Drug intelligence / Profile preview

apalutamide + gemfibrozil

Development stage
Preclinical
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

This entry refers to a **combination of apalutamide (JNJ-56021927)**, a small molecule androgen receptor inhibitor approved for treatment of non-metastatic castration-resistant prostate cancer, and **gemfibrozil**, a lipid-regulating agent primarily used to treat hyperlipidemia. - Apalutamide acts as a competitive antagonist at the androgen receptor, blocking androgen-mediated signaling and thus inhibiting growth in androgen-dependent prostate cancer cells[7]. - Gemfibrozil activates peroxisome proliferator-activated receptor alpha (PPARα), modulating the transcription of genes involved in lipid metabolism. There is evidence of important drug-drug interactions when apalutamide is combined with gemfibrozil, as gemfibrozil is a potent inhibitor of CYP2C8 and may alter the pharmacokinetics of apalutamide[1]. No approved indication exists for their use as a fixed-combination therapy; information about this combination arises primarily in the context of drug-drug interaction studies.

Brand names
Erleada
Other names
apalutamide + gemfibrozilJNJ-56021927 + gemfibrozil
02

Targets

AR (Adrenergic receptors)

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