Drug intelligence / Profile preview

doxorubicin + lonidamine + prednisone + sulindac

Development stage
Preclinical
Lead developer
Farmitalia
Modality
Small Molecules
Administration
Oral (prednisone, Sulindac, Lonidamine), Intravenous (doxorubicin)
01

Overview

A multi-agent **combination chemotherapy regimen** comprising doxorubicin, lonidamine, prednisone, and sulindac. Each component has a distinct mechanism of action: - **Doxorubicin** is a cytotoxic anthracycline that intercalates into DNA, inhibits topoisomerase II, and generates free radicals, leading to DNA damage and apoptosis in cancer cells. - **Lonidamine** is a small molecule inhibitor that targets tumor cell energy metabolism, inhibiting glycolysis and mitochondrial function, and can potentiate doxorubicin efficacy by de-energizing tumors and reversing drug resistance[1][2][3][4]. - **Prednisone** is a synthetic glucocorticoid used for its anti-inflammatory and immunosuppressive effects, and as a cytotoxic agent in some hematological malignancies. - **Sulindac** is a nonsteroidal anti-inflammatory drug (NSAID) with additional antitumor properties via inhibition of cyclooxygenase enzymes and effects on cell proliferation and apoptosis. Experimental data support the combination of doxorubicin and lonidamine for synergistic antitumor activity, especially in models of drug-resistant cancers. The specific four-drug combination (including prednisone and sulindac) does not appear in peer-reviewed published clinical trials or major guidelines as of 2024, but each drug is individually approved and their pharmacological actions are well characterized.

02

Targets

MPC (Mitochondrial pyruvate carrier)SLC16A1 (Mitochondrial Pyruvate Carrier)TOP2A (DNA topoisomerase II)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)GR (Glucocorticoid receptor)DNAMCT4 (Monocarboxylate transporter 4)PGHS-1 (Prostaglandin G/H Synthase 1)MCT2 (Monocarboxylate transporter 2)

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