Everolimus

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Everolimus is an ofp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2009. Its mechanism of action is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A4 Inhibitors and mTOR Inhibitors. DrugCentral lists 3 molecular targets, including MTOR, FKBP1A and ABCB1. Recorded indications include Angiomyolipoma of kidney, Carcinoma of breast, Hormone receptor positive malignant neoplasm of breast and Pancreatic Neuroendocrine Tumor.

• Approval status: ofp (first approved 2009 by the FDA).
• Drug class: Kinase Inhibitor; mTOR Inhibitor Immunosuppressant.
• Mechanism of action: Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A4 Inhibitors; mTOR Inhibitors.
• Molecular targets: MTOR, FKBP1A and ABCB1 (3 listed in DrugCentral).
• Indications: Angiomyolipoma of kidney, Carcinoma of breast, Hormone receptor positive malignant neoplasm of breast, Pancreatic Neuroendocrine Tumor and Prevention of Kidney Transplant Rejection and others.
• ATC code: L01EG02 (Mammalian target of rapamycin (mTOR) kinase inhibitors).
• Molecular formula: C53H83NO14; molecular weight 958.24 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (8)

• Angiomyolipoma of kidney
• Carcinoma of breast
• Hormone receptor positive malignant neoplasm of breast
• Pancreatic Neuroendocrine Tumor
• Prevention of Kidney Transplant Rejection
• Renal cell carcinoma
• Subependymal Giant Cell Astrocytoma associated with Tuberous Sclerosis
• Tuberous sclerosis syndrome

Contraindications (30)

• Acute infectious disease
• Acute nephropathy
• Anemia
• Ascites
• BK Polyomavirus Reactivation Nephropathy
• Breastfeeding (mother)
• Diabetes mellitus
• Disease of liver
• Edema
• Hemolytic uremic syndrome
• Hepatic failure
• Hypercholesterolemia
• Hyperglycemia
• Hyperlipidemia
• Hypertriglyceridemia
• Impaired wound healing
• Interstitial pneumonia
• Kidney disease
• Leukopenia
• Malignant lymphoma
• Neutropenic disorder
• Pericardial effusion
• Pleural Effusions
• Pregnancy, function
• Primary malignant neoplasm
• Proteinuria
• Stomatitis
• Thrombocytopenic disorder
• Thrombosis of renal artery
• Thrombotic thrombocytopenic purpura

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A4 Inhibitors; mTOR Inhibitors; Protein Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor; mTOR Inhibitor Immunosuppressant

Molecular targets (3)

Target	Gene	Action	Activity
Serine/threonine-protein kinase mTOR	MTOR	inhibitor	IC50 8.70
Peptidyl-prolyl cis-trans isomerase FKBP1A	FKBP1A	inhibitor	IC50 8.26
Multidrug resistance protein 1	ABCB1	unknown	—

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2019-08-22	PMDA	—	Novartis Pharma K.K.	Yes
2011-09-02	EMA	—	—
2009-03-30	FDA	—	NOVARTIS

ATC classification

ATC code	Therapeutic hierarchy
L01EG02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mammalian target of rapamycin (mTOR) kinase inhibitors
L04AH02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Mammalian target of rapamycin (mTOR) kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ERBB2, ESR1, ESR2 · Testing Required
• FDA label: ERBB2, ESR1, ESR2 · Testing Required
• HCSC label: ERBB2, ESR1, ESR2 · Testing Required
• PMDA label: ERBB2, ESR1, ESR2 · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Malignant neoplasm progression	5517.7
Metastases to liver	1870.7
Stomatitis	1678.0
Metastases to bone	1465.7
Pneumonitis	1459.2
Neoplasm progression	987.5
Metastases to lung	859.8
Polyomavirus-associated nephropathy	785.8
Death	687.6
BK virus infection	614.4
Transplant rejection	558.3
Interstitial lung disease	550.7

Chemical structure

• Molecular formula: C₅₃H₈₃NO₁₄
• Molecular weight: 958.24 g/mol
• CAS number: 159351-69-6
• InChIKey: HKVAMNSJSFKALM-GKUWKFKPSA-N
• PubChem CID: 6442177

CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)OC)CC[C@H]1OCCO

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Everolimus used for?

DrugCentral lists the following indications for Everolimus: Angiomyolipoma of kidney, Carcinoma of breast, Hormone receptor positive malignant neoplasm of breast, Pancreatic Neuroendocrine Tumor, Prevention of Kidney Transplant Rejection, Renal cell carcinoma, Subependymal Giant Cell Astrocytoma associated with Tuberous Sclerosis and Tuberous sclerosis syndrome.

How does Everolimus work?

Everolimus is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A4 Inhibitors and mTOR Inhibitors; its molecular targets in DrugCentral include MTOR (inhibitor), FKBP1A (inhibitor) and ABCB1.

When was Everolimus first approved?

Everolimus was first approved by the FDA in 2009.

What drug class does Everolimus belong to?

Everolimus is in the Kinase Inhibitor class.

What is the chemical formula of Everolimus?

Everolimus has the molecular formula C53H83NO14 and a molecular weight of 958.24 g/mol.

Sources

• DrugCentral drug card 1118 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1908360 — compound record and bioactivity
• PubChem CID 6442177 — chemical identifiers
• DrugBank DB01590 — drug record
• FDA UNII 9HW64Q8G6G — substance identity
• DailyMed: FDA labels for Everolimus — current prescribing information (label search)
• UniProt P42345 (MTOR) — target protein
• UniProt P62942 (FKBP1A) — target protein
• UniProt P08183 (ABCB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.