82

Quote | ReplyCombining a novel glycolysis inhibitor, 3-BrOP, with the mTOR inhibitor, rapamycin, induced more than 90% cell death in human tissue cultures of acute lymphocytic leukemia http://www.mdanderson.org/newsroom/news-releases/2008/new-dr  and http://www.ncbi.nlm.nih.gov/pubmed/21316758

Novel Cancer Drug Reduces Neuroblastoma Growth by 75% http://www.mdanderson.org/newsroom/news-releases/2009/novel-  and http://www.ncbi.nlm.nih.gov/pubmed/20890785

Effective Elimination of Cancer Stem Cells By a Novel Drug Combination Strategy http://www.cancercuremedicine.com/uploads/4/3/7/1/43718009/c  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3538380/

Results: 5 http://www.ncbi.nlm.nih.gov/pubmed/?term=3-BrOP

According to MD Anderson *We already knew that 3-BrOP was effective in preclinical research of glioblastoma, colon cancer and lymphoma* & *A Phase I clinical trial is planned to open this year for adult patients* (this was from 2009). Also it seems its a glycolysis inhibitor. If it is then what about mitochondrial ATP?
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterJcancom

* Add As Friend
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 10, 2015 05:38 PM
Quote | Reply"The inventors show that Glycolycin and its derivatives/analogs have superior pharmaceutical properties compared to other glycolytic inhibitors, and is able to effectively block glycolysis and cause a severe depletion of the cellular ATP pool and massive cell death, especially in cancer cells with increased dependency on glycolysis in a hypoxic environment or when mitochondrial respiration is defective."

http://www.freepatentsonline.com/y2006/0058383.html

It is interesting and disappointing that the optimal form of 3-BP does not appear to have yet established. The patent still needs to make broad claims for the best chemical composition. They still do not know!

"An ester of 3-halo-2-oxopropionate may also be 3-bromo-2-oxopropionic acid ethyl ester (which may be referred to herein as E-Glycolycin, also referred to as ethyl 3-bromo-2-oxopropionate or ethyl 3-bromopyruvate); 3-fluoro-2-oxopropionic acid ethyl ester; 3-chloro-2-oxopropionic acid ethyl ester; or 3-iodo-2-oxopropionic acid ethyl ester. An ester of 3-halo-2-oxopropionate may also be 3-bromo-2-oxopropionic acid methyl ester (which may be referred to herein as M-Glycolycin, also referred to as methyl 3-bromo-2-oxopropionate or methyl 3-bromopyruvate); ...."
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterJcancom

* Add As Friend
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 10, 2015 05:42 PM
Quote | ReplyCould someone share the SMILES for some of these chemicals?
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterjames-peters

* Add As Friend
* Private Reply
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by james-peters on Sun May 10, 2015 05:52 PM

Quote | Reply

On May 10, 2015 9:38 PM Jcancom wrote:

"The inventors show that Glycolycin and its derivatives/analogs have superior pharmaceutical properties compared to other glycolytic inhibitors, and is able to effectively block glycolysis and cause a severe depletion of the cellular ATP pool and massive cell death, especially in cancer cells with increased dependency on glycolysis in a hypoxic environment or when mitochondrial respiration is defective."

http://www.freepatentsonline.com/y2006/0058383.html "" target="\_blank" rel="nofollow">http://www.freepatentsonline.com/y2006/0058383.html " target="\_blank" rel="nofollow">http://www.freepatentsonline.com/y2006/0058383.html

It is interesting and disappointing that the optimal form of 3-BP does not appear to have yet established. The patent still needs to make broad claims for the best chemical composition. They still do not know!

"An ester of 3-halo-2-oxopropionate may also be 3-bromo-2-oxopropionic acid ethyl ester (which may be referred to herein as E-Glycolycin, also referred to as ethyl 3-bromo-2-oxopropionate or ethyl 3-bromopyruvate); 3-fluoro-2-oxopropionic acid ethyl ester; 3-chloro-2-oxopropionic acid ethyl ester; or 3-iodo-2-oxopropionic acid ethyl ester. An ester of 3-halo-2-oxopropionate may also be 3-bromo-2-oxopropionic acid methyl ester (which may be referred to herein as M-Glycolycin, also referred to as methyl 3-bromo-2-oxopropionate or methyl 3-bromopyruvate); ...."
Have they shown anything, or are they making claims?. Just 5 results from Pubmed, and no Phase I. I haven't read the patent in full, however cancer gets its energy two ways. They use glycolysis and mitochondrial which both produce ATP and cancer can use glutamine.
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterjames-peters

* Add As Friend
* Private Reply
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by james-peters on Sun May 10, 2015 05:56 PM
Quote | ReplyHexokinase II: Cancer’s double-edged sword acting as both facilitator and gatekeeper of malignancy when bound to mitochondria http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3385868/  Hexokinase-2 bound to mitochondria: Cancer's stygian link to the “Warburg effect” and a pivotal target for effective therapy http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2714668/  Cancer as a metabolic disease: implications for novel therapeutics http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3941741/  The Pivotal Roles of Mitochondria in Cancer: Warburg and Beyond and Encouraging Prospects for Effective Therapies http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2890051/  Dr. Peter Pedersen Explaining the Promise of 3-BP and the Warburg effect http://videocast.nih.gov/summary.asp?live=7542
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterJcancom

* Add As Friend
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 10, 2015 06:05 PM
Quote | ReplyYeah, it is very disappointing. 10 years after going through the patent process and they are still preparing for a phase 1 trial (page 4 below). How could ten years possibly be justified? 3-BrOP likely is a step-up from 3-BP- safer and more effective. Why the delay?

http://www.mdanderson.org/publications/children-s-cancer-hos
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterJcancom

* Add As Friend
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 10, 2015 06:09 PM
Quote | ReplyHow could the MD Anderson patent possibly be valid? Hopkins must have tried to sew up every possible chemical combination of 3-BP.

If it went to trial I do not know if a jury would buy the argument that 3-BrOP was sufficiently different from 3-BP to allow the patent.  The claimed method of action of 3-BrOP appears to be identical to that of 3-BP.
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterGenelle

* Add As Friend
* Private Reply
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Genelle on Sun May 10, 2015 06:11 PM
Quote | ReplyThey can all fight over it while we are dying.
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterJcancom

* Add As Friend
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 10, 2015 06:38 PM
Quote | ReplyThe real problem might be that all of these trival variances that result in new patent claims deter companies from starting clinical trials at all. 3-BP likely is not the optimal formulation, 3-BrOP is possibly better, though not optimal. It would be hard to justify investing hundreds of millions of dollars only to be outdone by someone who made a minor modification resulting in a better product. Perhaps granting broader patent rights to all related or similar compounds with a specific therapeutic intent would give companies the protection they need to bring products like 3-BP to market.

We are now 15 years out from the first reports of 3-BP anti-cancer properties! If patent laws have really played a part in such an embarrassment, patent laws should be changed.
Quote | ReplyMore Sharing ServicesShare Share on email Share on facebook Share on twitterGenelle

* Add As Friend
* Private Reply
* Report Abuse
* Stop Tracking
* Share on emailEmail Friend

### RE: Anyone used 3bp (3-bromopyruvate)?

by Genelle on Sun May 10, 2015 07:00 PM
Quote | ReplyYou would think that Germany or Switzerland would come up with something because they ave no FDA but I suppose the patent laws would apply there. Maybe China would do it and do medical tourism. It is easy for doctors here to get DCA but not 3BP.
Quote | Reply

Page 83