[HTML][HTML] HM30181A, a potent P-glycoprotein inhibitor, potentiates the absorption and in vivo antitumor efficacy of paclitaxel in an orthotopic brain tumor model

W Zeng, BYK Law, VKW Wong, DSB Chan… - Cancer Biology & …, 2020 - ncbi.nlm.nih.gov
Objective: Delivery of chemotherapeutic drugs to the brain has remained a major obstacle in
the treatment of glioma, owing to the presence of the blood-brain barrier and the activity of P …

Increased penetration of paclitaxel into the brain by inhibition of P-Glycoprotein

EM Kemper, AE van Zandbergen, C Cleypool… - Clinical Cancer …, 2003 - AACR
P-Glycoprotein (Pgp) in the blood-brain barrier limits the uptake of substrate drugs into the
brain. We have determined the efficacy of several (putative) inhibitors of Pgp (cyclosporin A …

Oral paclitaxel chemotherapy for brain tumors: ideal combination treatment of paclitaxel and P-glycoprotein inhibitor

KM Joo, K Park, DS Kong, SY Song… - Oncology …, 2008 - spandidos-publications.com
Oral chemotherapy has many advantages over parenteral chemotherapeutics
administration. To use the advantages of the oral chemotherapy and maximize anti-tumor …

The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice

EM Kemper, C Cleypool, W Boogerd… - Cancer chemotherapy …, 2004 - Springer
We determined the effect of zosuquidar· 3HCl, an inhibitor of P-gp, on the penetration of the
anticancer drug paclitaxel into the brain. Zosuquidar· 3HCl was administered orally at 25 …

Improved penetration of docetaxel into the brain by co-administration of inhibitors of P-glycoprotein

EM Kemper, M Verheij, W Boogerd, JH Beijnen… - European Journal of …, 2004 - Elsevier
P-glycoprotein (Pgp) in the blood–brain barrier limits the brain's uptake of many anticancer
drugs. We have investigated whether the Pgp inhibitors cyclosporin A, valspodar (PSC833) …

Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain …

KM Joo, SY Song, K Park, MH Kim… - International …, 2008 - spandidos-publications.com
Abstract P-glycoprotein (P-gp), a factor responsible for the multidrug resistance of tumors, is
specifically expressed in brain microenvironment. To test its roles in brain metastatic tumor …

Brain-targeted delivery of paclitaxel using glutathione-coated nanoparticles for brain cancers

W Geldenhuys, T Mbimba, T Bui, K Harrison… - Journal of drug …, 2011 - Taylor & Francis
Paclitaxel is not effective for treatment of brain cancers because it cannot cross the blood–
brain barrier (BBB) due to efflux by P-glycoprotein (P-gp). In this work, glutathione-coated …

Interaction of HM30181 with P-glycoprotein at the murine blood–brain barrier assessed with positron emission tomography

F Bauer, T Wanek, S Mairinger, J Stanek… - European journal of …, 2012 - Elsevier
HM30181, a potent and selective inhibitor of the adenosine triphosphate-binding cassette
transporter P-glycoprotein (Pgp), was shown to enhance oral bioavailability and improve …

Effect of coumarin derivative-mediated inhibition of P-glycoprotein on oral bioavailability and therapeutic efficacy of paclitaxel

K Lee, SW Chae, Y Xia, NH Kim, HJ Kim, S Rhie… - European Journal of …, 2014 - Elsevier
Since P-glycoprotein (P-gp) acts as a barrier to intestinal absorption of various drugs, P-gp
inhibitors have been studied as oral absorption enhancers of P-gp substrate drugs. Here, we …

Approaches to overcome the blood-brain barrier in the chemotherapy of primary and secondary brain tumors: Modulation of P-glycoprotein 170 and targeting of the …

M Hubensack - 2005 - epub.uni-regensburg.de
Chemotherapy of primary and secondary brain tumors is hampered by the existence of the
blood-brain-barrier (BBB) which reduce the brain concentrations of lipophilic cytostatic …