General Information of Drug (ID: DMUR49N)

Drug Name
Begacestat Drug Info
Synonyms GSI-953; PF-05212362; PF-5212362; WAY-201953; WAY-210953
Indication
Disease Entry ICD 11 Status REF
Alzheimer disease 8A20 Phase 1 [1]
Cross-matching ID
PubChem CID
11269353
CAS Number
CAS 769169-27-9
TTD Drug ID
DMUR49N

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Gamma-secretase (GS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nirogacestat DMUP5Z0 Desmoid tumour 2F7C Approved [3]
(S)-FLURBIPROFEN DMF2O4T Myalgia FB56.2 Preregistration [4]
AMG 386 DMQJXL4 Breast cancer 2C60-2C65 Phase 3 [5]
Semagacestat DML83IW Parkinson disease 8A00.0 Phase 3 [6]
R-flurbiprofen DMFIVSR N. A. N. A. Phase 2 [4]
MK-0752 DMLTAES Alzheimer disease 8A20 Phase 2 [7]
BMS-708163 DM51LTG Alzheimer disease 8A20 Phase 2 [8]
CHF-5074 DMTE071 Alzheimer disease 8A20 Phase 2 [9]
RO-4929097 DMXA6B3 Breast cancer 2C60-2C65 Phase 2 [10]
AL102 DMCTWIB Desmoid tumour 2F7C Phase 2 [11]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Gamma-secretase (GS) TT9W8GU APH1A_HUMAN; APH1B_HUMAN; PEN2_HUMAN; NICA_HUMAN; PSN1_HUMAN Modulator [2]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6979).
2 Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608.
3 Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.J Pharmacol Exp Ther.2010 Jul;334(1):269-77.
4 The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2219-23.
5 Clinical pipeline report, company report or official report of Roche (2009).
6 A phase 3 trial of semagacestat for treatment of Alzheimer's disease. N Engl J Med. 2013 Jul 25;369(4):341-50.
7 Determination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52.
8 Safety and tolerability of the gamma-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease. Arch Neurol. 2012 Nov;69(11):1430-40.
9 CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's disease.Br J Pharmacol.2009 Mar;156(6):982-93.
10 Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors. J Clin Oncol. 2012 Jul 1;30(19):2348-53.
11 Clinical pipeline report, company report or official report of Ayala Pharmaceuticals.