical proof that AZD1775 enhances carboplatin efficacy in TP53-mutated ovarian cancer, and the encouraging antitumor activity observed in patients who were refractory or resistant to first-line therapy warrants further development. Expand
Phase I/II study with ruthenium compound NAMI-A and gemcitabine in patients with non-small cell lung cancer after first line therapy
TLDR
Main adverse events consisted of neutropenia, anemia, elevated liver enzymes, transient creatinine elevation, nausea, vomiting, constipation, diarrhea, fatigue, and renal toxicity. Expand
A Phase I and Pharmacological Study of the Platinum Polymer AP5280 Given as an Intravenous Infusion Once Every 3 Weeks in Patients with Solid Tumors
TLDR
AP5280 can be administered safely as a 1-h i.v. infusion at a dose of 3300 mg Pt/m2 once every 3 weeks and produces prolonged plasma exposure compared with any of the free Pt-containing drugs, however, it remains to be determined whether AP52 80 can actually increase Pt delivery to the DNA of tumor cells in man as has been shown in experimental models. Expand
DNA repair mechanisms involved in gemcitabine cytotoxicity and in the interaction between gemcitabine and cisplatin.
TLDR
The results indicate that BER, NER, HR, and NHEJ are most likely incapable of modulating the cytotoxicity of gem citabine, and that HR is involved in the synergistic interaction between cisplatin and gemcitabine in the cell system. Expand
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