UNFORTUNATELY, ONLY A SMALL FRACTION OF L-DOPA EVER REACHES THE BRAINCategory:
UPDATE ON THE ROAD TO THE CURE
A REAL-TIME SCIENCE REPORT
Unfortunately, only a small fraction of L-dopa ever reaches the brain...
Parkinson’s disease (PD) is a common neurodegenerative disorder characterized by motor and gastrointestinal (GI) deficits. An estimated 12 million individuals are afflicted worldwide with the disease and the US alone has about 1.2 million Parkinson’s patients.
PD is a progressive neurodegenerative condition in which the dopamine-producing cells in a portion of the brain called the substantia nigra begin to sicken and die. Because these cells and their dopamine are critical for controlling movement, their death leads to the familiar tremor, difficulty moving, and the characteristic slow gait. As the disease progresses, cognitive and behavioral problems can take hold, including depression, personality shifts, and sleep disturbances. Despite its prevalence, the pathophysiology of PD is still not well understood.
For the 12 million people in the world now living with PD, and for those who have gone before them, L-dopa has been for the last 50 years the mainstay of treatment to help alleviate those motor symptoms. The drug is a precursor of dopamine, and, unlike dopamine, it has the advantage of crossing the blood-brain barrier. Once inside the brain, an enzyme called DOPA decarboxylase converts L-dopa to dopamine.
Unfortunately, only a small fraction of L-dopa ever reaches the brain, contributing to big differences in the drug’s efficacy from person to person. The reason for this is the role of gut microbiota in neurological disorders. Although it is too early to connect the dots between gut microbiota and PD to establish causation, there have been various previous hints that gut microbes influence the effectiveness of levodopa (L-dopa), which helps to ease the stiffness, rigidity, and slowness of movement associated with Parkinson’s disease.
Now, in findings published in Science, an NIH-funded team has identified a specific, gut-dwelling bacterium that consumes L-dopa and thus attenuates its effectiveness. The scientists have also identified the bacterial genes and enzymes involved in the process: a bacterium called Enterococcus faecalis (E. faecalis), which commonly resides in a healthy gut microbiome. In their tests, this bacterium avidly consumed all the L-dopa, using its own version of a decarboxylase enzyme.
Thus, scientists continue to uncover the many fascinating ways in which the trillions of microbes that inhabit the human body influence our health. Now comes yet another surprising discovery: a medicine-eating bacterium residing in the human gut that may affect how well someone responds to the most prescribed drug for Parkinson’s disease.
Impact of this study on PD Patients: Developing an inhibitor to the E. faecalis will prevent consumption of L-Dopa by this enzyme and significantly improve the efficacy and potency of L-Dopa. Efforts are underway to develop such a safe and effective inhibitor for E. faecalis.
ICB International, Inc. (“ICBII”), is considering developing such an enzyme inhibitor soon. It should be noted that improving the therapeutic efficacy of L-Dopa will not provide the outcome of disease modification, though it might improve the disease symptoms for a longer period.
ICBII was recently notified by the European Patent Office that it intends to grant one patent approval, making the total number of approved patents seven.
WOULD YOU LIKE TO HELP get ICBII’s drugs to market faster? The joy of being a part of this historical event can be had by helping ICBII find the funds to bring these trials to fruition through your investing, and by finding others with the financial ability and humanitarian mindset to accomplish the—until now—impossible. Please contact ICBII directly through their website ICBII.com or by phone at 858-455-9880, or contact Jo Rosen at PRO for a personal introduction to the scientists.
IMAGINE the world without Parkinson’s, MSA, or Alzheimer’s disease.