In vitro studies were conducted to identify the hepatic cytochrome P450 (CYP) forms involved in the oxidative metabolism of [14C]ABT-761 and its N-dehydroxylated metabolite, [14C]ABT-438, by human liver microsomes. The two compounds were metabolized by parallel pathways, to form the corresponding methylene bridge hydroxy metabolites. There was no evidence of sulfoxidation and/or ring hydroxylat...

BACKGROUND Factors influencing the oral flora of premature infants have not been adequately investigated. OBJECTIVE To investigate the effects of gestational age and of anti-bacterial therapy on the oral flora of premature infants. METHODS Oral cultures were obtained at age 1 day and age 10 days from 65 premature infants, divided into three groups: a) 24 neonates of 30-34 weeks gestation wh...

reason that Schoenwaelder and Jackson did not observe an increase in cytosolic free calcium at higher concentrations of ABT-263 is unclear but may well relate to differences such as higher platelet density (3 108 cells/mL used by them compared with the lower cell density 5 107 cells/mL used in our study).3 In this regard we have previously reported that the efficacy of both ABT-263 (Navitoclax)...

Nasopharyngeal specimens for culture of Chlamydia pneumoniae were obtained from patients with community-acquired pneumonia enrolled in a randomized study comparing the novel ketolide antibiotic ABT-773 at a dose of 150 mg once a day to 150 mg twice a day, by mouth for 10 days. C. pneumoniae was eradicated from the nasopharynx of 10 of 10 (100%) microbiologically evaluable patients. MICs and MBC...

HIV protease inhibitor ABT-378 (ABT-378) was metabolized very extensively and rapidly by liver microsomes from mouse, rat, dog, monkey, and humans. The rates of NADPH-dependent metabolism of ABT-378 ranged from 2.39 to 9.80 nmol.mg microsomal protein-1.min-1, with monkey liver microsomes exhibiting the highest rates of metabolism. ABT-378 was metabolized to 12 metabolites (M-1 to M-12), which w...

ABT-384 [1-piperazineacetamide, N-[5-(aminocarbonyl) tricyclo[3.3. 1.13,7]dec-2-yl]-a,a-dimethyl-4-[5-(trifluoromethyl)-2-pyridinyl]-, stereoisomer] is a potent and selective inhibitor of 11b-hydroxysteroid dehydrogenase type 1 (HSD-1). ABT-384 has been shown to be safe and well tolerated in humans at doses up to 100 mg daily, and to fully inhibit both peripheral and brain HSD-1 at a dose of 2 ...

Navitoclax (ABT-263), a Bcl-2 family inhibitor and ABT-199, a Bcl-2 selective inhibitor, are high molecular weight, high logP molecules that show low solubility in aqueous media. While these properties are associated with low oral bioavailability (F), both navitoclax and ABT-199 showed moderate F in preclinical species. The objective of the described study was to determine if lymphatic transpor...

Epithelial ovarian cancer (EOC) is the most lethal gynecologic malignancy and is often not diagnosed until late stages due to its asymptomatic nature.Women diagnosedwith EOC typically undergo surgical debulking followed by chemotherapy; however, disease recurrence often occurs. In this study,we evaluated the ability of the thrombospondin-1 mimetic peptide, ABT-898, to regress established, late-...