Acute Porphyria Drug Database

L01EG02 - Everolimus
Propably not porphyrinogenic
PNP

Important Information
Patients on drug therapy causing immunosuppression have an increased risk of infections. Since infections have a potential to trigger acute porphyric attacks vigilance is motivated regarding signs or symptoms of infection and/or possible symptoms of a porphyric attack. Side effects like diarrhoea, nausea and vomiting may potentially be porphyrinogenic through reduction in carbohydrate intake.
Side effects
Infections are common in patients using immunosuppressants and since infections might trigger an acute porphyric attack, vigilance regarding signs and symptoms of an infection and/ or a porphyric attack is recommended. Common adverse reactions of everolimus that can be confused with an acute porphyric attack are diarrhoea, vomiting, and nausea. These side effects may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Everolimus is not a mechanism based inhibitor of CYP3A4 or CYP2C9, and there are no signs of relevant in vivo induction of the liver drug metabolizing enzymes. No pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Everolimus is a hydroxyethyl derivative of rapamycin, which is a macrolide, isolated from the micro-organism Streptomyces hygroscopicus.
Therapeutic characteristics
Everolimus is an antineoplastic agent indicated for the treatment of patients with advanced renal cell carcinoma, neuroendocrine tumors of pancreatic origin and hormone receptor-positive advanced breast cancer. It is also used as a proliferation signal inhibitor in the prevention of graft rejection episodes in patients undergoing renal or cardiac transplantation as part of an immunosuppressive regimen that includes ciclosporin (microemulsifying) and corticosteroids. It is administered orally.
Metabolism and pharmacokinetics
The major enzyme responsible for the oxidative metabolism of everolimus in human liver microsomes was CYP3A4. Everolimus has shown to be a competitive inhibitor of the CYP3A4 and a mixed inhibitor of the CYP2D6. Everolimus has little or no effect on the metabolism of paclitaxel, tolbutamide and s-mephenytoin by CYP2C8, CYP2C9 and CYP2C19, respectively. There were no signs of relevant in vivo induction of the liver drug metabolizing enzymes by everolimus, although no data from hepatocytes were available.

References

  1. Drug reference publications
  2. McEvoy GK, editor. Everolimus. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (30.09.10). #2272
  3. Sweetman SC, editor. Martindale: The complete drug reference. Everolimus. Pharmaceutical Press 2009. #2273
  4. Summary of Product Characteristics
  5. The electronic Medicines Compendium (eMC). Afinitor. Summary of Product Characteristics (SPC). #2274

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