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UMB Pharmacy Researchers Develop Promising Chronic Pain Drug |
 A team of researchers led by Andrew
Coop, PhD, professor
and chair of the Department
of Pharmaceutical Sciences (PSC) at the University of Maryland School
of Pharmacy (UMSOP), has developed a new opioid drug that shows
great potential to advance treatment and improve quality of life for
individuals living with chronic pain. Spotlighted in a recent issue of ACS Chemical Neuroscience, the
compound, known as UMB 425, is as strong as morphine, but displays
diminished tolerance over time with no obvious toxic effects.
"UMB 425 is a breakthrough in the development of therapeutics to treat
chronic pain," says Coop (on the left in the photo). "Unlike other drugs developed to act on only
one biological target, UMB 425 acts on two different opioid receptors
in the body. When activated at the same time, these receptors work
together to provide pain relief and slow the body's development of
tolerance to the drug. This diminished tolerance allows a lower dose of
the opioid to be administered for a longer time period, while still
achieving the same level of pain relief."
For individuals living with chronic pain, either as a result of injury
or disease such as arthritis, opioids are the standard treatment. But
as the dosage increases to offset the body's tolerance to their
effects, opioids cause a number of adverse effects, including
constipation, nausea, drowsiness, and dizziness. The unique
dual-profile of UMB 425 - made possible through Coop's collaborations
with Alexander MacKerell, PhD, professor in PSC and director
of the School's Computer-
Aided Drug Design Center, and Maureen
Kane, PhD, assistant professor in PSC and co-director of the
School's Mass
Spectrometry Facility - provides both pain relief as well as
diminished tolerance in one drug.
"Historically, medicinal chemists have developed drugs aimed at only
one biological target," says Coop. "However, two drugs administered
together have the potential to metabolize differently in different
individuals, as well as affect patients' adherence to both drugs. A
single compound that is able to provide both pain relief and diminished
tolerance has the advantage of a defined ratio that we can optimize to
ensure patients receive the maximum pain relief, while experiencing
minimum adverse effects."
Coop and his team conducted several in vitro and in vivo studies to
determine the drug's effectiveness in alleviating pain and diminishing
tolerance over time. If future research and clinical trials are
successful, UMB 425 could have a significant impact on the treatment
and quality of life for individuals living with chronic pain.
"The clinical implication of this research has the potential to be
tremendous," says Mary Lynn
McPherson, PharmD, BCPS, CPE, professor and vice chair for
academic affairs in the Department
of Pharmacy Practice and Science, and an international authority in
the fields of pain management and palliative care. "If clinicians can
prescribe lower doses of opioids, they will not have to raise a
patient's dose because of tolerance to the analgesic effects. Using
lower doses will result in less severe adverse effects for the patient,
both short-term effects such as nausea and constipation, as well as
long-term adverse effects on the endocrine and immunologic systems.
This would be a highly significant advance in pain management."
Coop and his team will continue to test UMB 425 to determine an optimal
ratio at which it acts on the targeted opioid receptors to maximize
pain relief, while minimizing tolerance. The team's ultimate goal is to
develop two compounds derived from UMB 425 that will lead to Phase I
clinical trials.
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| Posting Date: 08/28/2013 |
| Contact Name: Malissa Carroll |
| Contact Phone: 410-706-1690 |
| Contact Email: mcarroll@rx.umaryland.edu |
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