Drug reference

Everolimus

Tyrosine Kinase Inhibitor · Immunosuppressant, Antineoplastic

Also known as AFINITOR, CERTICAN, VOTUBIA DISPERSIBLE TABLETS

Tyrosine Kinase InhibitorImmunosuppressant, AntineoplasticATC L01XE10

CDSCO approvedSchedule HATC L01XE10

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AcyclovirSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AmikacinSevereDatabaseDDInter
Amphotericin BSevereDatabaseDDInter

Mechanism

Everolimus is a protein kinase inhibitor that acts as a mammalian target of rapamycin (mTOR) inhibitor. This action targets growth-factor pathways, which substantially limits clonal expansion and potentially promotes tolerance.

Indications

Neuroendocrine tumours of pancreatic originNeuroendocrine tumours of gastro-intestinal originNeuroendocrine tumours of lung originRenal cell carcinomaHormone-receptor positive HER2-negative breast cancer [in combination with exemestane]Liver transplantationRenal transplantationHeart transplantationSubependymal giant cell astrocytoma associated with tuberous sclerosis complexastrocytomabreast cancerkidney and liver transplant reception prophylaxispancreatic neuroendocrine tumorrenal angiomyolipomarenal cell canceradvanced renal cell carcinomapostmenopausal women with advanced hormone receptor–positive, HER2-negative breast cancer (in combination with exemestane) after failure of treatment with letrozole or anastrozoleperipheral neuroendocrine tumors (PNETs)progressive, well-differentiated, nonfunctional NETs of GI or lung originTSC-related tumorsConsidered for patients without targetable mutations in ER-positive metastatic breast cancer, in combination with an aromatase inhibitor, shown to increase progression-free survival over endocrine therapy aloneAdvanced progressing pancreatic neuroendocrine tumors (NETs)Advanced extrapancreatic neuroendocrine tumors (NETs)Improving glycemic control in patients with insulinomaTSC-associated kidney tumorsnonkidney manifestations of Tuberous Sclerosis (TS)

Dosing

Adult: Neuroendocrine tumours (pancreatic, GI, lung), Renal cell carcinoma, Hormone-receptor positive HER2-negative breast cancer (in combination with exemestane): 10 mg once daily by mouth; for dose interruption or adjustments due to side effects—consult product literature.…
Renal adjustment: Manufacturer advises caution in severe impairment—monitor for signs of toxicity.
Hepatic adjustment: For everolimus, the dose should be reduced for patients with moderate hepatic impairment.

Pharmacokinetics

Duration

maintains inhibition of mTORC1 for 7 days in white blood cells

Half-life

30 h (elimination)

Metabolism

Pharmacokinetics distinct from sirolimus

Side effects

Common

Disturbance of glucose metabolismhyperlipidemiaanemialeukopeniathrombocytopeniagi effectsmouth ulcershyperkalemiamild maculopapular rashmucositisfatigue (30%–50%)hyperglycemiahypertriglyceridemiaStomatitisRash

Serious