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

General Information of Drug (ID: DM1IZ5D)

• Drug Name: Talabostat Drug Info
• Synonyms: Talabostat mesylate; Boroproline compounds, DARA BioSciences; Boroproline compounds, Point Therapeutics; PT-100; Val-boro-Pro

Indication

Disease Entry	ICD 11	Status	REF
Constitutional neutropenia	4B00.0	Phase 3	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 6918572
  CAS Number: CAS 149682-77-9
  TTD Drug ID: DM1IZ5D

Molecule-Related Drug Atlas

Drug(s) Targeting Dipeptidyl peptidase 8 (DPP-8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BXCL701	DMBPUIK	Prostate cancer	2C82.0	Phase 1/2	[3]
Thiomorpholine derivative 1	DMZP6KR	N. A.	N. A.	Patented	[4]
Thiomorpholine derivative 2	DMWOK1D	N. A.	N. A.	Patented	[4]
PMID20684603C24dd	DMWZK9U	Discovery agent	N.A.	Investigative	[5]
1G244	DMEB8CG	Discovery agent	N.A.	Investigative	[6]
PMID15664838C18	DM93RKC	Discovery agent	N.A.	Investigative	[7]

Drug(s) Targeting Prolyl endopeptidase FAP (FAP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIBH 1	DMHYZEK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
Sibrotuzumab	DMT4UC1	Metastatic colorectal cancer	2B91	Phase 2	[8]
NG-641	DMITVHM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
AMG 506	DMG64PE	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
RG7461	DM5OTGR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]
PT630	DM9SY8E	Colon cancer	2B90.Z	Preclinical	[11]
FAP5-DM1	DMYFVZ3	Solid tumour/cancer	2A00-2F9Z	Preclinical	[12]
ARI-3099	DMIMD0T	Discovery agent	N.A.	Investigative	[13]
MIP-1231	DM2IGD1	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
FE-999040	DM3UCWM	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]

Drug(s) Targeting Dipeptidyl peptidase 9 (DPP-9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BXCL701	DMBPUIK	Prostate cancer	2C82.0	Phase 1/2	[3]
Thiomorpholine derivative 1	DMZP6KR	N. A.	N. A.	Patented	[4]
Thiomorpholine derivative 2	DMWOK1D	N. A.	N. A.	Patented	[4]
PMID20684603C24dd	DMWZK9U	Discovery agent	N.A.	Investigative	[5]
1G244	DMEB8CG	Discovery agent	N.A.	Investigative	[6]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dipeptidyl peptidase 8 (DPP-8)	TTJGLZF	DPP8_HUMAN	Inhibitor	[2]
Dipeptidyl peptidase 9 (DPP-9)	TTNDUL7	DPP9_HUMAN	Inhibitor	[2]
Prolyl endopeptidase FAP (FAP)	TTGPQ0F	SEPR_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] DPP inhibition alters the CXCR3 axis and enhances NK and CD8+ T cell infiltration to improve anti-PD1 efficacy in murine models of pancreatic ductal adenocarcinoma. J Immunother Cancer. 2021 Nov;9(11):e002837.
• [4] DPP-4 inhibitors: a patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):209-36.
• [5] Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors. J Med Chem. 2010 Aug 12;53(15):5620-8.
• [6] Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor. Biochem Pharmacol. 2009 Jul 15;78(2):203-10.
• [7] Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8. Bioorg Med Chem Lett. 2005 Feb 1;15(3):687-91.
• [8] 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.
• [9] Clinical pipeline report, company report or official report of PsiOxus Therapeutics.
• [10] Clinical pipeline report, company report or official report of Amgen.
• [11] Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice. J Clin Invest. 2009 Dec;119(12):3613-25.
• [12] Effective immunoconjugate therapy in cancer models targeting a serine protease of tumor fibroblasts. Clin Cancer Res. 2008 Jul 15;14(14):4584-92.
• [13] Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem. 2013 May 9;56(9):3467-77.
• [14] 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).