Drug intelligence / Profile preview

nemtabrutinib + digoxin

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Nemtabrutinib + digoxin is a drug combination primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions (DDI). Nemtabrutinib (MK-1026, formerly ARQ 531) is an investigational, orally bioavailable, reversible, non-covalent inhibitor of Bruton's tyrosine kinase (BTK), including the C481S mutant form, developed by Merck & Co. (MSD) following the acquisition of ArQule. Digoxin is a cardiac glycoside that serves as a sensitive probe substrate for the P-glycoprotein (P-gp/ABCB1) efflux transporter. The combination is studied to assess whether nemtabrutinib acts as an inhibitor of P-gp, which could alter the pharmacokinetics of co-administered P-gp substrates like digoxin.

Other names
nemtabrutinib and digoxinMK-1026 and digoxinMK1026 and digoxinMK 1026 and digoxin
02

Targets

NF-κBATP1A (Sodium/potassium-transporting ATPase)HIF1A (Hypoxia-inducible factor 1-alpha)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BTK (Bruton tyrosine kinase)

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