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Afinitor (everolimus)

Novartis · FDA-approved active Quality 67/100

Afinitor works by blocking the mTOR protein, which is involved in cell growth and division.

Afinitor (everolimus) is a kinase inhibitor small molecule developed by Novartis that targets the serine/threonine-protein kinase mTOR. It is used to treat various conditions, including kidney and breast cancers, as well as a rare brain tumor associated with Tuberous Sclerosis. Afinitor is off-patent and has multiple generic manufacturers. It has been FDA-approved since 2009 for several indications. As a commercial product, it is available in the market with various generic options.

At a glance

Generic nameeverolimus
SponsorNovartis
Drug classKinase Inhibitor [EPC]
TargetSerine/threonine-protein kinase mTOR
Therapeutic areaOncology
PhaseFDA-approved
First approval2009
Annual revenue600

Mechanism of action

Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC). Everolimus binds to an intracellular protein, FKBP-12, resulting in an inhibitory complex formation with mTOR complex (mTORC1) and thus inhibition of mTOR kinase activity. Everolimus reduced the activity of S6 ribosomal protein kinase (S6K1) and eukaryotic initiation factor 4E-binding protein (4E-BP1), downstream effectors of mTOR, involved in protein synthesis. S6K1 is substrate of mTORC1 and phosphorylates the activation domain of the estrogen receptor which results in ligand-independent activation of the receptor. In addition, everolimus inhibited the expression of hypoxia-inducible factor (e.g., HIF-1) and reduced the expression of vascular endothelial growth factor (VEGF). Inhibition of mTOR by everolimus has been shown to reduce c

Approved indications

Common side effects

Drug interactions

Key clinical trials

Patents

PatentExpiryType
90062242028-07-01Method of Use
84101312025-11-01Method of Use
8410131*PED2026-05-01Compound

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity
SEC EDGARRevenue + earnings