Cyclosporine (Sandimmune, Neoral, Gengraf)
Other Medications · Approved since 1983
Description
Cyclosporine is a calcineurin inhibitor immunosuppressant that has been repurposed for colorectal cancer treatment as a multidrug resistance (MDR) reversal agent. In CRC, cyclosporine is used in combination with chemotherapy agents like irinotecan to overcome drug resistance mechanisms that limit treatment effectiveness. The drug's ability to inhibit P-glycoprotein efflux pumps makes it valuable for enhancing the efficacy of standard chemotherapy regimens in advanced and metastatic colorectal cancer.
Mechanism of Action
Cyclosporine inhibits calcineurin, a calcium-dependent phosphatase involved in T-cell activation, but in cancer treatment it primarily functions by blocking P-glycoprotein (ABCB1) efflux pumps in tumor cells. By inhibiting these drug efflux mechanisms, cyclosporine increases intracellular accumulation of chemotherapy agents like irinotecan, potentially overcoming multidrug resistance and enhancing cytotoxic effects against colorectal cancer cells.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Sandimmune, Neoral, Gengraf |
| Category | Other Medications |
 Status | Off-label |
 EMA Status | EMA Approved |
 Spain Access | Hospital use off-label in CRC |
| Administration | IV, Oral |
| Year Approved | 1983 |
| Clinical Trials | 3 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.