Active ingredient of the month January: Sirolimus

Sirolimus, also known as rapamycin, is an immunosuppressant and mTOR inhibitor with a macrolide structure. It is a product of the streptomycete Streptomyces hygroscopicus. This species of bacteria was first isolated from the soil of the island of Rapa Nui.

Active ingredient from Easter Island avoids restenosis in stents

Sirolimus is indicated for:

  • Prophylaxis of renal transplant rejection in adult patients with a low to moderate immunological risk
  • Treatment of patients with sporadic lymphangioleiomyomatosis
  • In the form of a gel for the local treatment of facial angiofibromas in the context of tuberous sclerosis.

Another area of application is in the field of cardiology. For example, sirolimus can prevent restenosis in stents. Background: Around 30 percent of patients develop restenosis after stent implantation.

Drug Eluting Stents with High Success Rate

DES, i.e. “drug eluting stents”, stands for a special stent variant. Here, the metal framework is coated from the inside with a drug, such as sirolimus. This prevents the stent from calcifying again or being overgrown by endothelial cells.

The first stents coated with sirolimus were used in Brazil and the Netherlands. While the patients in the first-in-man study did not experience any relevant restenosis or side effects, the comparison with conventional stents also showed interesting results: Of the approximately 240 patients, restenosis occurred in 26 percent of cases after just one year.
The sirolimus group remained permanently free of restenosis, including diabetics, who are at increased risk of restenosis.

Fixation of the active ingredient without the additional use of polymers

We, Cfm Oskar Tropitzsch GmbH, have been supplying Sirolimus for the production of drug eluting stents for years. Our partners succeeded in developing new surface structures and coating processes. These enable the active ingredient to be fixed without the additional use of polymers.

Do you have any questions about this topic or specifically about sirolimus/rapamycin?

Feel free to send us your inquiry or a message via our contact form. We will be happy to advise you.

Our product recommendations on the topic:

Rapamycin, GMP/API

Rapamycin, Research Reagent

Rapamycin fluorescein


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