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Everolimus

Generic Name
Everolimus
Brand Names
Afinitor, Votubia, Zortress
Drug Type
Small Molecule
Chemical Formula
C53H83NO14
CAS Number
159351-69-6
Unique Ingredient Identifier
9HW64Q8G6G

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

Published: Jul 16, 2025

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: C53​H83​NO14​ [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:

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/07/31
Not Applicable
Recruiting
2025/07/14
Not Applicable
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
8/12/2025
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
8/12/2025
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
8/12/2025
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

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

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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