pharmacopeia
GET
/api/v1/drug/everolimus

Mechanism of action

Sourced from openFDA

Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), a serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC).

Cytochrome P450 2D6Cytochrome P450 3A4Protein KinasemTOR

Indications

Sourced from openFDA
  • 1. INDICATIONS AND USAGE Everolimus tablets are a kinase inhibitor indicated for the treatment of: Postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole.ICD-10: C50.919

Contraindications

Sourced from openFDA
  • 4. CONTRAINDICATIONS Everolimus tablets/everolimus tablets for oral suspension are contraindicated in patients with clinically significant hypersensitivity to everolimus or to other rapamycin derivatives [see Warnings and Precautions (5.3) ].contraindicated

Dosage & administration

Sourced from openFDA

2. DOSAGE AND ADMINISTRATION Do not combine everolimus tablets and everolimus tablets for oral suspension to achieve the total daily dose. ( 2.1 ) Modify the dose for patients with hepatic impairment or for patients taking drugs that inhibit or induce P-glycoprotein (P-gp) and CYP3A4. ( 2.1 ) Breast Cancer: 10 mg orally once daily. ( 2.2 ) NET: 10 mg orally once daily. ( 2.3 ) RCC: 10 mg orally once daily. ( 2.4 ) TSC-Associated Renal Angiomyolipoma: 10 mg orally once daily. ( 2.5 ) TSC-Associated SEGA: 4.5 mg/m 2 orally once daily; adjust dose to attain trough concentrations of 5-15 ng/mL. ( 2.6 , 2.8 ) TSC-Associated Partial-Onset Seizures: 5 mg/ m 2 orally once daily; adjust dose to attain trough concentrations of 5-­15 ng/mL. ( 2.7 , 2.8 ) 2.1 Important Dosage Information Everolimus tablets and everolimus tablets for oral suspension are two different dosage forms. Select the recommended dosage form based on the indication [see Indications and Usage (1) ] . Do not combine everolimus tablets and everolimus tablets for oral suspension to achieve the total dose. Modify the dosage for patients with hepatic impairment or for patients taking drugs that inhibit or induce P-glycoprotein (P-gp) and CYP3A4 [see Dosage and Administration (2.10 , 2.11 , 2.12) ]. 2.2 Recommended Dosage for Hormone Receptor-Positive, HER2-Negative Breast Cancer The recommended dosage of everolimus tablets is 10 mg orally once daily until disease progression or unacceptable toxicity.

Warnings & precautions

Sourced from openFDA

5. WARNINGS AND PRECAUTIONS Non-Infectious Pneumonitis: Monitor for clinical symptoms or radiological changes. Withhold or permanently discontinue based on severity. ( 2.9 , 5.1 ) Infections: Monitor for signs and symptoms of infection. Withhold or permanently discontinue based on severity. ( 2.9 , 5.2 ) Severe Hypersensitivity Reactions: Permanently discontinue for clinically significant hypersensitivity. ( 5.3 ) Angioedema: Patients taking concomitant angiotensin-converting-enzyme (ACE) inhibitors may be at increased risk for angioedema. Permanently discontinue for angioedema. ( 5.4 , 7.2 ) Stomatitis: Initiate dexamethasone alcohol-free mouthwash when starting treatment. ( 5.5 , 6.1 ) Renal Failure: Monitor renal function prior to treatment and periodically thereafter. ( 5.6 ) Risk of Impaired Wound Healing: Withhold for at least 1 week prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of treatment after resolution of wound healing complications has not been established. ( 5.7 ) Geriatric Patients: Monitor and adjust dose for adverse reactions. ( 5.8 ) Metabolic Disorders: Monitor serum glucose and lipids prior to treatment and periodically thereafter. Withhold or permanently discontinue based on severity. ( 2.9 , 5.9 ) Myelosuppression: Monitor hematologic parameters prior to treatment and periodically thereafter. Withhold or permanently discontinue based on severity.

Adverse reactions

Sourced from openFDA

6. ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in the labeling: Non-Infectious Pneumonitis [see Warnings and Precautions (5.1) ] Infections [see Warnings and Precautions (5.2) ] Severe Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Angioedema with Concomitant Use of ACE inhibitors [see Warnings and Precautions (5.4) ] Stomatitis [see Warnings and Precautions (5.5) ] Renal Failure [see Warnings and Precautions (5.6) ] Impaired Wound Healing [see Warnings and Precautions (5.7) ] Metabolic Disorders [see Warnings and Precautions (5.9) ] Myelosuppression [see Warnings and Precautions (5.10) ] Radiation Sensitization and Radiation Recall [see Warnings and Precautions (5.12) ] Breast cancer, NET, RCC: Most common adverse reactions (incidence ≥ 30%) include stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, and decreased appetite. ( 6.1 ) TSC-Associated Renal Angiomyolipoma: Most common adverse reaction (incidence ≥ 30%) is stomatitis. ( 6.1 ) TSC-Associated SEGA: Most common adverse reactions (incidence ≥ 30%) are stomatitis and respiratory tract infection. ( 6.1 ) TSC-Associated Partial-Onset Seizures: Most common adverse reaction (incidence ≥ 30%) is stomatitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Breckenridge Pharmaceutical, Inc. at 1-800-367-3395 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Use in specific populations

Sourced from openFDA

8. USE IN SPECIFIC POPULATIONS For breast cancer, NET, RCC, or TSC-associated renal angiomyolipoma patients with hepatic impairment, reduce the dose. ( 2.10 , 8.6 ) For patients with TSC-associated SEGA or TSC-associated partial-onset seizures and severe hepatic impairment, reduce the starting dose and adjust dose to attain target trough concentrations. ( 2.8 , 2.10 , 8.6 ) 8.1 Pregnancy Risk Summary Based on animal studies and the mechanism of action [see Clinical Pharmacology (12.1) ] , everolimus tablets/everolimus tablets for oral suspension can cause fetal harm when administered to a pregnant woman. There are limited case reports of everolimus tablets use in pregnant women; however, these reports are not sufficient to inform about risks of birth defects or miscarriage. In animal studies, everolimus caused embryo-fetal toxicities in rats when administered during the period of organogenesis at maternal exposures that were lower than human exposures at the recommended dose of everolimus tablets 10 mg orally once daily (see Data ) . Advise pregnant women of the potential risk to the fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage is 2% to 4% and 15% to 20% of clinically recognized pregnancies, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption After administration of everolimus tablets in patients with advanced solid tumors, peak everolimus concentrations are reached 1 to 2 hours after administration of oral doses ranging from 5 mg to 70 mg. Following single doses, C max is dose-proportional with daily dosing between 5 mg and 10 mg.

Approval history

Sourced from openFDA
  • Mar 30, 2009NDANDA022334Novartis
  • Apr 20, 2010NDANDA021560Novartis
  • Aug 29, 2012NDANDA203985Novartis Pharm
  • Apr 12, 2018ANDAANDA206133Hikma
  • Dec 9, 2019ANDAANDA210050Teva Pharms Usa
  • Dec 9, 2019ANDAANDA207934Ph Health
  • Jun 8, 2020ANDAANDA207486Hikma
  • Feb 11, 2021ANDAANDA214182Biocon Pharma

FDA shortages

View JSON

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Everolimus, Tablet, 10 mg (NDC 0093-7769-24)To be discontinued
    Sponsor: Teva Pharmaceuticals USA, Inc.
    Updated
  • Everolimus, Tablet, 10 mg (NDC 49884-128-91)To be discontinued
    Sponsor: Endo Pharmaceuticals, Inc.
    Updated
  • Everolimus, Tablet, 2 mg (NDC 0378-0005-85)To be discontinued
    Sponsor: Mylan Pharmaceuticals Inc., a Viatris Company
    Updated
  • Everolimus, Tablet, 2.5 mg (NDC 0093-7766-24)To be discontinued
    Sponsor: Teva Pharmaceuticals USA, Inc.
    Updated
  • Everolimus, Tablet, 2.5 mg (NDC 49884-119-91)To be discontinued
    Sponsor: Endo Pharmaceuticals, Inc.
    Updated
  • Everolimus, Tablet, 3 mg (NDC 0378-0006-85)To be discontinued
    Sponsor: Mylan Pharmaceuticals Inc., a Viatris Company
    Updated
  • Everolimus, Tablet, 5 mg (NDC 0093-7767-24)To be discontinued
    Sponsor: Teva Pharmaceuticals USA, Inc.
    Updated
  • Everolimus, Tablet, 5 mg (NDC 0378-0007-85)To be discontinued
    Sponsor: Mylan Pharmaceuticals Inc., a Viatris Company
    Updated
  • Everolimus, Tablet, 5 mg (NDC 49884-125-91)To be discontinued
    Sponsor: Endo Pharmaceuticals, Inc.
    Updated
  • Everolimus, Tablet, 7.5 mg (NDC 0093-7768-24)To be discontinued
    Sponsor: Teva Pharmaceuticals USA, Inc.
    Updated
  • Everolimus, Tablet, 7.5 mg (NDC 49884-127-91)To be discontinued
    Sponsor: Endo Pharmaceuticals, Inc.
    Updated

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
50,182 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death6,33313%
  2. 2Malignant Neoplasm Progression4,6409.2%
  3. 3Diarrhoea4,0248.0%
  4. 4Fatigue3,7787.5%
  5. 5Stomatitis3,1746.3%
  6. 6Nausea2,8155.6%
  7. 7Dyspnoea2,6315.2%
  8. 8Drug Ineffective2,3264.6%
  9. 9Pyrexia2,1294.2%
  10. 10Vomiting2,1134.2%
  11. 11Decreased Appetite2,1024.2%
  12. 12Rash1,9713.9%
  13. 13Weight Decreased1,9263.8%
  14. 14Cough1,8893.8%
  15. 15Asthenia1,8803.7%

Literature

View JSON

Recent PubMed references pinned to Everolimus as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 1,213 ClinicalTrials.gov registrations naming Everolimus as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Everolimus work?
Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), a serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC).
What is Everolimus used for?
According to FDA labeling, Everolimus carries indications including: 1. INDICATIONS AND USAGE Everolimus tablets are a kinase inhibitor indicated for the treatment of: Postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Everolimus?
Everolimus is classified as Mammalian target of rapamycin (mTOR) kinase inhibitors, Kinase Inhibitor, mTOR Inhibitor Immunosuppressant, Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A4 Inhibitors, mTOR Inhibitors, Protein Kinase Inhibitors, Decreased Immunologic Activity.
What are the brand names for Everolimus?
Everolimus is marketed under brand names including Afinitor, Torpenz, Zortress.
What are the contraindications for Everolimus?
Everolimus labeling lists contraindications including: 4. CONTRAINDICATIONS Everolimus tablets/everolimus tablets for oral suspension are contraindicated in patients with clinically significant hypersensitivity to everolimus or to other rapamycin derivatives [see Warnings and Precautions (5.3) ].. Always consult the full prescribing information and a clinician.
Note. Data for everolimus is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients