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Diardylalkylamine and its use as an antiproliferative and proapoptotic agent

Anticancer agentsBrest cancerCyrcadian rythmsDiardylalkylamineREV-ERBa


The invention concerns new diarylalkylamine compounds and their use as antiproliferative and proapoptotic agents for cancer therapy. Specifically, these molecules act as inhibitors of REV-ERBa, intracellular transcription factor and key regulator of circadian rhythms in healthy cells, overexpressed and having a role of survival factor in breast cancer.

Technical features

Over the years, numerous REV-ERBa antagonists have been developed, having different chemical structures and therapeutic results. However, most include poor pharmacokinetic properties that limit their pharmacological uses. The main innovation of the new diarylalkylamine compounds lies in their versatility: it is possible to create compounds with different characteristics depending on the therapeutic need; For example, an isotope of the compound that includes deuterium will offer greater metabolic stability, very useful for a reduced dosage of the drug. The pharmaceutical compositions of this invention can be administered for a variety of routes, including oral, rectal, transdermal, subcutaneous, intravenous, intramuscular, intranasal, and pulmonary pathways. Compositions for oral administration may take the form of loose liquid solutions or suspensions, or loose powders. More commonly, however, compositions are presented in unit dosage forms to facilitate accurate dosing.

Possible Applications

  • Treatment of serious dysfunctions and pathologies of circadian rhythms
  • Treatment of cancer, specifically breast cancer


  • Ability to create different isotopes with different chemical and pharmaceutical characteristics depending on medical needs
  • High variety of administration routes