Orthopedics This Week | December 5, 2017 | Page 17

ORTHOPEDICS THIS WEEK
VOLUME 13, ISSUE 38 | DECEMBER 5, 2017
patients. The project is titled, “EZH2
inhibitors as endoprosthetic device
coatings that induce osteogenesis and
promote implant osseointegration.”
Uwe Klein, Ph.D., vice president of
Biology at Numerate, is the principal
investigator with co-investigator Andre
J. van Wijnen, Ph.D., professor of Bio-
chemistry and Molecular Biology, and
Orthopedic Surgery at the Mayo Clinic.
Dr. Klein told OTW, “The idea for this
project stems from scientific discus-
sions between us (Numerate) and Dr.
Andre van Wijnen at Mayo Clinic. Dr.
van Wijnen has discovered a key role of
the epigenetic enzyme EZH2 in regu-
lating differentiation of mesenchymal
stem cells to bone forming osteoblasts.”
“He has demonstrated with prototypi-
cal tool compounds that inhibition of
EZH2 can stimulate bone formation.
EZH2 inhibitors that are currently in
clinical development for oncology indi-
cations are not suitable for chronic oral
administration due to their substantial
systemic toxicity and myelosuppres-
sion.”
“Together we conceived the idea of a
locally delivered compound, which
when included in the surface coating of
an endoprosthetic device would stimu-
late bone formation at the device/bone
interface and improve device osseoin-
tegration.”
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cological and physicochemical proper-
ties, while Dr. van Wijnen’s laboratory
brings deep expertise in bone biology,
and has the experience and know-how
to conduct complex cell-based in vitro
and in vivo biological studies to provide
proof of our hypothesis.”
“The research plan for the SBIR [Small
Business Innovation Research] funded
program takes advantage of the syner-
gies that exist between Numerate and
Dr. van Wijnen’s laboratory.” “Dr. van Wijnen’s work will include
coating of surrogate titanium disks
and demonstration of differentiation
of mesenchymal stem cells grown on
the disk surface coated with test com-
pounds. Within the research plan, we
also involve a contract research labora-
tory, which will provide biochemical
data to confirm potency and selectiv-
ity of the compounds identified using
Numerate’s discovery platform.”
“Numerate’s AI [artificial intelligence]
driven drug discovery platform and
expertise in small-molecule drug dis-
covery is ideally suited to identify
compounds with the desired pharma- “If successful, this program will result
in the discovery and development of
novel drug/device combinations, which
would be easy to prepare and use in
the operating room, would provide safe
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