(Q38856951)

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Therapeutic Potential and Utility of Elacridar with Respect to P-glycoprotein Inhibition: An Insight from the Published In Vitro, Preclinical and Clinical Studies

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scholarly article

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

Therapeutic Potential and Utility of Elacridar with Respect to P-glycoprotein Inhibition: An Insight from the Published In Vitro, Preclinical and Clinical Studies (English)

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

author name string

Ranjeet Prasad Dash

1

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

R Jayachandra Babu

2

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

Nuggehally R Srinivas

3

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

publication date

3 April 2017

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

European Journal of Drug Metabolism and Pharmacokinetics

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

https://scigraph.springernature.com/pub.10.1007/s13318-017-0411-4

0 references

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Isolation of endothelial cells from brain, lung, and kidney: expression of the multidrug resistance P-glycoprotein isoforms

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Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites

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21 January 2018

Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier

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Transporters and drug-drug interactions: important determinants of drug disposition and effects

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21 January 2018

Effect of quercetin on Hoechst 33342 transport by purified and reconstituted P-glycoprotein.

1 reference

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21 January 2018

Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor

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21 January 2018

Phase I study of the multidrug resistance inhibitor zosuquidar administered in combination with vinorelbine in patients with advanced solid tumours

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21 January 2018

A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxorubicin in patients with advanced malignancy

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21 January 2018

Investigational ABC transporter inhibitors

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21 January 2018

Perspectives of P-glycoprotein modulating agents in oncology and neurodegenerative diseases: pharmaceutical, biological, and diagnostic potentials

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21 January 2018

Pharmacokinetic and pharmacodynamic study of tariquidar (XR9576), a P-glycoprotein inhibitor, in combination with doxorubicin, vinorelbine, or docetaxel in children and adolescents with refractory solid tumors.

1 reference

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21 January 2018

Understanding the role of tariquidar, a potent Pgp inhibitor, in combination trials with cytotoxic drugs: What is missing?

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21 January 2018

Characterisation and manipulation of docetaxel resistant prostate cancer cell lines

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21 January 2018

MDR1 modulators improve the chemotherapy response of human hepatoblastoma to doxorubicin in vitro

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21 January 2018

Simultaneous delivery of doxorubicin and GG918 (Elacridar) by new polymer-lipid hybrid nanoparticles (PLN) for enhanced treatment of multidrug-resistant breast cancer

1 reference

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21 January 2018

Chemosensitivity determinants of irinotecan hydrochloride in hepatocellular carcinoma cell lines

1 reference

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21 January 2018

Intestinal transport of irinotecan in Caco-2 cells and MDCK II cells overexpressing efflux transporters Pgp, cMOAT, and MRP1.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Ixabepilone, a novel microtubule-targeting agent for breast cancer, is a substrate for P-glycoprotein (P-gp/MDR1/ABCB1) but not breast cancer resistance protein (BCRP/ABCG2).

1 reference

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21 January 2018

Expression, localization, and functional characteristics of breast cancer resistance protein in Caco-2 cells

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Expression and functional activity of breast cancer resistance protein (BCRP, ABCG2) transporter in the human choriocarcinoma cell line BeWo.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

A model of secreting murine mammary epithelial HC11 cells comprising endogenous Bcrp/Abcg2 expression and function

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Resistance to paclitaxel in a cisplatin-resistant ovarian cancer cell line is mediated by P-glycoprotein

1 reference

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21 January 2018

The interaction of bortezomib with multidrug transporters: implications for therapeutic applications in advanced multiple myeloma and other neoplasias

1 reference

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21 January 2018

ABC transporters and the accumulation of imatinib and its active metabolite CGP74588 in rat C6 glioma cells.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Effect of drug efflux transporters on placental transport of antiretroviral agent abacavir.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Comparison of bidirectional lamivudine and zidovudine transport using MDCK, MDCK-MDR1, and Caco-2 cell monolayers.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors.

1 reference

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21 January 2018

The bioflavonoid kaempferol is an Abcg2 substrate and inhibits Abcg2-mediated quercetin efflux

1 reference

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21 January 2018

Inhibition of ABCB1 Overcomes Cancer Stem Cell-like Properties and Acquired Resistance to MET Inhibitors in Non-Small Cell Lung Cancer

1 reference

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21 January 2018

Danofloxacin-mesylate is a substrate for ATP-dependent efflux transporters

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Transport inhibition of digoxin using several common P-gp expressing cell lines is not necessarily reporting only on inhibitor binding to P-gp

1 reference

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21 January 2018

A phase I and pharmacologic study of the MDR converter GF120918 in combination with doxorubicin in patients with advanced solid tumors

1 reference

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21 January 2018

Hepatocellular Disposition and Transporter Interactions with Tolvaptan and Metabolites in Sandwich-Cultured Human Hepatocytes

1 reference

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21 January 2018

The complexity of intestinal absorption and exsorption of digoxin in rats.

1 reference

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21 January 2018

Preclinical pharmacokinetic properties of the P-glycoprotein inhibitor GF120918A (HCl salt of GF120918, 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the mouse, rat, d

1 reference

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21 January 2018

Brain distribution and bioavailability of elacridar after different routes of administration in the mouse

1 reference

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21 January 2018

Saturable active efflux by p-glycoprotein and breast cancer resistance protein at the blood-brain barrier leads to nonlinear distribution of elacridar to the central nervous system

1 reference

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21 January 2018

P-glycoprotein, CYP3A, and Plasma Carboxylesterase Determine Brain Disposition and Oral Availability of the Novel Taxane Cabazitaxel (Jevtana) in Mice.

1 reference

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21 January 2018

Abcc4 together with abcb1 and abcg2 form a robust cooperative drug efflux system that restricts the brain entry of camptothecin analogues

1 reference

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21 January 2018

Pharmacokinetic modeling to assess factors affecting the oral bioavailability of the lactone and carboxylate forms of the lipophilic camptothecin analogue AR-67 in rats

1 reference

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21 January 2018

P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan

1 reference

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21 January 2018

Evaluation of the P-glycoprotein- and breast cancer resistance protein-mediated brain penetration of 11C-labeled topotecan using small-animal positron emission tomography

1 reference

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21 January 2018

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

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Oral co-administration of elacridar and ritonavir enhances plasma levels of oral paclitaxel and docetaxel without affecting relative brain accumulation

1 reference

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21 January 2018

Enhanced brain accumulation of pazopanib by modulating P-gp and Bcrp1 mediated efflux with canertinib or erlotinib.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Role of P-glycoprotein on the brain penetration and brain pharmacodynamic activity of the MEK inhibitor cobimetinib.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

ABCG2 and ABCB1 Limit the Efficacy of Dasatinib in a PDGF-B-Driven Brainstem Glioma Model

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Function of the blood-brain barrier and restriction of drug delivery to invasive glioma cells: findings in an orthotopic rat xenograft model of glioma

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Breast Cancer Resistance Protein and P-Glycoprotein Influence In Vivo Disposition of 11C-Erlotinib.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [(11)C]gefitinib

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Pharmacokinetic assessment of efflux transport in sunitinib distribution to the brain

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

The role of the breast cancer resistance protein (ABCG2) in the distribution of sorafenib to the brain

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Co-administration strategy to enhance brain accumulation of vandetanib by modulating P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) mediated efflux with m-TOR inhibitors.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Role of P-glycoprotein in the distribution of the HIV protease inhibitor atazanavir in the brain and male genital tract.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Assessing safety and efficacy of directed P-glycoprotein inhibition to improve the pharmacokinetic properties of saquinavir coadministered with ritonavir

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Pharmacokinetic interactions between 20(S)-ginsenoside Rh2 and the HIV protease inhibitor ritonavir in vitro and in vivo.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Convallatoxin: a new P-glycoprotein substrate

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Factors Influencing the Central Nervous System Distribution of a Novel Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GSK2126458: Implications for Overcoming Resistance with Combination Therapy for Melanoma Brain Metastases

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

P-Glycoprotein (ABCB1) limits the brain distribution of YQA-14, a novel dopamine D3 receptor antagonist

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Investigation of efflux transport of dehydroepiandrosterone sulfate and mitoxantrone at the mouse blood-brain barrier: a minor role of breast cancer resistance protein

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Coadministration of P-glycoprotein modulators on loperamide pharmacokinetics and brain distribution.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Cerebral uptake of mefloquine enantiomers with and without the P-gp inhibitor elacridar (GF1210918) in mice

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Estimation of the unbound brain concentration of P-glycoprotein substrates or nonsubstrates by a serial cerebrospinal fluid sampling technique in rats.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Inhibiting drug efflux transporters improves efficacy of ALS therapeutics

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Interaction of innovative small molecule drugs used for cancer therapy with drug transporters

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

P-glycoprotein inhibition increases the brain distribution and antidepressant-like activity of escitalopram in rodents

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Whole-Body Distribution and Radiation Dosimetry of 11C-Elacridar and 11C-Tariquidar in Humans.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Pharmacokinetics of single ascending doses of the P-glycoprotein inhibitor tariquidar in healthy subjects

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer.

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

Influence of breast cancer resistance protein (Abcg2) and p-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec® ) across the mouse blood-brain barrier

1 reference

https://api.crossref.org/works/10.1007%2FS13318-017-0411-4

21 January 2018

In vitro transport of gimatecan (7-t-butoxyiminomethylcamptothecin) by breast cancer resistance protein, P-glycoprotein, and multidrug resistance protein 2.

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Phase I trial of XR9576 in healthy volunteers demonstrates modulation of P-glycoprotein in CD56+ lymphocytes after oral and intravenous administration.

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Clinical pharmacokinetics of doxorubicin in combination with GF120918, a potent inhibitor of MDR1 P-glycoprotein

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Expression of the mdr (P-glycoprotein) gene in Chinese hamster digestive tracts

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Oral bioavailability of digoxin is enhanced by talinolol: evidence for involvement of intestinal P-glycoprotein

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Role of human placental efflux transporter P-glycoprotein in the transfer of buprenorphine, levo-alpha-acetylmethadol, and paclitaxel

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A simplified protocol employing elacridar in rodents: a screening model in drug discovery to assess P-gp mediated efflux at the blood brain barrier

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel.

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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 inhibitors to enable the brain penetration of imatinib

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat.

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Ochratoxin A secretion by ATP-dependent membrane transporters in Caco-2 cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Potentiation of anticancer-drug cytotoxicity by multidrug-resistance chemosensitizers involves alterations in membrane fluidity leading to increased membrane permeability.

1 reference

https://pubmed.ncbi.nlm.nih.gov/28374336

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1007/S13318-017-0411-4

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

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0 references

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

7 September 2017

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