Drug intelligence / Profile preview

rilpivirine + metformin

Development stage
Phase 1
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

**rilpivirine + metformin** is a combination of two pharmaceutical drugs: rilpivirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI) used primarily as part of antiretroviral therapy for HIV-1 infection, and metformin, a biguanide commonly used for the treatment of type 2 diabetes mellitus. Rilpivirine acts by binding to and inhibiting the reverse transcriptase enzyme of HIV-1, thereby preventing viral replication in infected cells. Metformin lowers blood glucose levels mainly by decreasing hepatic glucose production and increasing insulin sensitivity in peripheral tissues. There is no evidence of a marketed fixed-dose combination product with these two agents; this entry refers to their co-administration. Rilpivirine is metabolized predominantly by CYP3A4, while metformin is primarily renal excreted unchanged. Drug-drug interaction studies show no clinically significant pharmacokinetic interaction between rilpivirine and metformin, meaning that their combined use does not generally require dose adjustment for either drug[3]. Both drugs have additional safety profiles: rilpivirine is associated with the risk of QT interval prolongation, and metformin can cause gastrointestinal side effects and, rarely, lactic acidosis.

02

Targets

ABCG2 (Breast cancer resistance protein)Human immunodeficiency virus type 1 reverse transcriptaseOCT1 (Organic cation transporter 1)OCT2 (Organic cation transporter 2)AMPK (Adenosine monophosphate–activated protein kinase)ND1 (Mitochondrial electron transport chain complex I)

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