6 ms·
Most pertinent quote here is that the only reason it was not pursued was because it is not orally bioavailable: "But because the drug comes as a liquid that ne
by matznerd 8y ago
Most pertinent quote here is that the only reason it was not pursued was because it is not orally bioavailable:
"But because the drug comes as a liquid that needs to be injected every day, it was unlikely to be popular with patients who already had alternatives, such as pills, that were easier to take. Pharmaceutical companies did not pursue it."
There are many other molecules out there that have advanced properties but have difficult delivery methods, including some nootropics (semax, selank, cerebrolysin, etc).
There is a group though that has no problem injecting things into themselves: bodybuilders and athletes. Fortunately for us, they have brought some other abandoned molecules back from the dead, mostly ones that heal injuries.
For example, there is a molecule found in human gastric juices, known as Body Protecting Compound 157 (BPC-157). Part of the intestinal lining has to regenerate itself nearly weekly. This compound, isolated from there, and then synthesized, is used prolifically by athletes/bodybuilders with tendon/ligament injuries, but can also be used for repairing stomach issues. etc. It is widely available on the internet. Here is the science for you:
"As has been demonstrated for many organoprotective agents using different models of various tissue lesions, despite the poorly understood final mechanism, practically all organ systems appear to benefit from BPC activity. These effects have been achieved in many species using very low dosages (mostly microgram and ng/kg range) after ip, ig, and intramucosal (local) application. The effect was apparent already after one application. Long lasting activity was also demonstrated. BPC was highly effective when applied simultaneously with noxious agents or in already pathological, as well as chronical, conditions. Therefore, it seems that BPC treatment does not share any of the so far known limitations for 'conventional organoprotectors'. No influence on different basal parameters and no toxicity were observed. These findings provide a breakthrough in stress theory. BPC, as a possible endogenous free radical scavenger and organoprotection mediator, could be a useful prototype of a new class of drugs, organoprotective agents."
https://www.ncbi.nlm.nih.gov/pubmed/8298609 https://www.ncbi.nlm.nih.gov/pubmed/8298609
"Pentadecapeptide BPC 157, composed of 15 amino acids, is a partial sequence of body protection compound (BPC) that is discovered in and isolated from human gastric juice. Experimentally it has been demonstrated to accelerate the healing of many different wounds, including transected rat Achilles tendon. This study was designed to investigate the potential mechanism of BPC 157 to enhance healing of injured tendon."
https://www.physiology.org/doi/full/10.1152/japplphysiol.00945.2010 https://www.physiology.org/doi/full/10.1152/japplphysiol.009...
"BPC 157 may serve as a novel mediator of Robert’s cytoprotection, involved in maintaining of GI mucosa integrity, with no toxic effect. BPC 157 was successful in the therapy of GI tract, periodontitis, liver and pancreas lesions, and in the healing of various tissues and wounds."
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5333585/ https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5333585/
" A novel stomach pentadecapeptide, BPC-157, improves wound and fracture healing in rats in addition to having an angiogenic effect. Therefore, in the present study, using a segmental osteoperiosteal bone defect (0.8 cm, in the middle of the left radius) that remained incompletely healed in all control rabbits for 6 weeks (assessed in 2 week intervals), pentadecapeptide BPC-157 was further studied (either percutaneously given locally [10 microg/kg body weight] into the bone defect, or applied intramuscularly [intermittently, at postoperative days 7, 9, 14, and 16 at 10 microg/kg body weight] or continuously [once per day, postoperative days 7-21 at 10 microg or 10 ng/kg body weight])...Pentadecapeptide BPC-157 significantly improved the healing of segmental bone defects."
https://www.ncbi.nlm.nih.gov/pubmed/10071911 https://www.ncbi.nlm.nih.gov/pubmed/10071911
"BPC 157 improved muscle healing, macroscopically (less hematoma and edema, no post-injury leg contracture), microscopically, functionally, and also based on enzyme activity (creatine kinase, lactate dehydrogenase, aspartate aminotransferase, alanine aminotransferase)...BPC 157, at all investigated intervals, given locally or intraperitoneally, accelerated post-injury muscle healing and also helped to restore the full function."
https://www.ncbi.nlm.nih.gov/pubmed/18668315 https://www.ncbi.nlm.nih.gov/pubmed/18668315
- amelius 8y agoI wonder, though, what the downsides are of this drug. If the human body can produce it and if there are only upsides, then why didn't evolution make the substance more abundantly available?
- entee 8y agoThings that cause growth are generally a very bad thing in biology, because they cause cancer. Look at a list of proteins key to cancer and you'll find tons of growth promoters, some of which have the word "growth" right there in the name (the G in EGFR, FGFR, VEGFR, IGFR). Growth must be tightly regulated to not end up as cancer, so that's why it's not abundantly available.
- gotocake 8y agoThe article makes the point that despite human trials originally, and later one-cell zebrafish embryo tests, no sign of carcinogenesis was detected. They further explain that given its limited range within the body, it only impacting damaged tissue and the short period of time it would be used, it’s unlikely to be carcinogenic.
- entee 8y agoOh sure, this agrees with the "tightly regulated" constraint. Short time, localized application/expression qualify. I'm not sure that long term exposure would be good, and in reference to BPC-157 let's not forget that intestinal cancers do occur (though I'm not at all sure if there's ever been a link between BPC-157 and intestinal cancer). It's great that the compound looks safe given the limited amount of information we have, but it sounds like there's not a whole lot of trials out there with the power to test the possibility that this could be cancerous long term. Happy to be proven wrong though!
- gotocake 8y agoRemember the initial human trials were using it systemically to control blood sugar, and specifically looked for carcinogenesis. Obviously there’s room for something to have been overlooked, but in the narrow case of this particular molecule I’d be hopeful. As for BPC-157 we’re very much on the same page, and I’d be very concerned about cancer.