Breastin is a product derived from a cold extract of Nerium oleander, characterized by specific quantities of glycosides, flavonoids, and polysaccharides. Extensive testing was conducted, including clonogenic assays on more than 70 established human patient-derived xenografts (PDX) and hematopoietic tumors from Oncotest panels, as well as on the bone marrow of three healthy donors.
The analysis of IC50 and IC70 values demonstrated the tumor-selective properties of Breastin. Comparison with a database of 180 known substances revealed correlations with 150 anticancer agents, including well-established clinical treatments such as Cisplatin, 5-FU, and Cyclophosphamide. Additionally, Breastin showed a correlation with mitosis-inhibiting drugs.
Further investigations using tubulin-GFP-transfected U2OS cells and confocal microscopy indicated that Breastin exhibited microtubule-disturbing effects like the tubulin-depolymerizing drug Paclitaxel. This finding was substantiated through in vitro tubulin polymerization assays and molecular docking studies in silico.
Recently, in a comparative analysis with 153 anticancer agents with known MoA on 74 tumor cell lines of an Oncotest panel, it has been shown a frequent correlation of Breastin to mitosis-inhibiting and DNA damaging drugs. Therefore, the antimicrotubular activity of Breastin was further explored using tubulin-GFP-transfected U2OS cells. Confocal microscopy verified that Breastin acts as a tubulin-depolymerizing agent, displaying behavior like paclitaxel, thus confirming the machine learning prediction made here (2023, 2024).
Finally, recent studies (2015) reported for the first time that oleandrin which is one of Breastin main components, acts as MELK inhibitor in A549 cells. It was suggested that oleandrin could be valuable in non-small lung cancer therapy in the future (2025).
In vivo studies demonstrated the effectiveness of Breastin against mammary and lung cancer, as well as melanomas and mitomycin-C.
Safety assessments included acute and repeated oral subacute tests in accordance with OECD guidelines, which did not reveal any adverse effects of Breastin at therapeutic doses. A micronucleus test, also following OECD guidelines, demonstrated that Breastin did not induce micronuclei in the bone marrow cells of mice compared to control mice.
Encouraging results emerged from uncontrolled Phase-1 and Phase-2 clinical studies conducted on a cohort of cancer patients. Comprehensive data generated throughout the research is available upon request, subject to an agreement.