Afinitor(everolimus)
Afinitor, Votubia, Zortress (everolimus) is a small molecule pharmaceutical. Everolimus was first approved as Afinitor on 2009-03-30. It has been approved in Europe to treat breast neoplasms, pancreatic neoplasms, renal cell carcinoma, and tuberous sclerosis. The pharmaceutical is active against serine/threonine-protein kinase mTOR.
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Novartis Pharmaceuticals
Drugs Approved for Childhood Cancers
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Commercial
Trade Name
FDA
EMA
Afinitor, Afinitor disperz, Zortress (generic drugs available since 2018-04-12)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| afinitor | New Drug Application | 2020-10-17 |
| everolimus | ANDA | 2023-06-08 |
| zortress | New Drug Application | 2021-01-20 |
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
EVEROLIMUS, AFINITOR DISPERZ, NOVARTIS PHARM | |||
| 2025-04-10 | ODE-169 | ||
EVEROLIMUS, AFINITOR, NOVARTIS | |||
| 2023-02-26 | ODE-108 | ||
ATC Codes
L: Antineoplastic and immunomodulating agents
— L01: Antineoplastic agents
— L01E: Protein kinase inhibitors, antineoplastic and immunomodulating agents
— L01EG: Mammalian target of rapamycin (mtor) kinase inhibitors
— L01EG02: Everolimus
— L04: Immunosuppressants
— L04A: Immunosuppressants
— L04AA: Selective immunosuppressants
— L04AA18: Everolimus
HCPCS
Code | Description |
|---|---|
| J7527 | Everolimus, oral, 0.25 mg |
Clinical
Clinical Trials
854 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 32 | 57 | 13 | 2 | 4 | 95 |
| Neoplasms | D009369 | C80 | 45 | 21 | 2 | 2 | 5 | 69 | |
| Coronary artery disease | D003324 | I25.1 | 1 | — | 8 | 26 | 33 | 68 | |
| Renal cell carcinoma | D002292 | 22 | 35 | 7 | 5 | 4 | 65 | ||
| Kidney transplantation | D016030 | — | 5 | 14 | 17 | 1 | 37 | ||
| Neuroendocrine tumors | D018358 | EFO_1001901 | D3A.8 | 12 | 12 | 6 | 3 | 3 | 33 |
| Liver transplantation | D016031 | EFO_0010682 | 3 | 4 | 10 | 5 | 1 | 20 | |
| Coronary disease | D003327 | — | — | 3 | 8 | 7 | 18 | ||
| Heart transplantation | D016027 | EFO_0010673 | — | — | 6 | 7 | — | 13 | |
| Coronary restenosis | D023903 | EFO_0004224 | — | — | 2 | 5 | 5 | 12 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Prostatic neoplasms | D011471 | C61 | 9 | 10 | 1 | — | — | 17 | |
| Kidney neoplasms | D007680 | EFO_0003865 | C64 | 5 | 12 | 1 | — | — | 17 |
| Tuberous sclerosis | D014402 | HP_0009720 | Q85.1 | 5 | 11 | 5 | — | — | 15 |
| Stomach neoplasms | D013274 | EFO_0003897 | C16 | 5 | 8 | 2 | — | — | 12 |
| Triple negative breast neoplasms | D064726 | 3 | 8 | 1 | — | — | 11 | ||
| Carcinoid tumor | D002276 | D3A.00 | 3 | 5 | 2 | — | — | 9 | |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 2 | 6 | 1 | — | — | 7 |
| Astrocytoma | D001254 | EFO_0000271 | 2 | 4 | 1 | — | — | 6 | |
| Large b-cell lymphoma diffuse | D016403 | C83.3 | 3 | 4 | 1 | — | — | 6 | |
| Diffuse intrinsic pontine glioma | D000080443 | 2 | 2 | 1 | — | — | 5 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 9 | 12 | — | — | — | 16 |
| Non-small-cell lung carcinoma | D002289 | 13 | 3 | — | — | — | 15 | ||
| Head and neck neoplasms | D006258 | 9 | 9 | — | — | — | 14 | ||
| Neuroendocrine carcinoma | D018278 | 2 | 10 | — | — | — | 11 | ||
| Sarcoma | D012509 | 4 | 7 | — | — | — | 10 | ||
| Colorectal neoplasms | D015179 | 5 | 8 | — | — | — | 10 | ||
| Hodgkin disease | D006689 | C81 | 7 | 6 | — | — | — | 9 | |
| Lymphoma | D008223 | C85.9 | 6 | 5 | — | — | — | 9 | |
| Glioma | D005910 | EFO_0000520 | 4 | 5 | — | — | — | 9 | |
| Neoplasm metastasis | D009362 | EFO_0009708 | 4 | 5 | — | — | 1 | 9 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Atherosclerosis | D050197 | EFO_0003914 | I25.1 | 1 | — | — | — | 4 | 5 |
| Non-hodgkin lymphoma | D008228 | C85.9 | 3 | — | — | — | — | 3 | |
| Squamous cell carcinoma | D002294 | 3 | — | — | — | — | 3 | ||
| Medullary carcinoma | D018276 | 2 | — | — | — | — | 2 | ||
| Salivary gland neoplasms | D012468 | EFO_0003826 | D11 | 2 | — | — | — | — | 2 |
| Tongue neoplasms | D014062 | EFO_0003871 | C02.9 | 2 | — | — | — | — | 2 |
| Verrucous carcinoma | D018289 | 2 | — | — | — | — | 2 | ||
| Hematologic neoplasms | D019337 | 1 | — | — | — | — | 1 | ||
| Myelomonocytic leukemia chronic | D015477 | C93.1 | 1 | — | — | — | — | 1 | |
| Anemia | D000740 | EFO_0004272 | D64.9 | 1 | — | — | — | — | 1 |
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Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | — | — | — | — | 4 | 4 |
| Angioplasty | D017130 | — | — | — | — | 2 | 2 | ||
| Heart diseases | D006331 | EFO_0003777 | I51.9 | — | — | — | — | 2 | 2 |
| Arterial occlusive diseases | D001157 | EFO_0009085 | — | — | — | — | 2 | 2 | |
| Infarction | D007238 | EFO_0009463 | — | — | — | — | 1 | 1 | |
| Necrosis | D009336 | — | — | — | — | 1 | 1 | ||
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | — | — | — | — | 1 | 1 |
| Drug-eluting stents | D054855 | — | — | — | — | 1 | 1 | ||
| Optical coherence tomography | D041623 | — | — | — | — | 1 | 1 | ||
| Arteriosclerosis | D001161 | EFO_0009086 | I70 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | EVEROLIMUS |
| INN | everolimus |
| Description | Everolimus is a macrocyclic lactone that is rapamycin in which the hydroxy group attached to the cyclohexyl moiety has been converted into the corresponding 2-hydroxyethyl ether. It is an immunosuppressant and antineoplastic agent. It has a role as an antineoplastic agent, an immunosuppressive agent, a mTOR inhibitor, an anticoronaviral agent and a geroprotector. It is a primary alcohol, a secondary alcohol, an ether, a cyclic ketone, a cyclic acetal and a macrolide lactam. It is functionally related to a member of sirolimus. |
| Classification | Small molecule |
| Drug class | immunosuppressives |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](OCCO)[C@H](OC)C2)CC(=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/1C |
Identifiers
| PDB | 6L3A |
| CAS-ID | 159351-69-6 |
| RxCUI | 141704 |
| ChEMBL ID | CHEMBL1908360 |
| ChEBI ID | 68478 |
| PubChem CID | 6442177 |
| DrugBank | DB01590 |
| UNII ID | 9HW64Q8G6G (ChemIDplus, GSRS) |
Target
Agency Approved
MTOR
MTOR
Organism
Homo sapiens
Gene name
MTOR
Gene synonyms
FRAP, FRAP1, FRAP2, RAFT1, RAPT1
NCBI Gene ID
Protein name
serine/threonine-protein kinase mTOR
Protein synonyms
FK506 binding protein 12-rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP-rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, Mammalian target of rapamycin, Mechanistic target of rapamycin, mechanistic target of rapamycin (serine/threonine kinase), mTOR, Rapamycin and FKBP12 target 1, rapamycin associated protein FRAP2, Rapamycin target protein 1
Uniprot ID
Mouse ortholog
Mtor (56717)
serine/threonine-protein kinase mTOR (Q9JLN9)
Alternate
No data
Variants
Clinical Variant
No data
Financial
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Afinitor - Novartis
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 31,467 documents
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Safety
Black-box Warning
Black-box warning for: Everolimus, Zortress
Adverse Events
Top Adverse Reactions
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2,278 adverse events reported
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