2022
P‐Glycoprotein and Breast Cancer Resistance Protein Transporter Inhibition by Cyclosporine and Quinidine on the Pharmacokinetics of Oral Rimegepant in Healthy Subjects
Bhardwaj R, Collins J, Stringfellow J, Madonia J, Anderson M, Finley J, Stock D, Coric V, Croop R, Bertz R. P‐Glycoprotein and Breast Cancer Resistance Protein Transporter Inhibition by Cyclosporine and Quinidine on the Pharmacokinetics of Oral Rimegepant in Healthy Subjects. Clinical Pharmacology In Drug Development 2022, 11: 889-897. PMID: 35304977, PMCID: PMC9311059, DOI: 10.1002/cpdd.1088.Peer-Reviewed Original ResearchConceptsBreast cancer resistance protein transporterPlasma concentration-time curveSingle oral doseGeometric mean ratiosConcentration-time curveP-glycoproteinOral doseHealthy subjectsSmall-molecule calcitonin gene-related peptide receptor antagonistCalcitonin gene-related peptide receptor antagonistStrong P-glycoprotein inhibitorBreast cancer resistance protein (BCRP) inhibitionPeptide receptor antagonistTime 0Mean ratioP-glycoprotein inhibitorsP-glycoprotein transporterConcomitant administrationCrossover studyReceptor antagonistPreventive treatmentCyclosporineCoadministrationTransporter inhibitionPharmacokinetics
2005
Phase II study of tariquidar, a selective P‐glycoprotein inhibitor, in patients with chemotherapy‐resistant, advanced breast carcinoma
Pusztai L, Wagner P, Ibrahim N, Rivera E, Theriault R, Booser D, Symmans FW, Wong F, Blumenschein G, Fleming DR, Rouzier R, Boniface G, Hortobagyi GN. Phase II study of tariquidar, a selective P‐glycoprotein inhibitor, in patients with chemotherapy‐resistant, advanced breast carcinoma. Cancer 2005, 104: 682-691. PMID: 15986399, DOI: 10.1002/cncr.21227.Peer-Reviewed Original ResearchConceptsAdministration of tariquidarP-gp expressionSestamibi scanBreast carcinomaSestamibi uptakeP-gp-positive tumorsTaxane-containing chemotherapy regimensDocetaxel-related toxicitiesLimited clinical activityObjective tumor responsePercent of patientsPhase II studyAdvanced breast carcinomaP-glycoprotein inhibitor tariquidarP-glycoprotein inhibitorsMultidrug resistance modulationP-gp transporterMultidrug resistance inhibitorsSame chemotherapyStable diseaseChemotherapy regimenChemotherapy regimensTaxane chemotherapyClinical responseDose modification
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