Drug intelligence / Profile preview

ibrutinib + everolimus

Development stage
Phase 2
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

Ibrutinib + everolimus is a combination of two small molecule drugs: ibrutinib, a Bruton’s tyrosine kinase (BTK) inhibitor, and everolimus, an inhibitor of the mammalian target of rapamycin (mTOR). This combination has been investigated primarily for use in solid tumors such as advanced renal cell carcinoma (RCC) after prior therapies, as well as in preclinical and early-phase clinical studies of various cancers. - **Ibrutinib** acts by irreversibly inhibiting BTK, thereby blocking B-cell receptor signaling critical for survival and proliferation of certain malignant B-cells. - **Everolimus** inhibits mTOR, a central regulator of cell growth, metabolism, proliferation, and survival, by binding to FKBP12 and blocking mTORC1 activity. Combined, these agents target distinct but potentially complementary pathways in tumor cell survival. Preclinical studies and early clinical trials have assessed safety and efficacy, with a recommended phase 2 dosing regimen established for RCC. However, efficacy signals in clinical trials versus historical controls have not been robust, though safety is considered acceptable[2][3][5].

02

Targets

BTK (Bruton tyrosine kinase)Mechanistic target of rapamycin complex 1

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