doxorubicin + tesmilifene

Doxorubicin + tesmilifene is a combination therapy investigated primarily for advanced and metastatic breast cancer. Doxorubicin is an anthracycline antibiotic widely used as a cytotoxic chemotherapeutic agent, acting mainly by intercalating DNA and inhibiting topoisomerase II, leading to apoptosis in rapidly dividing cells. Tesmilifene (DPPE; N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine) is a small-molecule chemopotentiator developed to enhance the efficacy of standard cytotoxic drugs such as anthracyclines. Tesmilifene acts as a selective ligand of antiestrogen binding sites without affinity for estrogen receptors and has been shown to potentiate the cytotoxicity of chemotherapy agents both in vitro and in vivo[3][6]. The proposed mechanism involves disruption of cancer cell energetics, reduction of drug resistance via effects on energy-dependent extrusion pumps like p-glycoprotein, and increased generation of reactive oxygen species within abnormal mitochondria[4][7]. In phase III clinical trials, this combination demonstrated significantly improved overall survival compared to doxorubicin alone but was associated with increased gastrointestinal and central nervous system toxicity[1][6][8]. Despite initial promise, further development was discontinued after subsequent studies failed to confirm consistent clinical benefit[2].

Brand names

tesmilifene

Other names

doxorubicin + DPPEdoxorubicin + N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine