Zotarolimus

Zotarolimus is a semi-synthetic derivative of rapamycin. It was developed by Abbott Laboratories and is used primarily in drug-eluting stents to prevent restenosis, a complication that can occur after angioplasty procedures. Zotarolimus works by inhibiting the proliferation of smooth muscle cells in the arterial wall, a key factor in the development of restenosis.

History

Zotarolimus was developed by Abbott Laboratories in the early 2000s as a new type of drug for use in drug-eluting stents. The drug was designed to be more lipophilic than its parent compound, rapamycin, in order to improve its distribution within the arterial wall.

Pharmacology

Zotarolimus is a semi-synthetic derivative of rapamycin, a naturally occurring compound produced by the bacterium Streptomyces hygroscopicus. Like rapamycin, zotarolimus works by binding to the protein FKBP12, which then inhibits the mTOR pathway. This inhibition prevents the proliferation of smooth muscle cells in the arterial wall, a key factor in the development of restenosis.

Clinical use

Zotarolimus is used primarily in drug-eluting stents, which are used in angioplasty procedures to treat coronary artery disease. The drug is released slowly from the stent over time, helping to prevent the development of restenosis.

Side effects

As with any drug, zotarolimus can have side effects. These can include hypotension, bradycardia, and peripheral edema. However, these side effects are generally rare and the drug is considered to be well-tolerated.

See also

• Rapamycin
• Drug-eluting stent
• Restenosis
• Angioplasty

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