Talabostat

Summary

Talabostat (CHEMBL67279) is a phase-3 clinical-stage small molecule targeting DPP4, DPP8, and DPP9; indicated across 8 conditions including non-small cell lung carcinoma and lung neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 3 (DPP4, DPP8, DPP9)
• Indications: 8 conditions
• Clinical trials: 4
• Chemistry: 214.07 Da · C9H19BN2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL67279
Name	Talabostat
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	6918572
Molecular formula	C9H19BN2O3
Molecular weight	214.07
InChIKey	FKCMADOPPWWGNZ-YUMQZZPRSA-N

SMILES: B([C@@H]1CCCN1C(=O)[C@H](C(C)C)N)(O)O

IUPAC name: [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid

Also known as: PT-100, Talabostat, Valinyl-l-boroproline, Boronic acid derivative, Ketopyrrolidine derivative, Pyrrolidine derivative, L-Val-L-boroPro, Valinyl-L-boroproline, (S)-Valinyl-(R)-boroproline, Val-boroPro, talabostat, TALABOSTAT

Parent form; salt/anhydrous children: CHEMBL3545064

Patent coverage: 8,222 distinct patent families (10,259 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
DPP4	dipeptidyl peptidase 4	Inhibition	9.74	0%	P27487
DPP8	dipeptidyl peptidase 8	Inhibition	8.82	0.1%	Q6V1X1
DPP9	dipeptidyl peptidase 9	Inhibition	9.12	0.2%	Q86TI2

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Dipeptidyl peptidase 4, Presequence protease, mitochondrial, Prolyl endopeptidase, Dipeptidyl peptidase 8/9, Dipeptidyl peptidase 2, Dipeptidyl peptidase 8, Prolyl endopeptidase FAP, Dipeptidyl peptidase 9, Prolyl endopeptidase FAP.

Bioactivity

ChEMBL activities: 64 potent at pChembl ≥ 5 of 67 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	10	IC50	0.1	nM	CHEMBL_ACT_2012718
DPP4	9.74	Ki	0.18	nM	CHEMBL_ACT_1861679
DPP4	9.74	Ki	0.18	nM	CHEMBL_ACT_2362705
DPP4	9.74	Ki	0.18	nM	CHEMBL_ACT_24689243
DPP9	9.12	Ki	0.76	nM	CHEMBL_ACT_2362707
DPP4	9.05	IC50	0.9	nM	CHEMBL_ACT_12667694
DPP8	8.82	Ki	1.5	nM	CHEMBL_ACT_2362706
DPP4	8.82	IC50	1.5	nM	CHEMBL_ACT_6164151
DPP4	8.8	IC50	1.6	nM	CHEMBL_ACT_1861682
DPP4	8.77	IC50	1.7	nM	CHEMBL_ACT_17660159
DPP4	8.7	Ki	2	nM	CHEMBL_ACT_128211
DPP4	8.7	Ki	2	nM	CHEMBL_ACT_1463627
DPP9	8.7	IC50	2	nM	CHEMBL_ACT_2012726
DPP9	8.66	IC50	2.2	nM	CHEMBL_ACT_12667680
FAP	8.3	Ki	5	nM	CHEMBL_ACT_24689242
DPP8	8.26	IC50	5.5	nM	CHEMBL_ACT_12667687
FAP	7.92	IC50	12	nM	CHEMBL_ACT_12667658
DPP7	7.82	IC50	15	nM	CHEMBL_ACT_168409
DPP8	7.77	IC50	17	nM	CHEMBL_ACT_2012724
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_10865566
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_13322388
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_14590270
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_15714182
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_18971668
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_22812736
DPP4	7.66	IC50	22	nM	CHEMBL_ACT_24868516
FAP	7.62	IC50	24	nM	CHEMBL_ACT_2012722
DPP4	7.58	IC50	26	nM	CHEMBL_ACT_168408
DPP7	7.52	IC50	30	nM	CHEMBL_ACT_2012720
P97321	7.18	IC50	66	nM	CHEMBL_ACT_10865568
P97321	7.18	IC50	66	nM	CHEMBL_ACT_14590278
FAP	7.18	IC50	66	nM	CHEMBL_ACT_18971669
FAP	7.18	Ki	66	nM	CHEMBL_ACT_24868508
P97321	7.16	IC50	70	nM	CHEMBL_ACT_13322425
FAP	7.16	IC50	70	nM	CHEMBL_ACT_15714163
FAP	7.16	IC50	70	nM	CHEMBL_ACT_22812686
PREP	7.14	IC50	73	nM	CHEMBL_ACT_12667636
DPP7	7.07	IC50	86	nM	CHEMBL_ACT_10865569
DPP7	7.07	IC50	86	nM	CHEMBL_ACT_13322318
DPP7	7.07	IC50	86	nM	CHEMBL_ACT_14590280
DPP7	7.07	IC50	86	nM	CHEMBL_ACT_15714287
DPP7	7.07	IC50	86	nM	CHEMBL_ACT_22812826
DPP7	6.9	Ki	125	nM	CHEMBL_ACT_128210
DPP7	6.9	Ki	125	nM	CHEMBL_ACT_1463628
FAP	6.65	IC50	224	nM	CHEMBL_ACT_20687777
DPP4	6.33	IC50	470	nM	CHEMBL_ACT_6164148
DPP4	6.16	IC50	700	nM	CHEMBL_ACT_28459841
PREP	6.01	IC50	980	nM	CHEMBL_ACT_10865577
PREP	6.01	IC50	980	nM	CHEMBL_ACT_13322283
PREP	6.01	IC50	980	nM	CHEMBL_ACT_14590297
PREP	6.01	IC50	980	nM	CHEMBL_ACT_15714217
PREP	6.01	IC50	980	nM	CHEMBL_ACT_18971673
PREP	6.01	IC50	980	nM	CHEMBL_ACT_22812776
DPP4	5.92	IC50	1200	nM	CHEMBL_ACT_17660187
DPP4	5.92	IC50	1200	nM	CHEMBL_ACT_1861686
DPP9	5.77	IC50	1700	nM	CHEMBL_ACT_28459838
DPP8	5.44	IC50	3600	nM	CHEMBL_ACT_28459835
FAP	5.26	IC50	5500	nM	CHEMBL_ACT_28854173
PITRM1	5.26	IC50	5500	nM	CHEMBL_ACT_28854185
FAP	5.26	IC50	5500	nM	CHEMBL_ACT_28854245
PITRM1	5.26	IC50	5500	nM	CHEMBL_ACT_28854254
DPP9	5.17	IC50	6800	nM	CHEMBL_ACT_2362758
PREP	5.1	IC50	7960	nM	CHEMBL_ACT_2012728
DPP7	5.09	IC50	8200	nM	CHEMBL_ACT_28459844

Target pathways

Aggregated over 3 target gene(s): DPP4, DPP8, DPP9.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)	1	DPP4
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)	1	DPP4

Dominant GO biological processes

GO term	Targets
proteolysis	3
negative regulation of programmed cell death	2
protein maturation	2
CARD8 inflammasome complex assembly	2
pyroptotic cell death	2
NLRP1 inflammasome complex assembly	2
behavioral fear response	1
response to hypoxia	1
cell adhesion	1
positive regulation of cell population proliferation	1
negative regulation of extracellular matrix disassembly	1
peptide hormone processing	1
receptor-mediated endocytosis of virus by host cell	1
T cell costimulation	1
regulation of cell-cell adhesion mediated by integrin	1

Indications & clinical

Indications

6 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
lung neoplasm	3	MONDO:0021117	MONDO:0008903
melanoma	2	MONDO:0005105	EFO:0000756
neoplasm	2	MONDO:0005070	EFO:0000616
kidney cancer	2	MONDO:0002367	MONDO:0002367
skin neoplasm	2	MONDO:0002531	MONDO:0002898

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE2	3
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00290017	PHASE3	TERMINATED	Study of Talabostat and Pemetrexed vs. Pemetrexed in Stage IIIB/IV Non-Small Cell Lung Cancer (NSCLC) After Failure of Platinum-Based Chemotherapy
NCT00080080	PHASE2	COMPLETED	Study of Talabostat and Docetaxel in Advanced Non-Small Cell Lung Cancer
NCT00083239	PHASE2	COMPLETED	Study of Talabostat in Advanced Melanoma
NCT00083252	PHASE2	COMPLETED	Study of Talabostat and Cisplatin in Advanced Melanoma

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

28 molecules share ≥1 primary target. Top 28 by shared-target count:

Molecule	Source	Status	Shared targets
ALOGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
SAXAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
GOSOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
SITAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
TENELIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
VILDAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
DUTOGLIPTIN	ChEMBL	Phase 3	DPP4, DPP8, DPP9
ANAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
EVOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
GEMIFLOXACIN	ChEMBL	Phase 4 (approved)	DPP4
METFORMIN	ChEMBL	Phase 4 (approved)	DPP4
OMARIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TRELAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
VIDARABINE	ChEMBL	Phase 4 (approved)	DPP4
CAFFEIC ACID	ChEMBL	Phase 3	DPP4
DBPR-108	ChEMBL	Phase 3	DPP4
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	DPP4
QUERCETIN	ChEMBL	Phase 3	DPP4
RESVERATROL	ChEMBL	Phase 3	DPP4
RETAGLIPTIN	ChEMBL	Phase 3	DPP4
CARMEGLIPTIN	ChEMBL	Phase 2	DPP4
COFROGLIPTIN	ChEMBL	Phase 2	DPP4
FLAVONE	ChEMBL	Phase 2	DPP4
GALLIC ACID	ChEMBL	Phase 2	DPP4
GENISTEIN	ChEMBL	Phase 2	DPP4
LUTEOLIN	ChEMBL	Phase 2	DPP4
Carfilzomib	PubChem	Approved	DPP4