Drug intelligence / Profile preview

nirogacestat + cocktail of CYP specific probe substrates

Development stage
Unknown
Lead developer
SpringWorks Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Nirogacestat + cocktail of CYP specific probe substrates refers to a drug combination used in a Phase 1 clinical trial conducted by SpringWorks Therapeutics to evaluate the drug-drug interaction potential of nirogacestat. Nirogacestat (brand name OGSIVEO) is an oral, selective, small molecule gamma secretase inhibitor that prevents the cleavage of transmembrane proteins, including Notch and BCMA, which are involved in tumor growth and survival. The cocktail consists of five specific probe substrates: bupropion (CYP2B6), repaglinide (CYP2C8), flurbiprofen (CYP2C9), omeprazole (CYP2C19), and midazolam (CYP3A4). This study was designed to determine if multiple doses of nirogacestat induce these cytochrome P450 enzymes in healthy adult males by measuring the pharmacokinetics of the probe substrates.

Brand names
OGSIVEO
Other names
nirogacestat + bupropion + repaglinide + flurbiprofen + omeprazole + midazolam
02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP2C19 (Cytochrome P450 2C19)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP1A2 (Cytochrome P450 1A2)GSEC (Gamma-Secretase Complex)CYP2B6 (Cytochrome P450 2B6)CYP2C8 (Cytochrome P450 2C8)

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