Drug intelligence / Profile preview

indisulam + capecitabine

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

Overview

This is a combination of **indisulam** and **capecitabine**, two small molecule chemotherapeutic agents tested together for anticancer activity, primarily in patients with advanced solid tumors and metastatic breast cancer. **Indisulam** (also known as E7070) acts as a multi-targeted cell cycle inhibitor, inducing cell cycle arrest in the G1 phase and promoting apoptosis by interfering with cyclin-dependent kinases and other cell cycle-regulating proteins. **Capecitabine** is an oral prodrug of 5-fluorouracil (5-FU), which is converted to 5-FU preferentially in tumor tissues; 5-FU acts as an antimetabolite, inhibiting thymidylate synthase and disrupting DNA synthesis in rapidly dividing cells. The combination is being investigated for its potential synergistic antineoplastic effects, but exhibits notable pharmacokinetic interaction leading to increased indisulam exposure and heightened risk of myelotoxicity (particularly neutropenia) in subsequent treatment cycles due to inhibition of CYP2C9-mediated metabolism of indisulam by capecitabine/5-FU. Indications explored include metastatic breast cancer and other solid tumors[2][4][6].

Brand names
Xeloda
Other names
capecitabineindisulam
02

Targets

TS (Thymidylate synthase)CDK2 (Cyclin-dependent kinase 2)

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