Drug intelligence / Profile preview

Tesetaxel + capecitabine

Development stage
Unknown
Lead developer
Odonate Therapeutics
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tesetaxel + capecitabine is an investigational all-oral combination chemotherapy regimen for the treatment of advanced solid tumors, particularly metastatic breast cancer. Tesetaxel is a novel oral taxane and semisynthetic microtubule inhibitor that disrupts cell division by stabilizing microtubules and preventing their depolymerization. Unlike other taxanes such as paclitaxel and docetaxel, tesetaxel is not effluxed by the P-glycoprotein pump and has high oral bioavailability with a long half-life. Capecitabine is an orally administered prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in tumor tissue; 5-FU acts as an antimetabolite inhibiting thymidylate synthase and interfering with DNA synthesis. The combination has shown improved progression-free survival compared to capecitabine alone in patients with HER2-negative, hormone receptor-positive metastatic breast cancer[2][4][5]. Tesetaxel was developed by Odonate Therapeutics.

02

Targets

TUBB (Tubulin (alpha and beta subunits))TS (Thymidylate synthase)

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