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

General Information of Drug (ID: DMT4UC1)

• Drug Name: Sibrotuzumab Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Metastatic colorectal cancer	2B91	Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DMT4UC1

Molecule-Related Drug Atlas

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	[3]
BIBH 1	DMHYZEK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]
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	[10]
FE-999040	DM3UCWM	Solid tumour/cancer	2A00-2F9Z	Investigative	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prolyl endopeptidase FAP (FAP)	TTGPQ0F	SEPR_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT02198274) Intravenous BIBH 1 in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
• [2] 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.
• [3] 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.
• [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.
• [10] 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).