Drug intelligence / Profile preview

fostamatinib + rifampicin

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

Overview

**fostamatinib + rifampicin** is a combination of the spleen tyrosine kinase inhibitor fostamatinib and the antibiotic rifampicin. Fostamatinib is primarily used for chronic immune thrombocytopenia (ITP) and acts through inhibition of spleen tyrosine kinase (Syk), thereby preventing antibody-mediated platelet destruction. Rifampicin is a potent antibacterial agent, commonly used for tuberculosis and other infections, and is known for its strong induction of cytochrome P450 enzymes, especially CYP3A4. Co-administration of rifampicin with fostamatinib leads to a major pharmacokinetic interaction: rifampicin strongly induces CYP3A4, significantly decreasing exposure to fostamatinib's active metabolite R406 (AUC reduced by 75%, Cmax by 59%), which can result in reduced efficacy of fostamatinib. This combination is not recommended unless under specific clinical investigation due to the marked reduction in fostamatinib's therapeutic effect[1][5][7].

Other names
fostamatinib disodiumR788R-788R 788R935788R-935788R 935788rifampin
02

Targets

SYK (Spleen Tyrosine Kinase)

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