OATP1B-type Transport Function Is a Determinant of Aromatase Inhibitor-Associated Arthralgia Susceptibility.

ABSTRACT:

Abstract

Aromatase inhibitors (AI) such as anastrozole, letrozole, and exemestane are used as adjuvant treatment for postmenopausal women with hormone receptor–positive breast cancer. The interindividual pharmacokinetic variability seen with AIs is extensive, and this phenomenon may have important ramification for AI-associated arthralgia, a common toxicity of which the etiology remains unclear. We speculated that hepatic uptake transporters involved in the elimination of AIs play a crucial role in explaining this pharmacologic variability. Using an array of in silico, in vitro, in vivo, and human studies, we identified OATP1B1 and OATP1B3 (in humans) as well as the murine ortholog Oatp1b2 as transporters that regulate the initial step in the elimination of AIs. Genetic deficiency

SUBMITTER: Taheri H 

PROVIDER: S-EPMC11948302 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature