Zotarolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by preparation of the 42-triflate ester, followed by displacement with tetrazole and purification of the two isomeric products. This structural change affords a less bioavailable product, a preferred profile for some applications. Zotarolimus is extensively cited in the literature with over 200 citations.
|Mechanism of Action||Zotarolimus binds to a receptor protein (FKBP12). The complex then binds to mTOR preventing it from interacting with target proteins.|
|References||Compositions, systems, and kits for administering zotarolimus and paclitaxel to blood vessel lumens. Burke S.E. et al. US Patent 7,357,942, 2008.|
Zotarolimus, a novel sirolimus analogue with potent anti-proliferative activity on coronary smooth muscle cells and reduced potential for systemic immunosuppression Chen Y.W. et al. J. Cardiovasc. Pharmacol. 2007, 49, 228.