Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Austria: Afinitor, Certican; Belgium: Afinitor, Certican; Bulgaria: Certican; Cyprus: Certican; Czech Republic: Afinitor, Certican; Denmark: Afinitor, Certican; Estonia: Afinitor, Certican; Finland: Afinitor, Certican; France: Afinitor, Certican; Germany: Afinitor, Certican; Greece: Afinitor, Certican; Hungary: Afinitor, Certican; Ireland: Afinitor; Italy: Afinitor, Certican; Latvia: Afinitor, Certican; Lithuania: Afinitor, Certican; Luxembourg: Afinitor, Certican; Malta: Afinitor, Certican; Netherlands: Afinitor, Certican; Poland: Afinitor, Certican; Portugal: Afinitor, Certican; Romania: Afinitor, Certican; Slovakia: Afinitor, Certican; Slovenia: Afinitor, Certican; Spain: Afinitor, Certican; Sweden: Afinitor, Certican, Everolimus; UK: Afinitor.

North America

Canada: Afinitor; USA: Afinitor, Zortress.

Latin America

Argentina: Certican; Mexico: Certican.

Drug combinations


Everolimus: C~53~H~83~NO~14~ Mw: 958.22. (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-{(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]-1-methylethyl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-aza-tricyclo[,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentaone. CAS-159351-69-6.

Pharmacologic Category

Antineoplastic Agents; mTOR (mammalian target of rapamycin) Kinase Inhibitor. (ATC-Code: L01XE10; L04AA18).

Mechanism of action

Everolimus has antiproliferative and antiangiogenic properties. Reduces protein synthesis and cell proliferation by binding to the FK binding protein-12 (FKBP-12), an intracellular protein, to form a complex that inhibits activation of mTOR (mammalian target of rapamycin) serine-threonine kinase activity. Also reduces angiogenesis by inhibiting vascular endothelial growth factor (VEGF) and hypoxia-inducible factor (HIF-1) expression.

Therapeutic use

Treatment of advanced renal cell cancer, after sunitinib or sorafenib failure.

Pregnancy and lactiation implications

May cause fetal harm if administered during pregnancy. Not recommended during lactation.

Unlabeled use

Immunosuppressant following solid organ transplant.


Hypersensitivity to everolimus, other rapamycin derivatives, or any component of the formulation.

Warnings and precautions

Decreases in hemoglobin, neutrophils, platelets, and lymphocytes have been reported. Everolimus has immunosuppressant properties; the risk for local, opportunistic, systemic infections, and/or sepsis is increased (should be discontinued if invasive systemic fungal infection is diagnosed). Use is associated with mouth ulcers, mucositis, and stomatitis. Non-infectious pneumonitis (sometimes fatal) has been observed with mTOR inhibitors, including everolimus (severe symptoms may require discontinuation). Elevations in serum creatinine (generally mild), blood glucose, and lipids have been observed. The use of live vaccines and close contact with those who have received live vaccines should be avoided during treatment.



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