product introduction :::
SPK-843 new antifungal agent
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A NEW INJECTABLE ANTIFUNGAL AGENT
Conclusions
SPA-S-753 is a new chemical entity obtained from the polyene partricin
A and is endowed with very high in vitro and in vivo antifungal activity.
The new diascorbate salt of the same active base, SPK-843, is even more promising
because of its improved chemico-physical properties and stability and has been
now addressed to the clinical development.
SPK-843 will be indicated in the form of a drip infusion in 10% Intralipid
? to the treatment of deep seated infections provoked by Candida, Aspergillus,
Cryptococcus and other sensitive microorganisms.
In comparison with amphotericin B, still nowadays the drug of choice in the
treatment of severe mycoses, and with its lipid complexes, SPK-843 is much
more effective in in vitro tests, not showing any resistant strain and also
having the greatest killing speed among all the antifungals know; also more
effective in the experimental infection tests, even after a very limited number
of doses and particularly in the immunocompromised host.
A series of experimental studies, including pharmacodynamic and safety tests
as well as acute and subacute toxicity trials in several animal species, have
always demonstrated that SPK-843 is also much better tolerated than amphotericin
B. We want to stress particularly its reduced nephrotoxic effects. Also the
local tolerability at the injection site is quite satisfactory.
A GCP single, ascending-dose, safety, tolerability and pharmacokinetic study
by drip infusion in healthy volunteers has been started on mid 2000 and is
about to be completed .
To conclude, it is emphasized that SPK-843 represents the first true improvement
over amphotericin B and the other current therapies. It may fulfil the most
important criteria for an ideal, more effective and safer antifungal agent,
for which there is at present a strong medical and market interest.