Drug intelligence / Profile preview

aprocitentan + midazolam

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

Overview

**aprocitentan + midazolam** refers to the concomitant use of two drugs: *aprocitentan*, an orally active dual endothelin receptor antagonist (targets both ETA and ETB receptors) developed for resistant hypertension, and *midazolam*, a short-acting benzodiazepine commonly used for sedation and anesthesia. Aprocitentan acts by blocking endothelin-1-induced vasoconstriction, lowering blood pressure in adults not adequately controlled by other antihypertensive agents. Midazolam functions as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor, enhancing inhibitory neurotransmission. Clinical studies demonstrate that aprocitentan does not significantly alter the pharmacokinetics, safety, or tolerability of midazolam when co-administered[1][2][3][4].

Other names
aprocitentanmidazolam
02

Targets

CYP3A4 (Cytochrome P450 3A4)EDNRB (Endothelin receptor type B)EDNRA (Endothelin receptor type A)

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