The present invention relates to pharmaceutical compositions in
particulate form or in solid dosage forms comprising sirolimus
(rapamycin) and/or derivatives and/or analogues thereof. Compositions of
the invention exhibit an acceptable bioavailability of sirolimus and/or a
derivative and/or an analogue thereof. The pharmaceutical compositions of
the invention are designed to release sirolimus in a controlled manner so
that the plasma levels stays within the narrow therapeutic window that
exist for this class of substances. An extended release profile, where
the peak concentration has been reduced without loosing significant
bioavailability, together with less variable absorption, is expected to
improve the safety/efficacy ratio of the drug. Furthermore, compositions
according to the invention provide for a significant reduced food effect
and a delayed release of sirolimus is expected to reduce the number of
gastro-intestinal related side effects.