Drug intelligence / Profile preview

capecitabine + exisulind

Development stage
Phase 2
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Capecitabine + exisulind is an investigational combination therapy consisting of two small molecule drugs, capecitabine and exisulind, studied primarily in metastatic breast cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU) that inhibits thymidylate synthase, interfering with DNA synthesis and leading to cell death in rapidly dividing tumor cells. Exisulind belongs to the class of selective apoptotic antineoplastic drugs (SAANDs); it induces apoptosis selectively in precancerous and cancerous cells by inhibiting cyclic guanosine monophosphate (cGMP) phosphodiesterases, particularly PDE-2 and PDE-5. The combination has been evaluated for safety and efficacy in patients with metastatic breast cancer who had previously received anthracycline and taxane chemotherapies. Clinical studies found the regimen to be generally well tolerated, with hand-foot syndrome, fatigue, diarrhea, and granulocytopenia as notable adverse events. The anticancer activity was similar to that of capecitabine alone[1][2][4][7][8].

02

Targets

NF-κBPDE2 (Phosphodiesterase 2)PDE5 (Phosphodiesterase 5A)TS (Thymidylate synthase)

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