Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers.
Olaparib has few of the adverse effects of conventional chemotherapy, inhibits PARP, and has antitumor activity in cancer associated with the BRCA1 or BRCa2 mutation.
Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.
A new tetracyclic analogue of FTC, Ko143, is evaluated as a practical inhibitor of BCRP, proving highly active for increasing the intracellular drug accumulation and reversing Bcrp1/BCRP-mediated multidrug resistance.
Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues.
The apical localization in the epithelium of the small intestine and colon indicates a possible role of BCRP in the regulation of the uptake of p.o. delivered B CRP substrates by back-transport of substrate drugs entering from the gut lumen and is consistent with the hypothesis of a protective role ofBCRP for the fetus.
An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons.
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for Dihydropyrimidine Dehydrogenase Genotype and Fluoropyrimidine Dosing: 2017 Update
- U. Amstutz, L. M. Henricks, M. Schwab
- Medicine, BiologyClinical pharmacology and therapy
- 1 February 2018
The purpose of this guideline is to provide information for the interpretation of clinical dihydropyrimidine dehydrogenase (DPYD) genotype tests so that the results can be used to guide dosing of…
Evidence for Two Interacting Ligand Binding Sites in Human Multidrug Resistance Protein 2 (ATP Binding Cassette C2)*
It is proposed that MRP2 contains two similar but nonidentical ligand binding sites: one site from which substrate is transported and a second site that regulates the affinity of the transport site for the substrate.
Clinical Pharmacokinetics of Therapeutic Monoclonal Antibodies
The parenteral administration, slow tissue distribution and long elimination half-life are the most pronounced clinical pharmacokinetic characteristics of mAbs.
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
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.
Dabrafenib and Trametinib Treatment in Patients With Locally Advanced or Metastatic BRAF V600-Mutant Anaplastic Thyroid Cancer.
Dabrafenib plus trametinib is the first regimen demonstrated to have robust clinical activity in BRAF V600E-mutated anaplastic thyroid cancer and was well tolerated, representing a meaningful therapeutic advance for this orphan disease.