Everolimus

INN name:	Everolimus
Lab codes:	RAD-001, SDZ RAD
Trade name:	Neoral, Sandimmun, Zortress, Certican, Afinitor, Votubia, Afinitor Disperz
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
Molecular formula:	C53H83NO14
Chemical Structure:
CAS Registry Number:	159351-69-6
Originator:	Novartis; University of Michigan Comprehensive Cancer Center
Developer:	Abbott Laboratories; Assistance Publique Hopitaux de Paris; Boston Scientific Corporation; Dana-Farber Cancer Institute; Hannover Medical School; New York University School of Medicine; Novartis; Sarcoma Alliance for Research through Collaboration; SCRI Development Innovations; University of California at San Francisco; University of Sydney; University of Texas M. D. Anderson Cancer Center; Yale University
Class:	Antineoplastics
Mechanism of Action:	B cell inhibitors; Immunosuppressants; MTOR protein inhibitors; T lymphocyte inhibitors, Growth-factor-induced cell proliferation inhibitor
WHO ATC code:	C (Cardiovascular System) C01 (Cardiac Therapy) G04 (Urologicals) L01X-E10 (Everolimus) L01X-Y (Combinations of antineoplastic agents) L04A-A18 (Everolimus) M01 (Antiinflammatory and Antirheumatic Products) N (Nervous System) N03A (Antiepileptics) R07A-X (Other respiratory system products)
EPhMRA code:	C1 (Cardiac Therapy) C6A (Other Cardiovascular Products) G4 (Urologicals) L1 (Antineoplastics) L1H (Protein Kinase Inhibitor Antineoplastics) L4X (Other Immunosuppressants) M1 (Anti-Inflammatory and Anti-Rheumatic Products) N (Nervous System) N3A (Anti-Epileptics) R7X (All Other Respiratory System Products)
FDA approval:	Yes
Clinical Trials: Indication Phase Status Cardiac Transplantation|Chronic Renal Insufficiency Phase 4 Active, not recruiting Chronic Allograft Dysfunction in Renal Transplantation Phase 4 Completed Chronic Rejection of Cardiac Transplant Phase 4 Completed Chronic Renal Failure (CRF)|Graft Failure|Transplant; Failure, Kidney|Renal Transplant Rejection Phase 4 Recruiting Delayed Function of Renal Transplant Phase 4 Recruiting Disorder Related to Renal Transplantation|Exercise, Aerobic|Muscle Strength Phase 4 Terminated Heart Transplantation Phase 4 Completed HIV|Kidney Transplant|Liver Transplant Phase 4 Not yet recruiting Kidney Diseases|Heart Transplantation Phase 4 Active, not recruiting Kidney Transplantation Phase 4 Completed Left Ventricular Hypertrophy Phase 4 Recruiting Metastatic Renal Cell Carcinoma Phase 4 Completed Metastatic Renal Cell Carcinoma|Failure of Exactly One Prior VEGF-targeted Therapy Phase 4 Recruiting Plexiform Neurofibroma Associated With Neurofibromatosis Type 1 Phase 4 Completed Renal Cell Carcinoma Phase 4 Not yet recruiting Renal Transplantation Phase 4 Completed Transplantation, Homologous|Immunosuppression Phase 4 Recruiting Cardiac Transplantation|Skin Cancer Phase 3 Active, not recruiting Coronary Artery Disease|Coronary Restenosis Phase 3 Recruiting De Novo Renal Transplantation Phase 3 Completed Graft Rejection Phase 3 Completed Kidney Failure, Chronic Phase 3 Terminated Metastatic Breast Cancer Phase 3 Terminated Polycystic Kidney Diseases Phase 2|Phase 3 Terminated Advanced Gastric Cancer Phase 2 Completed Bladder Cancer|Metastatic Transitional Cell Carcinoma Phase 2 Active, not recruiting Breast Cancer Phase 2 Completed Breast Cancer|Triple Negative Breast Cancer Phase 2 Recruiting Carcinoma|Neuroendocrine|Non Functioning Neuroendocrine Tumors/NET|Non Syndromic Neuroendocrine Tumors/NET|Carcinoids|Non Functioning Phase 2 Active, not recruiting Cholangiocarcinoma Phase 2 Active, not recruiting Clear-cell Renal Carcinoma|Clear-cell Metastatic Renal Cell Carcinoma Phase 2 Recruiting Condition After Allogenic Peripheral Stem Cell Transplantation (SCT) Phase 2 Recruiting Cutaneous T-Cell Lymphoma Phase 2 Recruiting Endometrial Cancer Phase 2 Completed Epilepsy|Tuberous Sclerosis Complex|Focal Cortical Dysplasia Phase 2 Recruiting Estrogen Receptor-positive Breast Cancer|Gastrinoma|Glucagonoma|HER2-negative Breast Cancer|Insulinoma|Mucositis|Oral Complications|Pancreatic Polypeptide Tumor|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Recurrent Islet Cell Carcinoma|Recurrent Renal Cell Cancer|Somatostatinoma|Stage III Renal Cell Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Stage IV Renal Cell Cancer Phase 2 Recruiting Gastrointestinal Tumors|Pancreatic Tumors|Gastrointestinal Neuroendocrine Tumors|Pancreatic Neuroendocrine Tumors Phase 2 Recruiting Germ Cell Tumor Phase 2 Recruiting Head and Neck Cancer Phase 2 Recruiting Kaposi Sarcoma Phase 2 Terminated Kidney Cancer Phase 2 Recruiting Leukemia|Lymphoma|Lymphoproliferative Disorder Phase 2 Completed Liver Failure|Liver Diseases|Liver Cirrhosis|Liver Neoplasms Phase 2 Recruiting Lymphoma Phase 2 Terminated Malignant Mesothelioma Phase 2 Active, not recruiting Malignant Pleural Mesothelioma Phase 2 Completed Marginal Zone B-cell Lymphoma Phase 2 Completed Melanoma (Skin) Phase 2 Completed Melanoma|TOR Serine-Threonine Kinases|Neoplasm Metastasis Phase 2 Recruiting Neoplasms Phase 2 Recruiting Neurofibromatosis 1 Phase 2 Recruiting Pediatric Recurrent Progressive Low-grade Gliomas|Pediatric Progressive Low-grade Gliomas Phase 2 Recruiting Peutz-Jeghers Syndrome Phase 2 Terminated Peutz-Jeghers Syndrome|Neoplastic Processes|Neoplasm Metastasis Phase 2 Withdrawn Prostate Cancer Phase 2 Active, not recruiting Recurrent Childhood Ependymoma Phase 2 Recruiting Refractory or Relapsed Osteosarcoma Phase 2 Recruiting Refractory or Relapsed RMS and Soft Tissue Sarcomas Phase 2 Recruiting Renal Cancer|Chromophobe Renal Cell Carcinoma|Birt-Hogg-Dube Syndrome Phase 2 Recruiting Renal Cell Carcinoma|Renal Cancer Phase 2 Active, not recruiting Solid Tumor Phase 2 Recruiting Sturge Weber Syndrome Phase 2 Recruiting Testicular Cancer|Germ Cell Cancer Phase 2 Completed Thymoma and Thymic Carcinoma Phase 2 Active, not recruiting TSC1|TSC2|Tuberous Sclerosis Complex|MTOR Phase 2 Recruiting Uveitis Phase 2 Completed Advanced or Metastatic Pancreatic Adenocarcinoma Phase 1|Phase 2 Completed Carcinoma, Neuroendocrine Phase 1|Phase 2 Not yet recruiting Epilepsy|Tuberous Sclerosis Complex Phase 1|Phase 2 Active, not recruiting Metastatic Renal Cell Cancer Phase 1|Phase 2 Recruiting Tuberous Sclerosis|Subependymal Giant Cell Astrocytoma Phase 1|Phase 2 Completed Graft Versus Host Disease Phase 1 Terminated Hepatic Insufficiency Phase 1 Completed Locally Advanced Cervical Cancer Phase 1 Completed Non-Hodgkin's Lymphoma Phase 1 Completed Non-small Cell Lung Cancer|Locally Advanced Disease Phase 1 Recruiting Small-Cell Lung Cancer Phase 1 Completed Tumors|Brain Tumors|Rhabdomyosarcoma|Sarcoma, Soft Tissue Phase 1 Completed Carcinoma, Renal Cell Active, not recruiting End Stage Renal Failure With Renal Transplant Terminated Unspecified Adult Solid Tumor, Protocol Specific Recruiting
Product Patent Expiry: USA March 2020* South Korea December 2014* Canada September 2013 Japan September 2018* * Patent expiry including patent term extension It is possible to extend the term of a patent in USA, KR and JP. The extension granted at the time of writing this post has been included and marked with *. Please leave a comment below for any update.
Sales of the product (Source: From company report): Years Sales* 2009 215 2010 240 2011 256 2012 256 2013 247 2014 205 *USD millions
Recent activities on the drug: