Overview
Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.
Indication
Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole. Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.
Associated Conditions
- Heart Transplant Rejection
- Kidney Transplant Rejection
- Liver Transplant Rejection
- Progressive Neuroendocrine Tumors of pancreatic origin
- Renal angiomyolipoma, tuberous sclerosis complex
- Subependymal giant cell astrocytoma, tuberous sclerosis complex
- Waldenstrom's Macroglobulinemia Refractory
- Advanced Carcinoid tumor
- Locally advanced Progressive Neuroendocrine Tumors of gastrointestinal origin
- Locally advanced lung origin Progressive Neuroendocrine Tumors
- Metastatic gastrointestinal origin Progressive Neuroendocrine Tumors
- Metastatic lung origin Progressive Neuroendocrine Tumors
- Refractory Advanced Renal Cell Carcinoma
- Refractory, advanced Breast cancer
- Unresectable gastrointestinal origin Progressive Neuroendocrine Tumors
- Unresectable lung origin Progressive Neuroendocrine Tumors
Research Report
Everolimus (DB01590): A Comprehensive Monograph on its Pharmacology, Clinical Applications, and Safety Profile
Introduction and Drug Profile
Overview and Identification
Everolimus is a seminal small molecule drug, a derivative of sirolimus, that functions as a potent and selective inhibitor of the mammalian target of rapamycin (mTOR) kinase, a central regulator of cellular growth, proliferation, and metabolism.[1] This compound occupies a unique position in modern pharmacotherapy, embodying a dual identity as both a targeted antineoplastic agent and a critical immunosuppressant in the context of solid organ transplantation.[3] Its development and application highlight the therapeutic potential of modulating fundamental cellular signaling pathways. The clinical utility of everolimus spans a diverse range of conditions, from advanced cancers of the breast, kidney, and neuroendocrine system to the prevention of organ rejection and the management of benign tumors in the genetic disorder tuberous sclerosis complex. This monograph provides a comprehensive analysis of its chemical properties, pharmacological profile, clinical efficacy, and safety considerations, offering a detailed perspective on its role in contemporary medicine.
Key Identifiers:
- DrugBank ID: DB01590 [5]
- CAS Number: 159351-69-6 [6]
- Type: Small Molecule [5]
- Molecular Formula: C53H83NO14 [6]
- Molecular Weight: 958.22 g/mol [6]
- Harmonized System (HS) Code: 294190 [7]
- RTECS Number: VE6255000 [9]
Synonyms and Commercial Formulations
To ensure clarity in clinical and research settings, it is essential to recognize the various nomenclatures for everolimus. Its chemical and research synonyms reflect its structure as a rapamycin derivative, while its commercial brand names are deliberately segregated by therapeutic area—a critical strategy to ensure patient safety.
Chemical and Research Synonyms:
Clinical Trials
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Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2023/11/13 | Phase 2 | Recruiting | Central Hospital, Nancy, France | ||
2023/10/27 | Phase 2 | Active, not recruiting | |||
2023/08/09 | Phase 2 | Recruiting | |||
2023/07/20 | Phase 3 | Recruiting | |||
2023/07/18 | Phase 1 | Recruiting | |||
2023/07/18 | Phase 2 | Recruiting | |||
2023/07/06 | Phase 2 | Recruiting | |||
2023/06/26 | Phase 3 | Recruiting | Grupo Espanol de Tumores Neuroendocrinos | ||
2023/05/06 | Phase 2 | Recruiting | |||
2023/05/01 | Phase 2 | Recruiting |
FDA Drug Approvals
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Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Mylan Pharmaceuticals Inc. | 0378-0006 | ORAL | 3 mg in 1 1 | 3/10/2022 | |
| Ascend Laboratories, LLC | 67877-721 | ORAL | 1 mg in 1 1 | 12/21/2021 | |
| Novartis Pharmaceuticals Corporation | 0078-0627 | ORAL | 3 mg in 1 1 | 1/29/2016 | |
| Ascend Laboratories, LLC | 67877-718 | ORAL | 0.25 mg in 1 1 | 12/21/2021 | |
| Novartis Pharmaceuticals Corporation | 0078-0414 | ORAL | 0.5 mg in 1 1 | 8/10/2018 | |
| Natco Pharma Limited | 63850-0064 | ORAL | 0.75 mg in 1 1 | 6/8/2023 | |
| Mylan Pharmaceuticals Inc. | 0378-3096 | ORAL | 2.5 mg in 1 1 | 10/15/2023 | |
| Breckenridge Pharmaceutical, Inc. | 51991-380 | ORAL | 0.5 mg in 1 1 | 12/31/2023 | |
| Teva Pharmaceuticals USA, Inc. | 0093-7767 | ORAL | 5 mg in 1 1 | 10/23/2023 | |
| Hikma Pharmaceuticals USA Inc. | 0054-0481 | ORAL | 5 mg in 1 1 | 5/13/2022 |
EMA Drug Approvals
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Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
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|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
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|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
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Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
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| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
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Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| AFINITOR everolimus 5 mg dispersible tablet blister pack | 200205 | Medicine | A | 8/28/2013 | |
| EVEROLIMUS-TEVA everolimus 2.5 mg tablet blister pack | 277284 | Medicine | A | 4/20/2017 | |
| EVEROCAN everolimus 0.25 mg tablet blister pack | 335146 | Medicine | A | 4/21/2021 | |
| AFINITOR everolimus 3 mg dispersible tablet blister pack | 200204 | Medicine | A | 8/28/2013 | |
| TEVA-EVEROLIMUS everolimus 2.5 mg tablet blister pack | 277301 | Medicine | A | 4/20/2017 | |
| EVEROCAN everolimus 0.75 mg tablet blister pack | 335142 | Medicine | A | 4/21/2021 | |
| PHARMACOR EVEROLIMUS everolimus 1 mg tablet bottle pack | 335147 | Medicine | A | 4/21/2021 | |
| AFINITOR everolimus 2.5 mg tablet blister pack | 177648 | Medicine | A | 1/30/2012 | |
| EVEROCAN everolimus 1 mg tablet bottle pack | 335148 | Medicine | A | 4/21/2021 |
Health Canada Drug Approvals
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Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| AFINITOR | novartis pharmaceuticals canada inc | 02369257 | Tablet - Oral | 2.5 MG | 8/5/2011 |
| TEVA-EVEROLIMUS | teva canada limited | 02463245 | Tablet - Oral | 7.5 MG | N/A |
| REDDY-EVEROLIMUS | dr reddy's laboratories ltd | 02532433 | Tablet - Oral | 10 MG | 8/27/2024 |
| REDDY-EVEROLIMUS | dr reddy's laboratories ltd | 02532425 | Tablet - Oral | 7.5 MG | N/A |
| AFINITOR DISPERZ | novartis pharmaceuticals canada inc | 02425645 | Tablet For Suspension - Oral | 2 MG | 11/28/2014 |
| NAT-EVEROLIMUS | natco pharma (canada) inc | 02530112 | Tablet - Oral | 7.5 MG | N/A |
| SANDOZ EVEROLIMUS | 02492946 | Tablet - Oral | 10 MG | 9/17/2020 | |
| SANDOZ EVEROLIMUS | 02492911 | Tablet - Oral | 2.5 MG | 9/17/2020 |
CIMA AEMPS Drug Approvals
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| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
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| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
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| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
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| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
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Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
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| No UK EMC drug information found for this drug. | |||||
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