Everolimus
Everolimus was first approved by Swiss Agency for therapeutic products，Swissmedic on July 18, 2003, then approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on April 23, 2004, and approved by the U.S. Food and Drug Administration (FDA) on Mar 30, 2009, approved by European Medicine Agency (EMA) on Aug 3, 2009. It was developed and marketed as Certican® by Novartis in SE.
Everolimus is an inhibitor of mammalian target of rapamycin (mTOR). It is indicated for the treatment of renal cell cancer and other tumours and currently used as an immunosuppressant to prevent rejection of organ transplants.
Certican® is available as tablet for oral use, containing 0.25, 0.5 or 0.75 mg of free Everolimus. The recommended dose is 10 mg once daily with or without food for advanced HR+ breast cancer, advanced progressive neuroendocrine tumors, advanced renal cell carcinoma or renal angiomyolipoma with tuberous sclerosis complex.
Update Date：2016-06-03
- Drug Name：
- Everolimus
- Research Code：
- RAD-001; SDZ-RAD
- Trade Name：
- Certican® / Zortress® / Afinitor®
- MOA：
- mTOR inhibitor
- Indication：
- Rejection of organ transplantation; Renal cell carcinoma; Advanced renal cell carcinoma (RCC); Advanced breast cancer; Pancreatic cancer; Renal angiomyolipoma; Tuberous sclerosis complex (TSC); Rejection in heart transplantation; Rejection of suppression renal transplantation; Subependymal giant cell astrocytoma; neuroendocrine tumors (NET); Advanced gastrointestinal tumors
- Status：
- Approved
- Company：
- Novartis (Originator)
- Sales：
-
$1,942 Million (Y2015);
$1,902 Million (Y2014);
$1,558 Million (Y2013);
$1,007 Million (Y2012);
$630 Million (Y2011); - ATC Code：
- L04AA18
Update Date：2016-06-03
| Approval Date | Approval Type | Trade Name | Indication | Dosage Form | Strength | Company | Review Classification |
|---|---|---|---|---|---|---|---|
| 2012-08-29 | New dosage form | Afinitor Disperz | Renal cell carcinoma , Advanced breast cancer, Pancreatic cancer, Renal angiomyolipoma, Tuberous sclerosis complex (TSC) | Tablet, For suspension | 2 mg/3 mg/5 mg | Novartis | Priority |
| 2010-04-20 | New strength | Zortress | Advanced renal cell carcinoma (RCC) | Tablet | 0.25 mg/0.5 mg/0.75 mg | Novartis | |
| 2009-03-30 | Marketing approval | Afinitor | Advanced renal cell carcinoma (RCC) | Tablet | 2.5 mg/5 mg/7.5 mg/10 mg | Novartis | Priority |
| Approval Date | Approval Type | Trade Name | Indication | Dosage Form | Strength | Company | Review Classification |
|---|---|---|---|---|---|---|---|
| 2016-06-02 | New indication | Afinitor | neuroendocrine tumors (NET), Advanced gastrointestinal tumors | Tablet | Novartis | ||
| 2011-09-02 | Marketing approval | Votubia | Advanced breast cancer, Renal cell carcinoma , Pancreatic cancer | Tablet | 2.5 mg/5 mg/10 mg | Novartis | Orphan; Conditional Approval |
| 2011-09-02 | Marketing approval | Votubia | Advanced breast cancer, Renal cell carcinoma , Pancreatic cancer | Tablet, Orally disintegrating | 2 mg/3 mg/5 mg | Novartis | Orphan; Conditional Approval |
| 2009-08-03 | Marketing approval | Afinitor | Advanced breast cancer, Renal cell carcinoma , Pancreatic cancer | Tablet | 2.5 mg/5 mg/10 mg | Novartis |
| Approval Date | Approval Type | Trade Name | Indication | Dosage Form | Strength | Company | Review Classification |
|---|---|---|---|---|---|---|---|
| 2011-12-22 | New indication | Certican | Rejection of suppression renal transplantation | Tablet | 0.25 mg/0.5 mg/0.75 mg | Novartis | |
| 2007-01-26 | Marketing approval | Certican | Rejection in heart transplantation | Tablet | 0.25 mg/0.5 mg/0.75 mg | Novartis |
| Approval Date | Approval Type | Trade Name | Indication | Dosage Form | Strength | Company | Review Classification |
|---|---|---|---|---|---|---|---|
| 2014-02-13 | Marketing approval | 飞尼妥/Afinitor | Advanced renal cell carcinoma (RCC), Subependymal giant cell astrocytoma | Tablet | 2.5 mg | Novartis | |
| 2013-01-22 | Marketing approval | 飞尼妥/Afinitor | Advanced renal cell carcinoma (RCC), Subependymal giant cell astrocytoma | Tablet | 10 mg | Novartis | |
| 2013-01-22 | Marketing approval | 飞尼妥/Afinitor | Advanced renal cell carcinoma (RCC), Subependymal giant cell astrocytoma | Tablet | 5 mg | Novartis |
| Approval Date | Approval Type | Trade Name | Indication | Dosage Form | Strength | Company | Review Classification |
|---|---|---|---|---|---|---|---|
| 2003-07-18 | Marketing approval | Certican | Rejection of organ transplantation, Renal cell carcinoma | Tablet | 0.25 mg/0.5 mg/0.75 mg | Novartis |
Update Date：2015-08-27
|
Molecular Weight | 958.22 | ||||||||||||
| Formula | C53H83NO14 | |||||||||||||
| CAS No. | 159351-69-6 (Everolimus); | |||||||||||||
| Chemical Name | (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-Dihydroxy-12-{(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]-1-methylethyl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentaone | |||||||||||||
| Everolimus （Free Acid/Base）Parameters： | ||||||||||||||
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| *：Calculated by ACD/Labs software V11.02. | ||||||||||||||
Update Date：2016-01-07
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