Overview

Generic Name(s):
everolimus
Trade Name(s):
Afinitor
NCI Definition [1]:
A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. (NCI05)

Biomarker-Directed Therapies

Everolimus has been investigated in 84 clinical trials, of which 61 are open and 23 are closed. Of the trials investigating everolimus, 3 are early phase 1 (3 open), 22 are phase 1 (16 open), 12 are phase 1/phase 2 (9 open), 35 are phase 2 (23 open), 10 are phase 3 (8 open), and 2 are no phase specified (2 open).

HER2 Deficient Expression, HER2 Negative, and ER Positive are the most frequent biomarker inclusion criteria for everolimus clinical trials.

Breast carcinoma, malignant solid tumor, and clear cell renal cell carcinoma are the most common diseases being investigated in everolimus clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Everolimus
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Everolimus
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating everolimus and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,931 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
rad001, Afinitor, everolimus [chemical/ingredient], 40-o-(2-hydroxyethyl)-rapamycin, 42-o-(2-hydroxy)ethyl rapamycin, everolimus, 001, rad, rad 001, sdz-rad, zortress, 42-o-(2-hydroxy)ethyl rapamycin, everolimus (substance), certican, (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, votubia, everolimus (product), rad, sdz, sdz rad, everolimus
Drug Categories [2]:
Allosteric mTORC1 inhibitors
Drug Target(s) [2]:
FKBP1A, MTOR
NCIT ID [1]:
C48387
SNOMED ID [1]:
F-621F3

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.