MedPath

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.

Background

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

FDA Approved Products

Zortress
Manufacturer:Novartis Pharmaceuticals Corporation
Route:ORAL
Strength:0.75 mg in 1 1
Approved: 2018/08/10
NDC:0078-0415
Everolimus
Manufacturer:Natco Pharma Limited
Route:ORAL
Strength:0.75 mg in 1 1
Approved: 2023/06/08
NDC:63850-0064
Everolimus
Manufacturer:Natco Pharma Limited
Route:ORAL
Strength:0.5 mg in 1 1
Approved: 2023/06/08
NDC:63850-0063
Everolimus
Manufacturer:Natco Pharma Limited
Route:ORAL
Strength:0.25 mg in 1 1
Approved: 2023/06/08
NDC:63850-0062
Everolimus
Manufacturer:Par Pharmaceutical, Inc.
Route:ORAL
Strength:0.5 mg in 1 1
Approved: 2022/04/21
NDC:49884-159

Singapore Approved Products

CERTICAN TABLETS 0.5 MG
Manufacturer:NOVARTIS PHARMA STEIN AG, Lek Pharmaceuticals d.d. (DP Intermediate Manufacturer)
Form:TABLET
Strength:0.5 MG
Online:Yes
Approved: 2006/04/18
Approval:SIN13196P
Afinitor Tablet 5mg
Manufacturer:Novartis Pharma Stein AG, Lek Pharmaceuticals d.d. (drug product intermediate manufacturer), Novartis Pharma AG (drug product intermediate manufacturer)
Form:TABLET
Strength:5.00mg
Online:Yes
Approved: 2010/01/06
Approval:SIN13750P
CERTICAN TABLETS 0.25 MG
Manufacturer:NOVARTIS PHARMA STEIN AG, Lek Pharmaceuticals d.d. (DP Intermediate Manufacturer)
Form:TABLET
Strength:0.25 MG
Online:Yes
Approved: 2006/04/18
Approval:SIN13194P
CERTICAN TABLETS 0.75 MG
Manufacturer:NOVARTIS PHARMA STEIN AG, Lek Pharmaceuticals d.d. (DP Intermediate Manufacturer)
Form:TABLET
Strength:0.75 MG
Online:Yes
Approved: 2006/04/18
Approval:SIN13195P
Afinitor Tablet 10mg
Manufacturer:Novartis Pharma Stein AG, Lek Pharmaceuticals d.d. (drug product intermediate manufacturer), Novartis Pharma AG (drug product intermediate manufacturer)
Form:TABLET
Strength:10.00mg
Online:Yes
Approved: 2010/01/06
Approval:SIN13749P

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