Drug intelligence / Profile preview

taxane + mitoxantrone + thiotepa

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination chemotherapy regimen comprised of a **taxane** (such as docetaxel or paclitaxel), **mitoxantrone**, and **thiotepa**, most commonly evaluated in high-dose chemotherapy or salvage therapy for metastatic breast cancer and potentially other advanced malignancies. - **Taxanes** (e.g., docetaxel, paclitaxel) are microtubule inhibitors that disrupt cell division by stabilizing tubulin, thus inhibiting microtubule depolymerization and halting mitosis. - **Mitoxantrone** is an anthracenedione that intercalates into DNA and inhibits topoisomerase II, resulting in DNA damage and cell death. - **Thiotepa** is an alkylating agent that cross-links DNA, preventing cell replication and leading to apoptosis. This combination is researched primarily as part of high-dose regimens for treatment-refractory or metastatic cancers, especially **breast cancer**. The regimen is associated with potent myelosuppression and requires specialized supportive care.

02

Targets

DNAMDM2 (Mouse double minute 2 homolog)CHEK1 (Checkpoint kinase 1)TOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))mTOR (Mammalian target of rapamycin kinase)

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