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Doxorubicin, Methotrexate

Gustave Roussy, Cancer Campus, Grand Paris · Phase 3 active Small molecule

This combination uses doxorubicin to intercalate DNA and inhibit topoisomerase II, while methotrexate inhibits dihydrofolate reductase to disrupt nucleotide synthesis, together producing synergistic cytotoxic effects against cancer cells.

This combination uses doxorubicin to intercalate DNA and inhibit topoisomerase II, while methotrexate inhibits dihydrofolate reductase to disrupt nucleotide synthesis, together producing synergistic cytotoxic effects against cancer cells. Used for Breast cancer (likely primary indication given phase 3 status), Other solid tumors or hematologic malignancies (specific indication not provided).

At a glance

Generic nameDoxorubicin, Methotrexate
SponsorGustave Roussy, Cancer Campus, Grand Paris
Drug classChemotherapy combination (anthracycline + antimetabolite)
TargetTopoisomerase II (doxorubicin); Dihydrofolate reductase (methotrexate)
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Doxorubicin is an anthracycline chemotherapy agent that intercalates into DNA and prevents topoisomerase II-mediated DNA repair, leading to DNA strand breaks and cell death. Methotrexate is an antimetabolite that inhibits dihydrofolate reductase, blocking thymidylate synthase and reducing dTMP production, thereby impairing DNA synthesis. The combination exploits complementary mechanisms to enhance cytotoxicity across multiple cancer cell populations.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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