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R406, an Orally Available Spleen Tyrosine Kinase Inhibitor Blocks Fc Receptor Signaling and Reduces Immune Complex-Mediated Inflammation
- Sylvia Braselmann, V. Taylor, +18 authors E. S. Masuda
- Chemistry, Medicine
- Journal of Pharmacology and Experimental…
- 1 December 2006
Recent compelling evidence has lead to renewed interest in the role of antibodies and immune complexes in the pathogenesis of several autoimmune disorders, such as rheumatoid arthritis. These immune… Expand
Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen
- J. Mclaughlin, Vadim Markovtsov, +31 authors Y. Hitoshi
- Medicine, Biology
- Journal of Cancer Research and Clinical Oncology
PurposeAurora kinases play a key role in mitotic progression. Over-expression of Aurora kinases is found in several human cancers and correlated with histological malignancy and clinical outcomes.… Expand
An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus.
OBJECTIVE To assess whether R788, an orally bioavailable small molecule inhibitor of spleen tyrosine kinase (Syk)-dependent signaling, could modulate disease in lupus-prone (NZB x NZW)F1 (NZB/NZW)… Expand
Developmental toxicity associated with receptor tyrosine kinase Ret inhibition in reproductive toxicity testing.
- George R. Clemens, R. Schroeder, +6 authors E. Grossbard
- Birth defects research. Part A, Clinical and…
- 1 February 2009
BACKGROUND Urogenital abnormalities are among the most common of all human birth defects. In developmental toxicity studies with the Syk kinase inhibitor R788, a spectrum of findings, including renal… Expand
The importance of intestinal residence time of absorption enhancer on drug absorption and implication on formulative considerations
Abstract Absorption enhancers are efficient in small body cavities such as the nasal and the rectum. However, in the gastrointestinal tract, where the volume and amount of liquids are large and… Expand
Pharmacokinetics of fostamatinib, a spleen tyrosine kinase (SYK) inhibitor, in healthy human subjects following single and multiple oral dosing in three phase I studies.
- Muhammad Baluom, E. Grossbard, T. Mant, D. T. Lau
- British journal of clinical pharmacology
- 1 July 2013
AIM Fostamatinib (R788) is an orally dosed prodrug designed to deliver the active metabolite R940406 (R406), a spleen tyrosine kinase (SYK) inhibitor, for the treatment of rheumatoid arthritis. The… Expand
Absorption enhancement of calcitonin in the rat intestine by carbopol-containing submicron emulsions
The absorption of salmon calcitonin (sCT) in the jejunum and the colon of the rat from submicron emulsions with (MA SME) and without (SME) the adhesive polymer Carbopol®940 was studied in… Expand
The rationale for peptide drug delivery to the colon and the potential of polymeric carriers as effective tools
Abstract The explicit use of colon-specific drug delivery systems is for the local treatment of colon diseases such as ulcerative colitis. Some efficient therapeutic systems, primarily prodrugs and… Expand
The effect of soluble complement receptor type 1 on acute humoral xenograft rejection in hDAF-transgenic pig-to-primate life-supporting kidney xenografts.
BACKGROUND In pig-to-nonhuman primate solid organ xenotransplantation using organs from donors transgenic for human decay-accelerating factor (hDAF), the main type of rejection is antibody-mediated… Expand
Novel percutaneous adventitial drug delivery system for regional vascular treatment
- F. Ikeno, J. Lyons, H. Kaneda, Muhammad Baluom, L. Benet, Mehrdad Rezaee
- Catheterization and cardiovascular interventions…
- 1 October 2004
A novel intracoronary microsyringe system (MicroSyringe) was developed for regulated drug injection into the adventitial space. In this report, the feasibility, safety, and distribution pattern of… Expand