Drug intelligence / Profile preview

tofacitinib + midazolam

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

Overview

A **combination of tofacitinib**, an oral Janus kinase inhibitor used primarily in the treatment of rheumatoid arthritis and other autoimmune conditions, and **midazolam**, a short-acting benzodiazepine used for sedation, anesthesia, and the treatment of acute seizures. This combination is not a marketed pharmaceutical product; rather, it is used in clinical pharmacokinetic drug–drug interaction studies. Tofacitinib does **not significantly affect the pharmacokinetics of midazolam**, indicating a lack of clinically relevant CYP3A4 inhibition or induction. Both drugs are small molecules: tofacitinib works by inhibiting Janus kinases (mainly JAK1 and JAK3), which downregulates immune signaling, while midazolam acts as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor to enhance inhibitory neurotransmission[1].

Brand names
tofacitinib + midazolam
Other names
tofacitinib plus midazolam
02

Targets

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