Drug intelligence / Profile preview

nirogacestat + famotidine

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

Overview

This is a combination of **nirogacestat**, an oral, selective small molecule gamma-secretase inhibitor indicated for the treatment of progressing desmoid tumors, and **famotidine**, an oral and parenteral histamine H2 receptor antagonist used for a variety of gastric acid-related disorders. The combination is not a fixed-dose combination product but rather represents the concurrent administration of two distinct drugs, sometimes used in clinical pharmacokinetic (PK) interaction studies. Nirogacestat inhibits gamma-secretase, thereby blocking proteolytic activation of the Notch receptor, which is implicated in desmoid tumor growth. Famotidine competitively antagonizes the histamine H2 receptor, thus inhibiting gastric acid secretion. In clinical research, famotidine is administered to investigate its effects on the pharmacokinetics of nirogacestat, particularly since H2 blockers can alter absorption of other drugs by increasing gastric pH[1][2][3][5].

02

Targets

GSEC (Gamma-Secretase Complex)HRH2 (Histamine H2 Receptor)

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