Drug intelligence / Profile preview

zoledronic acid + cyclophosphamide + epirubicin + S-1 + methotrexate

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

A multi-agent **combination chemotherapy regimen** consisting of zoledronic acid, cyclophosphamide, epirubicin, S-1, and methotrexate. This combination targets cancer through multiple mechanisms: - **Zoledronic acid** is a potent bisphosphonate primarily used to inhibit bone resorption and is commonly administered for bone metastases and related complications. It also exerts direct and indirect antitumor effects, including apoptosis induction and inhibition of tumor cell proliferation. - **Cyclophosphamide** is an alkylating agent that crosslinks DNA, leading to cell death, and it possesses both cytotoxic and immunosuppressive effects. - **Epirubicin** is an anthracycline antibiotic that intercalates into DNA and inhibits topoisomerase II, resulting in DNA breakage and inhibition of cell replication. - **S-1** is an oral fluoropyrimidine combination that includes tegafur (a prodrug of 5-fluorouracil), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (which reduces gastrointestinal toxicity); it inhibits DNA synthesis in rapidly dividing cells. - **Methotrexate** is an antimetabolite and antifolate agent, inhibiting dihydrofolate reductase, thereby blocking DNA synthesis and cell replication. This specific combination does not correspond to a standardized, named regimen but is sometimes used or investigated in the context of advanced cancers, particularly where multiple mechanisms of action and synergistic effects are desired, especially in metastatic or refractory settings[1][3][7].

02

Targets

TOP2A (DNA topoisomerase II)TS (Thymidylate synthase)DPYD (Dihydropyrimidine dehydrogenase)DHFR (Dihydrofolate reductase)DNAFDPS (Farnesyl pyrophosphate synthase)OPRT (Orotidine 5'-phosphate decarboxylase)

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