Gamma Secretase Inhibitors and Modulators

Gamma Secretase Inhibitors and Modulators
Accession Number

Agents that suppress GAMMA-SECRETASE by inhibiting or modulating its activities. Targeted enzymatic activities include its involvement in accumulation of toxic AMYLOID BETA-PEPTIDES (e.g., Aβ42) in ALZHEIMER DISEASE and activation of NOTCH RECEPTOR mediated SIGNAL PATHWAYS in certain cancer types.

DrugDrug Description
E-2012Investigated for use/treatment in alzheimer's disease.
AvagacestatAvagacestat has been investigated for the basic science and treatment of Alzheimer Disease.
NirogacestatA gamma-secretase inhibitor used to treat desmoid tumors
BegacestatBegacestat has been used in trials studying the treatment and basic science of Alzheimer Disease.
SemagacestatSemagacestat has been used in trials studying the treatment of Alzheimer Disease.
MK-0752Mk 0752 is under investigation in clinical trial NCT00572182 (MK0752 in Treating Young Patients With Recurrent or Refractory CNS Cancer).
BMS-986115BMS-986115 has been used in trials studying the treatment of Various Advanced Cancer.
TarenflurbilInvestigated for use/treatment in alzheimer's disease and prostate cancer.
RG-4733Ro4929097 has been used in trials studying the treatment of Sarcoma, LYMPHOMA, Neoplasms, Wilm's Tumor, and OSTEOSARCOMA, among others.
ItanapracedNot Annotated
MRK-003MRK-003 is a potent and selective γ-secretase inhibitor developed by Merck. It is the preclinical analog of MK-0752, a drug in clinical development.
Drugs & Drug Targets
E-2012Gamma-secretase subunit APH-1Atarget
E-2012Gamma-secretase subunit PEN-2target
NirogacestatCytochrome P450 3A4enzyme
NirogacestatCytochrome P450 2C9enzyme
NirogacestatCytochrome P450 2C19enzyme
NirogacestatCytochrome P450 2D6enzyme
NirogacestatCytochrome P450 2B6enzyme
NirogacestatSerum albumincarrier
Nirogacestatalpha1-acid glycoproteincarrier
NirogacestatP-glycoprotein 1transporter
NirogacestatCytochrome P450 2C8enzyme
MK-0752Gamma-secretase subunit APH-1Atarget
TarenflurbilNF-kappa-B essential modulatortarget