Skip to main content
Key Specialties
Cardiology Diabetology Endocrinology Gastroenterology Geriatrics and Gerontology Gynecology and Obstetrics Hematology Infectious Disease Internal Medicine Nephrology Neurology Oncology Pediatrics Respiratory Medicine Rheumatology Surgery
Congress Coverage
2024 ACC Congress 2023 ESMO Congress 2023 EASD Congress 2023 ERS Congress 2023 ESC Congress 2023 EHA Congress 2023 ASCO Annual Meeting
Clinical Collections
Advances in Alzheimer’s

Keynote webinar | Spotlight on sleep in brain health

LIVE: Thursday 2nd May 2024, 18:00-19:30 (CEST)

Quality sleep is essential for health. But what happens to our brains when sleep patterns are disturbed? Join our experts to explore the interplay between sleep disruption and neurological diseases, and the questions that you need to be asking your patients to help you prevent the harmful effects of sleep deprivation.
ADVANCED SEARCH
Log in
Top
Cancer Chemotherapy and Pharmacology
Published in: Cancer Chemotherapy and Pharmacology 5/2016

01-11-2016 | Letter to the Editor

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

Author: Nuggehally R. Srinivas

Published in: Cancer Chemotherapy and Pharmacology | Issue 5/2016

Login to get access

Excerpt

Fox et al. report an interesting pharmacokinetic/pharmacodynamic study of tariquidar, a potent Pgp inhibitor, in combination with three cytotoxic drugs agents namely docetaxel, vinorelbine, and doxorubicin [1]. The functional tracking of the ability of tariquidar to block Pgp efflux was monitored using rhodamine assay in the PBMCs prepared from the blood samples of patients, and the pharmacodynamic activity was measured by 99mTc-sestamibi scintigraphy imaging in tumors [1]. …
Literature
1.
Fox E, Widemann BC, Pastakia D et al (2015) 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. Cancer Chemother Pharmacol 76:1273–1283CrossRefPubMed
2.
Bruno R, Sanderink GJ (1993) Pharmacokinetics and metabolism of Taxotere (docetaxel). Cancer Surv 17:305–313PubMed
3.
4.
van Zuylen L, Verweij J, Nooter K et al (2000) Role of intestinal P-glycoprotein in the plasma and fecal disposition of docetaxel in humans. Clin Cancer Res 6:2598–2603PubMed
5.
Kelly RJ, Draper D, Chen CC et al (2011) A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer. Clin Cancer Res 17:569–580CrossRefPubMed
6.
Levêque D, Jehl F (1996) Clinical pharmacokinetics of vinorelbine. Clin Pharmacokinet 31:184–197CrossRefPubMed
7.
Wargin WA, Lucas VS (1994) The clinical pharmacokinetics of vinorelbine (Navelbine). Semin Oncol 21(5 Suppl 10):21–27PubMed
8.
Levêque D, Merle-Melet M, Bresler L et al (1993) Biliary elimination and pharmacokinetics of vinorelbine in micropigs. Cancer Chemother Pharmacol 32:487–490CrossRefPubMed
9.
Abraham J, Edgerly M, Wilson R et al (2009) A phase I study of the P-glycoprotein antagonist tariquidar in combination with vinorelbine. Clin Cancer Res 15:3574–3582CrossRefPubMed
10.
Mross K, Mayer U, Langenbuch T, Hamm K, Burk K, Hossfeld D (1990) Toxicity, pharmacokinetics and metabolism of iododoxorubicin in cancer patients. Eur J Cancer 26:1156–1162CrossRefPubMed
11.
Ballet F, Vrignaud P, Robert J, Rey C, Poupon R (1987) Hepatic extraction, metabolism and biliary excretion of doxorubicin in the isolated perfused rat liver. Cancer Chemother Pharmacol 19:240–245CrossRefPubMed
12.
Camaggi CM, Strocchi E, Comparsi R, Testoni F, Angelelli B, Pannuti F (1986) Biliary excretion and pharmacokinetics of 4’epidoxorubicin (epirubicin) in advanced cancer patients. Cancer Chemother Pharmacol 18:47–50CrossRefPubMed
13.
Asakura E, Nakayama H, Sugie M et al (2004) Azithromycin reverses anticancer drug resistance and modifies hepatobiliary excretion of doxorubicin in rats. Eur J Pharmacol 484:333–339CrossRefPubMed
Metadata
Title
Understanding the role of tariquidar, a potent Pgp inhibitor, in combination trials with cytotoxic drugs: What is missing?
Author
Nuggehally R. Srinivas
Publication date
01-11-2016
Publisher
Springer Berlin Heidelberg
Published in
Cancer Chemotherapy and Pharmacology / Issue 5/2016
Print ISSN: 0344-5704
Electronic ISSN: 1432-0843
DOI
https://doi.org/10.1007/s00280-016-3044-4

Other articles of this Issue 5/2016

Cancer Chemotherapy and Pharmacology 5/2016 Go to the issue

Original Article

JD enhances the anti-tumour effects of low-dose paclitaxel on gastric cancer MKN45 cells both in vitro and in vivo

Original Article

The UCA1/miR-204/Sirt1 axis modulates docetaxel sensitivity of prostate cancer cells

Original Article

Randomized phase 1 crossover study assessing the bioequivalence of capsule and tablet formulations of dovitinib (TKI258) in patients with advanced solid tumors

Original Article

Synthesis of polydopamine as a new and biocompatible coating of magnetic nanoparticles for delivery of doxorubicin in mouse breast adenocarcinoma

Original Article

Potential influence of being overweight on the development of hepatic dysfunction in Japanese patients with EGFR-mutated non-small cell lung cancer undergoing gefitinib monotherapy: the Okayama Lung Cancer Study Group experience

Original Article

Population pharmacokinetic–pharmacodynamic modeling and model-based prediction of docetaxel-induced neutropenia in Japanese patients with non-small cell lung cancer
Webinar | 19-02-2024 | 17:30 (CET)

Keynote webinar | Spotlight on antibody–drug conjugates in cancer

Watch now

Antibody–drug conjugates (ADCs) are novel agents that have shown promise across multiple tumor types. Explore the current landscape of ADCs in breast and lung cancer with our experts, and gain insights into the mechanism of action, key clinical trials data, existing challenges, and future directions.

Dr. Véronique Diéras
Prof. Fabrice Barlesi
Developed by: Springer Medicine
Image Credits