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

General Information of Drug (ID: DM9SY8E)

• Drug Name: PT630 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Colon cancer	2B90.Z	Preclinical	[1]
Lung cancer	2C25.0	Preclinical	[1]

• Cross-matching ID:
  PubChem CID: 11673176
  TTD Drug ID: DM9SY8E

Molecule-Related Drug Atlas

Drug(s) Targeting Dipeptidyl peptidase 4 (DPP-4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Saxagliptin	DMGXENV	Type-2 diabetes	5A11	Approved	[2]
Sitagliptin	DMGDKXN	Cystic fibrosis	CA25	Approved	[3]
Alogliptin	DM8WI3R	Type-2 diabetes	5A11	Approved	[4]
Linagliptin	DMWFJTR	Non-insulin dependent diabetes	5A11	Approved	[5]
Vildagliptin	DMYN59P	Type-2 diabetes	5A11	Approved	[6]
Dapagliflozin Propanediol; Saxagliptin Hydrochloride	DM34TXO	Type-2 diabetes	5A11	Approved	[7]
Anagliptin	DMJXIC9	Type-2 diabetes	5A11	Approved	[8]
SaxaDapa FDC	DMAPRWV	Diabetic complication	5A2Y	Phase 3	[9]
LC-150444	DM09RKB	Type-2 diabetes	5A11	Phase 3	[10]
Dutogliptin	DMM5VTA	Type-2 diabetes	5A11	Phase 3	[11]

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	[12]
BIBH 1	DMHYZEK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
Sibrotuzumab	DMT4UC1	Metastatic colorectal cancer	2B91	Phase 2	[13]
NG-641	DMITVHM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
AMG 506	DMG64PE	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
RG7461	DM5OTGR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
FAP5-DM1	DMYFVZ3	Solid tumour/cancer	2A00-2F9Z	Preclinical	[17]
ARI-3099	DMIMD0T	Discovery agent	N.A.	Investigative	[18]
MIP-1231	DM2IGD1	Solid tumour/cancer	2A00-2F9Z	Investigative	[19]
FE-999040	DM3UCWM	Solid tumour/cancer	2A00-2F9Z	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dipeptidyl peptidase 4 (DPP-4)	TTDIGC1	DPP4_HUMAN	Inhibitor	[1]
Prolyl endopeptidase FAP (FAP)	TTGPQ0F	SEPR_HUMAN	Inhibitor	[1]

References

• [1] Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice. J Clin Invest. 2009 Dec;119(12):3613-25.
• [2] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [3] Novel therapeutics for type 2 diabetes: incretin hormone mimetics (glucagon-like peptide-1 receptor agonists) and dipeptidyl peptidase-4 inhibitors. Pharmacol Ther. 2009 Oct;124(1):113-38.
• [4] Clinical pipeline report, company report or official report of Takeda (2009).
• [5] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [6] Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [8] Diabetes Treatment. Diabetes Care. 2009 March; 32(3): e25-e30.
• [9] Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for type 2 diabetes. Cardiol Rev. 2010 Jul-Aug;18(4):213-7.
• [10] Clinical pipeline report, company report or official report of ShangHai APIs Chemical.
• [11] Dutogliptin, a selective DPP4 inhibitor, improves glycaemic control in patients with type 2 diabetes: a 12-week, double-blind, randomized, placebo-controlled, multicentre trial. Diabetes Obes Metab. 2010 Apr;12(4):348-55.
• [12] 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.
• [13] 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.
• [14] Clinical pipeline report, company report or official report of PsiOxus Therapeutics.
• [15] Clinical pipeline report, company report or official report of Amgen.
• [16] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [17] Effective immunoconjugate therapy in cancer models targeting a serine protease of tumor fibroblasts. Clin Cancer Res. 2008 Jul 15;14(14):4584-92.
• [18] Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem. 2013 May 9;56(9):3467-77.
• [19] 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).