I have an enlarged prostate and came across an article at the NIH that used Rapatar. Is Rapatar available at the same places that sell Rapamycin?
I’ve never heard of it being commercially available… but I’ve not looked into it much:
We’ve talked about it a bit here: Rapamycin and Benign Prostate Hyperplasia (BPH) - #4 by RapAdmin
and here: Rapamycin and AD - #4 by scta123
thank you for replying. I did a search on this site and saw the first article which is the same one I have before me. If you dig deeper it says that Rapatar at the dose of 25 mg/kg corresponds to 0.5 mg/kg of rapamycin. But aren’t their formulation different? Can you just replace the one with the other?
It seems like Rapatar was a new formulation of rapamycin produced by a company called Everon biosciences: Everon Biosciences | LinkedIn
It seems it was tested in animals for a number of years, but no commercial product was ever developed, and tested in humans (no phase 1 or phase 2 studies that I can find easily). It sounds like the compound did not go much past some early animal testing…
I’ve not seen any significant description of the formulation. Perhaps looking through old patent applications may provide more information…
I found this: EP2790700B1 - Rapamycin composition - Google Patents
It seems that the company is now out of business (their website is defunct): http://www.everonbio.com
Looking at the wayback machine, it seems the company was most active from around 2017 to 2019:
from the old website:
Leading the quest for drugs against aging
Everon Biosciences, Inc. was founded in 2010 with the goal of developing anti-aging medicines. Company’s scientific program and vision are based on principles of eradicating the cellular foundations of aging formulated by Prof. Andrei Gudkov, Senior Vice President of Research Programming and Development of Roswell Park Cancer Institute, the world’s oldest cancer research center. From the very beginning, the institute has been Everon’s supportive shareholder and a reliable partner, providing access to its rich technical infrastructure and its scientists and physicians. This strategic collaboration resulted in the development of pharmacological and immunological approaches to treatment of age-related frailty. Everon holds a unique position among recently launched anti-aging companies in its approach to the treatment of aging from all major R&D aspects: mechanistic understanding of aging process, access to targets, availability of proprietary drug candidates, strong preclinical efficacy indications, the development of diagnostic tools and clinical strategy.
https://www.crunchbase.com/organization/everon-biosciences
CONFLICTS OF INTEREST
M.P.A. and A.V.G. served as consultants for Everon Biosciences, Inc.; O.V.C. and A.V.G. are co-founders and shareholders of Everon Biosciences, Inc.
From this paper: Superior cancer preventive efficacy of low versus high dose of mTOR inhibitor in a mouse model of prostate cancer - PMC
and from the patent application:
Therefore, there is a need for pharmaceutical formulations of rapamycin which can take advantage of the ABC mediated efflux inhibition exhibited by hydrophobic poloxamers (which copolymers are liquids at room temperature), which formulations do not aggregate under physiological conditions, and which are suitable for the production of tablets and other dry forms of application.
- [0009]
U.S. Patent Application Publication No. 2008/275076 discloses pharmaceutical compositions in particulate form or in solid dosage forms comprising sirolimus (rapamycin) and/or derivatives and/or analogues thereof. Compositions of the invention exhibit an acceptable bioavailability of sirolimus and/or a derivative and/or an analogue thereof. The pharmaceutical compositions of the invention are designed to release sirolimus in a controlled manner so that the plasma levels stays within the narrow therapeutic window that exist for this class of substances. An extended release profile, where the peak concentration has been reduced without losing significant bioavailability, together with less variable absorption, is expected to improve the safety/efficacy ratio of the drug. Furthermore, compositions according to the invention provide for a significant reduced food effect and a delayed release of sirolimus is expected to reduce the number of gastro-intestinal related side effects.
- [0010]
Accordingly, it is an object of this invention to provide a rapamycin composition comprising such hydrophobic poloxamers, which composition is in the form of a free flowing, compressible powder.
If you really wanted to learn more - you can probably contact some of the researchers involved…
I found this on one of the links you sent. Do you think rapamycin works the same way as rapatar. I’ve read on here people discussing cancer and rapamycin.
" While under normal homeostatic conditions autophagy is an essential and beneficial catabolic mechanism, its overactivation in tumors promotes tumor cell survival (reviewed in [[45] We propose that these dose-dependent side effects underlie the differences in chemopreventive efficacy observed for different Rapatar doses.
High dose Rapatar treatment promotes development of reactive stroma through feedback activation of Akt
Emerging studies indicate that the mTOR signaling pathway is regulated by complex processes, including several feedback loops which may be activated by mTORC1 inhibition."
(Superior cancer preventive efficacy of low versus high dose of mTOR inhibitor in a mouse model of prostate cancer - PMC)]).