Macropinocytosis Inhibitors
Recently, scientists at Augusta University in USA, have performed an extensive study, testing 640 FDA‐approved compounds in order to identify macropinocytosis inhibitors (Ref.).
Of all the drugs investigated, Imipramine stood out the most. It is one of the most effective macropinocytosis inhibitor. In addition, a major advantage is that it has a very well known safety profile, given that it has been introduced into medicine in the 1960s as a tricyclic antidepressant (TCA). The authors argued that other advantages of imipramine compared with currently used macropinocytosis inhibitors are its excellent bioavailability following p.o. administration (95%) and its relatively long biological half‐life (~20 h) (Ref.).
Note: as soon as possible I will also serch for supplements that may help on this line.
Imipramine and Cancer
Beyond macropinocytosis inhibition activity, there is a large amount of scientific data on the anti-cancer activity (and even antiparasitic action) of Imipramine, in various cancer types, via various mechanisms:
Source and Application
Source: FDA approved drug – available under prescription and easily accessible for cancer patients as an anti depression medication.
According to the reports above, the daily dose used by the patients experiencing positive results was in the range of 75 mg to 150 mg.
Ideas to improve the effectiveness of Imipramine
Combo with Nicolsamide https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8033521/
Combo with Autophagy inhibitors such as HydroxyChloroquine or the proton pump inhibitor Omepazole that strongly affects lysosomes as well.
Disc
Recently, scientists at Augusta University in USA, have performed an extensive study, testing 640 FDA‐approved compounds in order to identify macropinocytosis inhibitors (Ref.).
Of all the drugs investigated, Imipramine stood out the most. It is one of the most effective macropinocytosis inhibitor. In addition, a major advantage is that it has a very well known safety profile, given that it has been introduced into medicine in the 1960s as a tricyclic antidepressant (TCA). The authors argued that other advantages of imipramine compared with currently used macropinocytosis inhibitors are its excellent bioavailability following p.o. administration (95%) and its relatively long biological half‐life (~20 h) (Ref.).
Note: as soon as possible I will also serch for supplements that may help on this line.
Imipramine and Cancer
Beyond macropinocytosis inhibition activity, there is a large amount of scientific data on the anti-cancer activity (and even antiparasitic action) of Imipramine, in various cancer types, via various mechanisms:
- is a fascin1 blocker with anti-invasive and antimetastatic activities in colorectal cancer cells (Ref.)
- it is more effective than radiotherapy in prostate cancer cells (Ref.)
- is effective against TNBC and ER+ breast cancer cells (Ref.) – note: a clinical trials has been started to investigate the effectiveness of Imipramine in TNBCS patients (Ref.)
- Imipramine inhibits migration and invasion in metastatic castration-resistant prostate cancer (Ref.)
- it halts head and neck cancer invasion (Ref.)
- block the invasion of glioblastoma multiforme (Ref.1, Ref.2)
- found to inhibit the growth of Small cell lung cancer (SCLC) and other neuroendocrine tumors, including pancreatic neuroendocrine tumors and Merkel cell carcinoma (Ref.)
- Imipramine Protects against Bone Loss by Inhibition of Osteoblast-Derived Microvesicles (Ref.)
- It has antimalarial properties (Ref.)
- antiparasitic – acts against both Antimony s
Source and Application
Source: FDA approved drug – available under prescription and easily accessible for cancer patients as an anti depression medication.
According to the reports above, the daily dose used by the patients experiencing positive results was in the range of 75 mg to 150 mg.
Ideas to improve the effectiveness of Imipramine
Combo with Nicolsamide https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8033521/
Combo with Autophagy inhibitors such as HydroxyChloroquine or the proton pump inhibitor Omepazole that strongly affects lysosomes as well.
Disc
