Drug intelligence / Profile preview

rilpivirine + digoxin

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This combination refers to the co-administration of **rilpivirine (TMC278)** and **digoxin**. Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated for the treatment of HIV-1 infection. It inhibits HIV-1 replication by binding to reverse transcriptase and blocking the conversion of viral RNA into DNA. Digoxin is a cardiac glycoside used to manage heart failure and atrial fibrillation; it increases myocardial contractility by inhibiting the sodium–potassium adenosine triphosphatase (Na+/K+-ATPase), resulting in increased intracellular calcium in myocardial tissue. Neither is formulated as a fixed-dose combination; the interest lies in their pharmacokinetic interaction, where rilpivirine may act as a weak inhibitor of P-glycoprotein, potentially leading to mild increases in digoxin exposure, but not requiring dose modification under normal circumstances.

Brand names
EdurantLanoxin
Other names
TMC278TMC-278TMC 278rilpivirine hydrochlorideEdurantdigoxinLanoxin
02

Targets

ABCB1 (P-glycoprotein)

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