Drug intelligence / Profile preview

fostamatinib + paclitaxel

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

Overview

Fostamatinib + paclitaxel is a combination therapy under investigation primarily for the treatment of recurrent platinum-resistant ovarian cancer. Fostamatinib is an orally available small molecule prodrug that inhibits spleen tyrosine kinase (SYK), a key mediator in immune cell signaling and implicated in resistance to chemotherapy, particularly taxanes like paclitaxel. Paclitaxel is a well-established chemotherapeutic agent that stabilizes microtubules, thereby inhibiting cell division and promoting apoptosis in rapidly dividing cells. Preclinical studies have shown that SYK inhibition by fostamatinib can sensitize resistant ovarian cancer cells to the cytotoxic effects of paclitaxel, enhancing G2/M arrest and apoptosis. This combination has entered phase 1 clinical trials for patients with recurrent platinum-resistant ovarian cancer[2][4][6][8]. Fostamatinib was developed by Rigel Pharmaceuticals and is marketed as Tavalisse for chronic immune thrombocytopenia; paclitaxel was originally developed by the National Cancer Institute and marketed as Taxol.

Other names
R788 (for fostamatinib)R406 (active metabolite of fostamatinib)NSC 125973 (for paclitaxel)
02

Targets

TUBB (Tubulin (alpha and beta subunits))LYN (LYN proto-oncogene, Src family tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)SYK (Spleen Tyrosine Kinase)

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