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