Drug intelligence / Profile preview

fostamatinib + pioglitazone

Development stage
Unknown
Lead developer
Rigel Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

**fostamatinib + pioglitazone** refers to the coadministration of two small molecule drugs: fostamatinib, an oral spleen tyrosine kinase (Syk) inhibitor originally developed for autoimmune diseases such as rheumatoid arthritis and approved for chronic immune thrombocytopenia, and pioglitazone, a thiazolidinedione class peroxisome proliferator-activated receptor gamma (PPARγ) agonist used as an insulin sensitizer in type 2 diabetes. The combination has been studied for pharmacokinetic drug–drug interactions; fostamatinib is a prodrug metabolized to R406, which can modulate CYP2C8 activity and potentially affect pioglitazone metabolism[1][3][5]. No unique clinical indication for the combined use has been approved, but formal studies found no major changes in safety or pharmacokinetics in healthy volunteers, and vigilance is advised when coadministering, due to possible CYP2C8 and transporter-mediated interactions[1][2].

Other names
fostamatinib disodiumR788R-788R 788R406R-406R 406pioglitazone hydrochloride
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)VEGFR2 (Vascular endothelial growth factor receptor 2)SFK (SRC family kinases)SYK (Spleen Tyrosine Kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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