Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases.

Abstract

Everolimus is a potent, oral inhibitor of the mammalian target of rapamycin (mTOR) that has been investigated in multiple clinical development programs since 1996. A unique collaboration between academic and pharmaceutical experts fostered research that progressed rapidly, with simultaneous indication findings across numerous tumor types. Initially developed for the prophylaxis of organ transplant rejection, everolimus has demonstrated efficacy and safety for the treatment of patients with various types of cancer (renal cell carcinoma, neuroendocrine tumors of pancreatic origin, and breast cancer) and for adult and pediatric patients with tuberous sclerosis complex. The FDA approval of everolimus for these diseases has addressed several unmet medical needs and is widely accepted by the medical community where treatment options may be limited. An extensive clinical development program is ongoing to establish the role of everolimus as monotherapy, or in combination with other agents, in the treatment of a broad spectrum of malignancies.

• Authors: David Lebwohl, Ozlem Anak, Tarek Sahmoud, Judith Klimovsky, Ingrid Elmroth, Tomas Haas, Joseph Posluszny, Stephen Saletan, William Berg
• Journal: Annals of the New York Academy of Sciences (Ann N Y Acad Sci) Vol. 1291 Pg. 14-32 (Jul 2013) ISSN: 1749-6632 [Electronic] United States
• PMID: 23659703 (Publication Type: Journal Article, Review)
• Copyright: © 2013 New York Academy of Sciences.

Chemical References

• Antineoplastic Agents
• Immunosuppressive Agents
• Everolimus
• MTOR protein, human
• TOR Serine-Threonine Kinases
• Sirolimus

Topics

• Administration, Oral
• Animals
• Antineoplastic Agents (administration & dosage, immunology)
• Clinical Trials as Topic (methods)
• Everolimus
• Humans
• Immunosuppressive Agents (administration & dosage, chemistry)
• Neoplasms (drug therapy, immunology)
• Sirolimus (administration & dosage, analogs & derivatives, immunology)
• TOR Serine-Threonine Kinases (antagonists & inhibitors, immunology)
• Tuberous Sclerosis (drug therapy, immunology)