Next, the researchers looked at what would happen to PBRM when they injected it under the skin of live mice and how the body of the animals processes the potential drug. Not only did PBRM-O not have any estrogenic activity, it also inhibited 17β-HSD1 almost as well as PBRM. They found that with time PBRM turned into the oxidized form of the molecule called PBRM-O and no other metabolites or waste products were formed. In order to study the pharmaceutical behavior of PBRM, and further characterize this potential new drug, the researchers conducted a number of studies both in cells grown in the laboratory and in mouse models.įirst, they used human liver cells to evaluate the stability of PBRM.

Therefore blocking the activity of 17β-HSD1 could be a promising approach to treat hormone-dependent cancers and endometriosis. It is known that too much estradiol can lead to a number of diseases including breast and endometrial cancer, as well as endometriosis. This enzyme is overproduced in breast cancer and is responsible for the production of estradiol, the most potent female hormone. The same team has recently reported the development of PBRM as an inhibitor, or blocker, of an enzyme called 17β-HSD1. In the study that was published in The Journal of Steroid Biochemistry and Molecular Biology, researchers characterized the pharmaceutical behavior of PBRM using a mouse model. It is important to note that this is a very early stage pre-clinical study conducted in an animal model and the results obtained may not be the same in human clinical trials.Ī steroid derivative called PBRM could be a new emerging drug to treat endometriosis according to a study by Canadian scientists.PBRM was well-tolerated by the mice and showed no signs of toxicity.PBRM was mainly extracted from the body via feces.A high-quality absolute bioavailability value was obtained when PBRM was given to the mice orally suggesting that could potentially be developed into a drug to be taken by mouth daily.After under-the-skin injection, PBRM was observed in the liver, kidney, and gastrointestinal tract of the mice, which gradually decreased and disappeared altogether after 72 hours and did not accumulate in any organs.When injected under the skin of the mice, PBRM showed favorable values regarding half-life, absolute bioavailability, distribution volume, and clearance rate.The sole metabolite of PBRM was PBRM-O, which did not have any estrogenic activity, and which inhibited the 17β-HSD1 enzyme as well as PBRM.Being a blocker of an enzyme that is known to be involved in the development of breast cancer and endometriosis, PBRM could potentially be a new emerging drug to treat these life-threatening diseases,.Researchers analyzed in detail the pharmaceutical behavior of the steroid derivative PBRM using a mouse model.

Canadian researchers characterized the pharmacological behavior of the steroid derivative PBRM.

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