Current Drug Metabolism - Volume 11, Issue 7, 2010

Glucuronidation is one of the main phase II metabolic reactions in humans and animals. A variety of analytical techniques and methods have been used for the detection and quantification of glucuronides of both endogenous and xenobiotic compounds from different biological samples of humans and animals. Drug metabolism has been extensively studied with both in vitro and in vivo experiments under various conditions. Read More

The in vitro metabolic stability assays are indispensable for screening the metabolic liability of new chemical entities (NCEs) in drug discovery. Intrinsic clearance (CLint) values from liver microsomes and/or hepatocytes are frequently used to assess metabolic stability as well as to quantitatively predict in vivo hepatic plasma clearance (CLH). An often used approximation is the so called wellstirred model which has g Read More

Bleomycin is a potent chemotherapeutic agent that can mediate cell killing by attacking the DNA. It is used in combination with other antineoplastic agents to effectively treat lymphomas, testicular carcinomas and squamous cell carcinomas of the cervix, head and neck. However, resistance to bleomycin remains a persistent limitation in exploiting the full therapeutic benefit of the drug for other types of cancers. Herein, we revi Read More

The human breast cancer resistance protein (BCRP/ABCG2) is the second member of the G subfamily of the large ATPbinding cassette (ABC) transporter superfamily. BCRP was initially discovered in multidrug resistant breast cancer cell lines where it confers resistance to chemotherapeutic agents such as mitoxantrone, topotecan and methotrexate by extruding these compounds out of the cell. BCRP is ca Read More

Tyrosine kinase inhibitors (TKIs) are a new class of highly-selective and molecularly targeted anticancer agents. Most of these newly developed TKIs are hydrophobic, thus allowing them to rapidly penetrate the cell membrane to reach their specific intracellular targets. However, their therapeutic potential could be significantly hindered by the overexpression of certain ATP binding cassette (ABC) membrane transporters, which extr Read More