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
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/07/31 | Not Applicable | Recruiting | |||
2025/07/14 | Not Applicable | Not yet recruiting | |||
2025/06/25 | Phase 2 | Recruiting | |||
2025/06/03 | Phase 1 | Not yet recruiting | Forward Pharmaceuticals Co., Ltd. | ||
2025/05/29 | Phase 1 | Not yet recruiting | Captor Therapeutics S.A. | ||
2025/04/24 | Phase 2 | Recruiting | |||
2025/04/24 | Phase 4 | Not yet recruiting | |||
2025/02/18 | Phase 1 | Not yet recruiting | |||
2025/01/23 | Phase 2 | Recruiting | |||
2024/12/10 | Phase 1 | Not yet recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Novartis Pharmaceuticals Corporation | 0078-0628 | ORAL | 5 mg in 1 1 | 1/29/2016 | |
| Mylan Pharmaceuticals Inc. | 0378-0005 | ORAL | 2 mg in 1 1 | 3/10/2022 | |
| Natco Pharma Limited | 63850-0058 | ORAL | 2.5 mg in 1 1 | 6/8/2023 | |
| Biocon Pharma Inc. | 70377-010 | ORAL | 2.5 mg in 1 1 | 6/2/2023 | |
| Novartis Pharmaceuticals Corporation | 0078-0566 | ORAL | 5 mg in 1 1 | 1/29/2016 | |
| Breckenridge Pharmaceutical, Inc. | 51991-990 | ORAL | 2 mg in 1 1 | 7/30/2025 | |
| Novartis Pharmaceuticals Corporation | 0078-0626 | ORAL | 2 mg in 1 1 | 1/29/2016 | |
| Teva Pharmaceuticals USA, Inc. | 0093-7766 | ORAL | 2.5 mg in 1 1 | 10/23/2023 | |
| Teva Pharmaceuticals USA, Inc. | 0093-7769 | ORAL | 10 mg in 1 1 | 10/23/2023 | |
| Par Pharmaceutical, Inc. | 49884-160 | ORAL | 0.75 mg in 1 1 | 4/21/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 9/2/2011 | ||
Authorised | 8/2/2009 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| CERTICAN TABLETS 0.5 MG | SIN13196P | TABLET | 0.5 MG | 4/18/2006 | |
| Afinitor Tablet 5mg | SIN13750P | TABLET | 5.00mg | 1/6/2010 | |
| CERTICAN TABLETS 0.25 MG | SIN13194P | TABLET | 0.25 MG | 4/18/2006 | |
| CERTICAN TABLETS 0.75 MG | SIN13195P | TABLET | 0.75 MG | 4/18/2006 | |
| Afinitor Tablet 10mg | SIN13749P | TABLET | 10.00mg | 1/6/2010 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| EVERCHEM TABLETS 2.5MG | N/A | N/A | N/A | 10/24/2024 | |
| EVERCHEM TABLETS 5MG | N/A | N/A | N/A | 10/24/2024 | |
| EVERCHEM TABLETS 10MG | N/A | N/A | N/A | 10/24/2024 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| TEVA-EVEROLIMUS everolimus 5 mg tablet blister pack | 277302 | Medicine | A | 4/20/2017 | |
| TEVA-EVEROLIMUS everolimus 10 mg tablet blister pack | 277304 | Medicine | A | 4/20/2017 | |
| CERTICAN everolimus 0.75mg tablet blister pack | 97509 | Medicine | A | 3/17/2005 | |
| AFINITOR everolimus 10 mg tablet blister pack | 154663 | Medicine | A | 8/6/2009 | |
| EVEROLIMUS-TEVA everolimus 10 mg tablet blister pack | 277287 | Medicine | A | 4/20/2017 | |
| CERTICAN everolimus 0.1mg dispersible tablet blister pack | 97520 | Medicine | A | 3/17/2005 | |
| CERTICAN everolimus 0.5mg tablet blister pack | 97506 | Medicine | A | 3/17/2005 | |
| EVEROLIMUS-TEVA everolimus 5 mg tablet blister pack | 277285 | Medicine | A | 4/20/2017 | |
| CERTICAN everolimus 1mg tablet blister pack | 97516 | Medicine | A | 3/17/2005 | |
| PHARMACOR EVEROLIMUS everolimus 0.5 mg tablet blister pack | 335143 | Medicine | A | 4/21/2021 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| CERTICAN | novartis pharmaceuticals canada inc | 02375923 | Tablet - Oral | 0.75 MG | N/A |
| TEVA-EVEROLIMUS | teva canada limited | 02463253 | Tablet - Oral | 10 MG | 12/6/2019 |
| PMS-EVEROLIMUS | 02504693 | Tablet - Oral | 10 MG | 9/8/2021 | |
| SANDOZ EVEROLIMUS | 02492938 | Tablet - Oral | 5 MG | 9/17/2020 | |
| REDDY-EVEROLIMUS | dr reddy's laboratories ltd | 02532409 | Tablet - Oral | 2.5 MG | 8/27/2024 |
| AFINITOR | novartis pharmaceuticals canada inc | 02339501 | Tablet - Oral | 5 MG | 3/15/2010 |
| NAT-EVEROLIMUS | natco pharma (canada) inc | 02530090 | Tablet - Oral | 2.5 MG | 4/5/2023 |
| REDDY-EVEROLIMUS | dr reddy's laboratories ltd | 02532417 | Tablet - Oral | 5 MG | 8/27/2024 |
| PMS-EVEROLIMUS | 02504677 | Tablet - Oral | 2.5 MG | 9/8/2021 | |
| PMS-EVEROLIMUS | 02504685 | Tablet - Oral | 5 MG | 9/8/2021 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| EVEROLIMUS SANDOZ 10 MG COMPRIMIDOS EFG | Sandoz Farmaceutica S.A. | 83919 | COMPRIMIDO | Diagnóstico Hospitalario | Not Commercialized |
| EVEROLIMUS TAD 5 MG COMPRIMIDOS EFG | 83527 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized | |
| EVEROLIMUS AVALON 2,5 MG COMPRIMIDOS EFG | Avalon Laboratorios S.L. | 84203 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized |
| EVEROLIMUS ETHYPHARM 10 MG COMPRIMIDOS EFG | 83479 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized | |
| CERTICAN 0,25 mg COMPRIMIDOS DISPERSABLES | Novartis Farmaceutica S.A. | 66002 | COMPRIMIDO DISPERSABLE | Diagnóstico Hospitalario | Commercialized |
| EVEROLIMUS TEVA 2,5 MG COMPRIMIDOS EFG | Teva Pharma S.L.U. | 83185 | COMPRIMIDO | Diagnóstico Hospitalario | Not Commercialized |
| EVEROLIMUS SWANPOND INVESTMENTS 5 MG COMPRIMIDOS EFG | Swan Pond Investments Limited | 85346 | COMPRIMIDO | Diagnóstico Hospitalario | Not Commercialized |
| EVEROLIMUS ETHYPHARM 2,5 MG COMPRIMIDOS EFG | 83478 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized | |
| CERTICAN 0,25 mg COMPRIMIDOS | Novartis Farmaceutica S.A. | 66001 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized |
| CERTICAN 0,75 mg COMPRIMIDOS | Novartis Farmaceutica S.A. | 66007 | COMPRIMIDO | Diagnóstico Hospitalario | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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