Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM3UCWM)

Drug Name

FE-999040 Drug Info

Synonyms

FAP inhibitors, Vantia; Fibroblast activation protein inhibitors (sc/oral, cancer/pulmonary fibrosis/IBD), Vantia

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Investigative	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Preclinical Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Prolyl endopeptidase FAP (FAP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Talabostat	DM1IZ5D	Constitutional neutropenia	4B00.0	Phase 3	[2]
BIBH 1	DMHYZEK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]
Sibrotuzumab	DMT4UC1	Metastatic colorectal cancer	2B91	Phase 2	[3]
NG-641	DMITVHM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[4]
AMG 506	DMG64PE	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
RG7461	DM5OTGR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
PT630	DM9SY8E	Colon cancer	2B90.Z	Preclinical	[7]
FAP5-DM1	DMYFVZ3	Solid tumour/cancer	2A00-2F9Z	Preclinical	[8]
ARI-3099	DMIMD0T	Discovery agent	N.A.	Investigative	[9]
MIP-1231	DM2IGD1	Solid tumour/cancer	2A00-2F9Z	Investigative	[1]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prolyl endopeptidase FAP (FAP)	TTGPQ0F	SEPR_HUMAN	Inhibitor	[1]

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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. (Target id: 2365).
2	Phase II trial of single agent Val-boroPro (Talabostat) inhibiting Fibroblast Activation Protein in patients with metastatic colorectal cancer. Cancer Biol Ther. 2007 Nov;6(11):1691-9.
3	A Phase I dose-escalation study of sibrotuzumab in patients with advanced or metastatic fibroblast activation protein-positive cancer. Clin Cancer Res. 2003 May;9(5):1639-47.
4	Clinical pipeline report, company report or official report of PsiOxus Therapeutics.
5	Clinical pipeline report, company report or official report of Amgen.
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice. J Clin Invest. 2009 Dec;119(12):3613-25.
8	Effective immunoconjugate therapy in cancer models targeting a serine protease of tumor fibroblasts. Clin Cancer Res. 2008 Jul 15;14(14):4584-92.
9	Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem. 2013 May 9;56(9):3467-77.