Rolimus 5mg Tablet (Everolimus)

The Rolimus 5mg Tablet contains everolimus 5 mg, an mTOR inhibitor. The medicine is used in the treatment of organ transplantation as well as breast cancer, lung cancer, pancreatic cancer, and kidney cancer. However, at this strength, the product is principally aligned with transplant immunosuppression rather than the higher-dose oncology formulations commonly used in cancer.

Everolimus tablet suppresses lymphocyte proliferation by inhibiting mTOR, helping reduce the risk that the immune system attacks a transplanted organ. It is generally used with a reduced-exposure calcineurin inhibitor and corticosteroids in selected kidney or liver transplant recipients. The drug concentration must be monitored at all times to ensure that it remains within the correct range. The 5 mg transplant strength cannot be considered appropriate for use in oncology without prior verification.

• Kidney transplant—Helps to avoid organ rejection following kidney transplant.
• Liver transplant—Helps to avoid organ rejection following liver transplant.
• Breast cancer—Recommended for advanced breast cancer positive for hormone receptors and negative for HER2.
• Lung cancer—Used for advanced lung neuroendocrine tumors.
• Pancreatic cancer—Used for advanced pancreatic neuroendocrine tumors.
• Kidney cancer—Used for advanced kidney (renal cell) carcinoma.
  

Transplantation formulation of 5 mg is mostly used along with other immunosuppressants to avoid organ rejection. The use of the everolimus 5mg tablet for treating cancer is different from that of transplantation; therefore, it should be considered as separate indications.

The Rolimus 5mg Tablet binds to the FKBP-12 protein, inhibiting the mTORC1 pathway, which plays a vital role in the growth and proliferation of the immune cells. This makes the T and B lymphocytes inactive, thus suppressing the response of the immune system to the graft.

Kidney-transplant studies: The everolimus tablet with reduced calcineurin-inhibitor exposure has shown effective rejection prevention in selected kidney-transplant recipients.

TRANSFORM: A large study supported the Everolimus 5mg tablet plus reduced calcineurin inhibitor exposure as a viable immunosuppression strategy.

The Rolimus Tablet can result in various adverse effects on the body that can range from mild side effects to severe side effects, including

Common side effects

• Mouth ulcers
• Infections
• High lipids
• Edema
• Anemia
• Diarrhea
• Headache
• Proteinuria

Serious side effects

• Serious/opportunistic infection
• Non-infectious pneumonitis
• Impaired wound healing
• Graft-vessel thrombosis considerations
• Kidney dysfunction/proteinuria
• Malignancy risk from immunosuppression
  

Important: These are only general references to be used when giving treatments. The physician will prescribe the proper dosage, frequency, interaction with other drugs, adjustment of dosage because of renal or hepatic dysfunction, and management of adverse effects depending on the patient's status.

If a dose is missed, do not double the next dose. Follow the transplant team’s instructions and report repeated missed doses promptly to the doctor because stable immunosuppression protects the graft.

• Check everolimus 5mg tablet levels in the blood periodically to ensure that the drug is maintained at an appropriate level.
• Test kidney function and protein in the urine to identify any kidney-related side effects.
• Perform CBC tests to evaluate the RBCs, WBCs, and platelets.
• Monitor cholesterol and triglyceride levels since the Rolimus 5 mg tablet can raise levels of blood lipids.
• Check the function of your liver using periodic blood tests.
• Notify your healthcare provider in case you have a fever, cough, difficulty breathing, or other infection symptoms.
• Monitor the function of your graft for proper functioning of the transplant organ.​
  

• Current everolimus transplant prescribing information (Zortress/Certican or local equivalent) https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021560s008lbl.pdf​
• Pascual J, et al. TRANSFORM study https://pubmed.ncbi.nlm.nih.gov/31152476/​
• Current transplant-centre/KDIGO guidance as applicable https://kdigo.org/guidelines/transplant-candidate/​
• National Kidney Foundation. KDIGO Clinical Practice Guideline for the Care of Kidney Transplant Recipients https://kdigo.org/wp-content/uploads/2017/02/KITxpGL_summary.pdf​
• European Medicines Agency. Certican (everolimus) – Product Information https://www.medicines.org.uk/emc/product/1920/smpc#gref​