- A novel
drug has been developed for treating bone fractures
drug is a conjugate of an existing anti-cancer drug with the amino acid
aspartic acid to synthesize
the drug is injected intravenously, it localizes at the fracture site. It
accelerates the healing process, reduces the recovery time and rapidly
increases bone density
novel strategy could be a major breakthrough and a paradigm shift in the
way bone fractures are treated
Fractures are very common. Approximately 1 in 2 women and
1 in 5 men over 50 years of age suffer from bone fractures worldwide. It has
been estimated that globally, 9 million new fracture cases are reported
annually, of which 6 million are from the USA alone. This translates into
billions of dollars towards treatment costs, as well as loss of productivity at
Conventionally, plaster casts have been used for fractures
. Nowadays, surgery is also quite common,
which involves the insertion of metallic pins and plates until the fracture heals.
The only medicine currently available for accelerating the healing process has
to be directly applied to the fracture during surgery. However, this is
inconvenient and is not applicable to all types of fractures.
New Drug that could be
a Game Changer
A new study has revealed the potential of a
novel bone anabolic agent
for accelerating the
healing of fractures. The drug, when injected into the blood can reduce the
healing time of femur fractures
by 60%, without causing any harm to adjacent tissues. The study, entitled, "Bone fracture-targeted
dasatinib conjugate potently enhances fracture repair in vivo"
, has been presented at the 2018 American Association of Pharmaceutical Scientists (AAPS) PharmSci 360
Meeting, held on 4-7 November, 2018 at the Walter E. Washington
Convention Center, Washington, DC, USA.
How Does the New Drug
Scientists at the Purdue Institute for Drug Discovery, Purdue University,
Lafayette, Indiana, USA have developed this novel drug. They have
used an existing anti-cancer drug, dasatinib
and chemically attached the amino acid aspartic acid to
synthesize dasatinib-aspartate10-conjugate (DAC)
. This new drug has been
found to promote the growth of new bone tissue.
‘A new drug for treating bone fractures has been developed. The drug, when injected intravenously, specifically targets the fracture site and accelerates the healing process. The time for complete healing is significantly shortened, accompanied by an appreciable increase in bone density. This could be a major breakthrough in the treatment of fractures.’
When injected intravenously, the drug is targeted to the
fracture site and accelerates the repair of the bone and increases the bone
density. While it normally takes around 8 weeks for a fracture to completely
heal; with this new drug, the time can be reduced to 3-4 weeks.
Mingding Wang, PhD Candidate at the Purdue Institute for Drug
Discovery and the presenting author, said: "We
foresee a significant need for this type of therapy." "Even though many broken
bones don't need surgery, most require a prolonged healing process that can
lead to morbidity, loss of work productivity, and in some cases even death. By
developing a therapy that can accelerate bone fracture repair without damaging
healthy bones or tissues, we can hopefully address these critical issues."
The study found that administration of DAC on alternate days for 3 weeks
was equally as effective as administering the drug every day, which increased
the bone density by a staggering 114%. This alternate-day approach was found to
be the most effective treatment regimen. However, if the drug was administered
every 4 days, the clinical efficacy of DAC decreased appreciably.
It is well established that the blood supply in the vicinity of a
fracture is disrupted soon after it occurs. The study found that if DAC
administration was delayed for a couple of weeks in order to give a chance for
the blood vessels to regenerate at the fracture site, there was no negative
impact on the drug's efficacy or the time required for complete healing.
It was also found that when dasatinib was
administered alone, there was only a marginal improvement in fracture healing,
since this drug is non-targeted. However, when DAC was administered, there was
a dramatic improvement in healing, with a doubling of bone density. This arose
from the fact that DAC directly targets the fracture site. Moreover, since
dasatinib itself is not significantly toxic when used in chronic cancer
patients, it is quite plausible that its targeted form (DAC) would be much less
toxic as it would be concentrated at the fracture site, without harming other
healthy tissues in the body.
Professor Philip S. Low, Ralph C. Corley
Distinguished Professor of Chemistry and Director of the Purdue Institute for
Drug Discovery and also the Principal Investigator of the study, said: "While the use of casts, rods, or pins may
still be required in some cases, the ability of this therapy to accelerate the
return of a fracture patient to normal function and lifestyle could have
widespread benefits to the entire orthopedic community."
The research team plans to investigate the efficacy of DAC in other types
of fractures such as long-bone fractures, hip fractures, craniofacial
fractures, nonunion fractures, and spinal fusions.
- AAPS Press Room - (https://www.aaps.org/news/for-media/press-room)
- Fracture Epidemiology - (https://www.capturethefracture.org/fracture-epidemiology)