Drug intelligence / Profile preview

taletrectinib + digoxin

Development stage
Unknown
Lead developer
Nuvation Bio
Modality
Small Molecules
Administration
Oral
01

Overview

**Taletrectinib + digoxin** is a combination regimen composed of taletrectinib (AB-106), a small molecule kinase inhibitor targeting oncogenic drivers C-ros oncogene 1 (ROS1) and neurotrophic tyrosine receptor kinase (NTRK), and digoxin, a cardiac glycoside primarily indicated for heart failure and atrial fibrillation. Taletrectinib has demonstrated antineoplastic activity via inhibition of ROS1 and NTRK1/2/3, leading to interruption of proliferative signaling in cancers such as solid tumors with NTRK fusion genes. Digoxin acts by inhibiting Na+/K+ ATPase, thereby increasing intracellular calcium and enhancing cardiac contractility. Recent clinical pharmacology studies have investigated the drug-drug interaction between taletrectinib (AB-106) and digoxin, due to digoxin being a classic substrate of P-glycoprotein (P-gp), and the potential for taletrectinib to affect digoxin’s pharmacokinetics[5]. Combination therapy of P-gp substrates (such as digoxin) with kinase inhibitors may alter digoxin exposure, requiring clinical monitoring.

Brand names
Ibtrozi
Other names
AB-106 + digoxintaletrectinib + digoxin
02

Targets

NTRK2 (Tropomyosin-related kinase receptor type B)ABCB1 (P-glycoprotein)NTRK1 (Tropomyosin-related receptor kinase A)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK3 (Tropomyosin receptor kinase C)

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