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SSR69071: A highly potent elastase inhibitor More than one
million new and recurrent cases of coronary attack occurred in the US in 1998.
Forty percent of these patients died, 220,000 before even reaching hospital,
making coronary heart disease the single leading cause of death in America. In
the event of coronary attack the primary aim is to reverse ischemia, limit
infarct size, reduce cardiac work and over the longer-term, to prevent
recurrence. Immediate treatment of myocardial infarction includes the use of
thrombolytics to reverse ischemia. Human leukocyte
elastase (HLE) is a proteinase, capable of degrading a variety of proteins.
Under normal circumstances, the proteolytic activity of HLE is effectively
controlled by its natural inhibitors. However, an imbalance between elastase
and its endogenous inhibitors may result in several pathophysiological states
such as chronic inflammatory diseases, cardiovascular disorders and chronic
obstructive pulmonary disease (including emphysema and chronic bronchitis).
The therapeutic targeting of HLE as well as other key targets in the context
of COPD is reviewed in our state of the art COPD dossier. SSR69071 is a
potent (0.02nM) inhibitor of HLE that exhibits oral activity in the mg/kg
range. SSR69071 decreases significantly the acute lung haemorrhage induced by
HLE as well as carrageenan and HLE-induced paw oedema in rats Neutrophil
elastase contributes to the severity of cardiac damage following coronary
ischemia and reperfusion. Thus Sanofi-Synthelabo researchers have recently
evaluated the effect of SSR69071 on infarct size in anaesthetized rabbits with
coronary ischemia/reperfusion injury. SSR69071 reduced cardiac infarct size
when administered before ischemia (-39%, P<0.05) or just prior to
reperfusion (-37%, P<0.05). This cardioprotective activity was associated
with inhibition of cardiac elastase. Entry date March, 2003 Adapted from Bidouard et al, Eur J Pharmacol 2003 Feb 7;461(1):49-52.
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