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Rensselaer
Team Develops Novel Opioid Receptor Compounds Licensed to
Alkermes, Inc.
Discovery
May Lead to Further Development of Compounds to Treat Central
Nervous System Disorders and Addiction
Troy, N.Y. — Mark
Wentland, professor of chemistry and chemical biology at
Rensselaer Polytechnic Institute, has led a team in the discovery
of a family of novel opioid receptor compounds that may be used
in treating central nervous system disorders and addiction. The
team included more than 15 undergraduate, graduate, and
postdoctoral students in Rensselaer’s department of
chemistry and chemical biology. Jean Bidlack, professor of
pharmacology and physiology at the University of Rochester, along
with members of her pharmacology group, also contributed to the
research.
In October, Rensselaer
announced that they had entered into a license agreement granting
Alkermes, Inc. — a biotechnology company based in
Massachusetts — with exclusive rights to the compounds
discovered by Wentland and his team.
“This latest discovery is
the result of an interdisciplinary collaboration between chemists
and biologists,” said Wentland. “In the process, we
are working together to identify novel therapies to treat human
diseases and find possible solutions that work. Most importantly,
this discovery allows us to see the significant role that
biotechnology plays in improving health, creating new
materials for myriads of applications, and addressing some of the
world’s most challenging scientific problems. I am pleased
to see this exciting technology move from the laboratory toward
treating patients.”
According to Alkermes, the
compounds represent an opportunity for the company to develop
important therapeutics for a broad range of diseases and medical
conditions, including addiction, pain and other central nervous
system (CNS) disorders. Alkermes will screen the library of
compounds and plans to pursue preclinical work of an undisclosed,
lead oral compound that has already been identified. The company
will be responsible for the continued research and development of
any resulting product candidates.;
“This agreement
underscores Alkermes’ commitment to building our franchise
in the area of CNS, including addiction,” stated Richard
Pops, CEO of Alkermes. “We are excited to begin development
of this promising family of compounds, which provides us with the
opportunity to leverage our success and experience with VIVITROL
and build our proprietary product portfolio.”
“We are delighted to
partner with Alkermes,” said Ron Kudla, executive director
of the Office of Intellectual Property, Technology Transfer and
New Ventures at Rensselaer. “This is a wonderful example of
progress under the Rensselaer Plan in the areas of biotechnology
and technology transfer that demonstrates Rensselaer’s
unique strength in its ability to translate scientific
discoveries into practical application.”
The initial research leading to
Wentland’s latest discovery was funded in 1999 through an
$826,000 grant from the National Institutes of Health/National
Institute on Drug Abuse (NIH-NIDA) in an effort to discover novel
drugs to treat cocaine abuse. In 2002, Wentland’s NIH grant
was renewed for an additional $1.6 million, and he was awarded
new funding from Albany Molecular Research, Inc. for a
postdoctoral associate position.
Cyclazocine
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In his NIH-funded research
program, Wentland has deliberately chosen an area with an unmet
therapeutic need, cocaine addiction. One of Wentland’s
starting points is an opiate drug discovered in the 1960’s
called cyclazocine, which may produce the desired pharmacological
effect. Cocaine itself stimulates reward pathways in the brain by
increasing the release of a neurotransmitter called dopamine.
Cyclazocine may dampen dopamine release by acting on two
different types of cell surface receptors, according to Wentland.
However, cyclazocine’s short duration of action is a
detriment to its therapeutic usefulness. The major thrust of his
group’s research was to correct this deficiency in
cyclazocine and other lead compounds by designing and evaluating
new derivatives.
Wentland earned his bachelor’s
degree in chemistry from Central Connecticut State University,
and his Ph.D. in synthetic organic chemistry from Rice
University. For more than 24 years, he conducted drug discovery
research in the medicinal chemistry department at Sterling
Winthrop, serving as a Sterling Winthrop Fellow and Oncology
Discovery Co-Chair, respectively. During this time, Wentland also
served as an adjunct professor at Rensselaer from 1971-1994 and
taught over 30 graduate-level organic and medicinal chemistry
courses. Currently a full-time faculty member, Wentland teaches
courses on drug discovery.
Wentland straddles the boundary
between basic and applied research. “Medicinal chemistry,
foremost among traditional approaches to drug discovery and
development, retains its value in a high-tech world,” he
said. A medicinal chemist is “a person whose primary aim is
to get a drug into the clinic,” he added.
In the future, Wentland will
continue to work with Alkermes to develop the existing family of
compounds and possible application to other diseases.
Source
/ Credit Rensselaer Polytechnic Institute
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