Effect of vepdegestrant, a PROTAC oestrogen receptor degrader, on dabigatran and rosuvastatin pharmacokinetics in healthy participants.

ABSTRACT:

Aims

To evaluate the effects of vepdegestrant, a PROteolysis TArgeting Chimera (PROTAC) oestrogen receptor degrader, on the pharmacokinetics of dabigatran (a P-glycoprotein [P-gp] substrate) and rosuvastatin (a breast cancer resistance protein [BCRP] substrate).

Methods

In two phase 1, open-label, two-period, fixed-sequence studies, healthy adult participants received a single oral dose of dabigatran etexilate 75 mg or rosuvastatin 10 mg alone and with a single dose of vepdegestrant 200 mg. Serial plasma samples were collected after dosing, and pharmacokinetic parameters for dabigatran and rosuvastatin were estimated by standard noncompartmental analysis.

Results

Coadministration of the P-gp substrate dabigatran etexilate with vepdegestrant increased dabigatran area u

SUBMITTER: Yang DZ 

PROVIDER: S-EPMC12648365 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature