LetterPhase II study of oral miltefosine in patients with squamous cell head and neck cancer
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Evaluation of release and pharmacokinetics of hexadecylphosphocholine (miltefosine) in phosphatidyldiglycerol-based thermosensitive liposomes
2021, Biochimica et Biophysica Acta - BiomembranesCitation Excerpt :Hexadecylphosphocholine (HePC) represents a lead compound from the group of alkyphosphocholines [34] which is approved for a topical treatment of metastasized breast cancer [35,36]. Preclinically, HePC showed a promising anti-cancer activity on many tumor cell lines in-vitro as well as in animal tumor models in vivo [37,38] but failed later to progress in clinical studies on patients due to a dose-limiting gastrointestinal toxicity following the oral administration [39–41]. Parenteral application of the drug is not possible since HePC has hemolytic effects on blood cells [42].
Improving the miltefosine efficacy against leishmaniasis by using different nanoassemblies made from surfactants or amphiphilic antimony (V) complex
2021, Applications of Nanobiotechnology for Neglected Tropical DiseasesExploring the new horizons of drug repurposing: A vital tool for turning hard work into smart work
2019, European Journal of Medicinal ChemistryRepurposed Molecules: A New Hope in Tackling Neglected Infectious Diseases
2019, In Silico Drug Design: Repurposing Techniques and MethodologiesIn vitro effects of the antitumor drug miltefosine on human erythrocytes and molecular models of its membrane
2019, Biochimica et Biophysica Acta - BiomembranesCitation Excerpt :Moreover, it is effective against various tumor cells, including soft tissue sarcomas, metastatic colorectal cancer, head and neck squamous cell carcinoma, hematological malignancies, and brain tumors [7,8]; besides, it has been proven to be effective in the treatment of infections with fungi, bacteria and parasites [7,9,10]. However, miltefosine exhibits toxicity in the epithelial cells of the gastrointestinal tract when the administration is oral, and it was found to be highly hemolytic when it is parenterally administered [11,12]. These severe side effects limited its maximum-tolerated daily dose, preventing antiproliferative effects in vivo and its use as a systemic agent [13].
Inhibition of Akt and other AGC kinases: A target for clinical cancer therapy?
2018, Seminars in Cancer BiologyCitation Excerpt :It can be incorporated into cell membranes and inhibits the membrane-linked protein kinase C (PKC) as well as Akt signaling [8,9]. Miltefosine was evaluated in patients with soft tissue sarcomas [10], colorectal cancer [11] and squamous cell carcinoma of the head and neck [12]. Unfortunately, the dose required for an anti-tumor effect was above the maximum tolerated dose (MTD) and thus this drug was not developed as a systemic anti-cancer drug.