Everolimus
- Atc Codes:L01XE10#L04AA18
- CAS Codes:159351-69-6
- PHARMGKB ID:159351-69-6
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
Chemistry
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[30.3.1.04,9]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.
Contraindications
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.