Camostat

Summary

Camostat (CHEMBL590799) is a phase-3 clinical-stage small-molecule anticoronaviral agent (ATC B02AB04) targeting PRSS1 and TMPRSS2; indicated across 3 conditions including severe acute respiratory syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: B02AB04
• Targets: 2 (PRSS1, TMPRSS2)
• Indications: 3 conditions
• Clinical trials: 7
• Chemistry: 398.4 Da · C20H22N4O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL590799
Name	Camostat
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	2536
ChEBI	CHEBI:135632
ATC	B02AB04
Molecular formula	C20H22N4O5
Molecular weight	398.4
InChIKey	XASIMHXSUQUHLV-UHFFFAOYSA-N

SMILES: CN(C)C(=O)COC(=O)CC1=CC=C(C=C1)OC(=O)C2=CC=C(C=C2)N=C(N)N

IUPAC name: [4-[2-[2-(dimethylamino)-2-oxoethoxy]-2-oxoethyl]phenyl] 4-(diaminomethylideneamino)benzoate

ChEBI definition: A benzoate ester resulting from the formal condensation of the carboxy group of 4-guanidinobenzoic acid with the hydroxy group of 2-(dimethylamino)-2-oxoethyl (4-hydroxyphenyl)acetate. It is a potent inhibitor of the human transmembrane protease serine 2 (TMPRSS2) and its mesylate salt is currently under investigation for its effectiveness in COVID-19 patients.

Pharmacological roles (ChEBI): anticoronaviral agent, serine protease inhibitor, antifibrinolytic drug, anti-inflammatory agent, antiviral agent, antihypertensive agent, antineoplastic agent.

Also known as: Camostat, SID50112779, camostat, SID174006694, CAMOSTAT, US9199927, Camostat Mesilate (FOY-305)

Parent form; salt/anhydrous children: CHEMBL85164

Patent coverage: 2,058 distinct patent families (6,733 SureChEMBL compound mentions), from 2 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
PRSS1	serine protease 1	Inhibition	7.3	0.2%	P07477
TMPRSS2	transmembrane serine protease 2	Inhibition	6	0.1%	O15393

Broader ChEMBL bioactivity targets: 14 (assay-derived). Sample: Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, Transmembrane protease serine 2, Prothrombin, Serine protease hepsin, Serine protease 1, Trypsin, Cannabinoid receptor 1, Alpha-1A adrenergic receptor.

Bioactivity

ChEMBL activities: 13 potent at pChembl ≥ 5 of 17 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CNR1	9.52	AC50	0.3	nM	CHEMBL_ACT_25116748
PRSS1	8.8	IC50	1.6	nM	CHEMBL_ACT_17722444
PRSS1	8.46	IC50	3.5	nM	CHEMBL_ACT_19043434
TMPRSS2	8.41	IC50	3.9	nM	CHEMBL_ACT_25848521
PRSS1	8.34	IC50	4.6	nM	CHEMBL_ACT_17722388
HPN	7.54	IC50	29	nM	CHEMBL_ACT_18289610
F2	6.42	AC50	380	nM	CHEMBL_ACT_25196648
F2	6.11	IC50	780	nM	CHEMBL_ACT_19043429
TMPRSS2	6	EC50	1000	nM	CHEMBL_ACT_22849638
ADRA1A	5.68	AC50	2089	nM	CHEMBL_ACT_25137795
SLC47A1	5.54	IC50	2900	nM	CHEMBL_ACT_12637860
OPRD1	5.31	AC50	4900	nM	CHEMBL_ACT_25153832
CTSL	5	IC50	10000	nM	CHEMBL_ACT_24992619

Target pathways

Aggregated over 2 target gene(s): PRSS1, TMPRSS2.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Activation of Matrix Metalloproteinases	1	PRSS1
Attachment and Entry	1	TMPRSS2
Induction of Cell-Cell Fusion	1	TMPRSS2
Uptake of dietary cobalamins into enterocytes	1	PRSS1
Developmental Lineage of Pancreatic Acinar Cells	1	PRSS1

Dominant GO biological processes

GO term	Targets
proteolysis	2
digestion	1
extracellular matrix disassembly	1
protein autoprocessing	1
positive regulation of viral entry into host cell	1
entry receptor-mediated virion attachment to host cell	1
viral translation	1
symbiont-mediated induction of syncytium formation	1

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
severe acute respiratory syndrome	3	MONDO:0005091	EFO:0000694

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

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	5
PHASE2/PHASE3	1
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04518410	PHASE2/PHASE3	COMPLETED	ACTIV-2: A Study for Outpatients With COVID-19
NCT04730206	PHASE3	TERMINATED	The DAWN Antivirals Trial for Ambulatory COVID-19 Patients
NCT04455815	PHASE2	TERMINATED	A Trial Looking at the Use of Camostat in People Who Have Tested Positive for Coronavirus (COVID-19) (SPIKE-1)
NCT04625114	PHASE2	TERMINATED	The Potential of Camostat in COVID-19
NCT04662073	PHASE2	TERMINATED	COVID-19 Outpatient Pragmatic Platform Study (COPPS) - Camostat Sub-Protocol
NCT04662086	PHASE2	COMPLETED	COVID-19 Outpatient Pragmatic Platform Study (COPPS) - Master Protocol
NCT04750759	PHASE2	TERMINATED	Safety and Preliminary Efficacy of the Combination of Niclosamide and Camostat

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.

23 molecules share ≥1 primary target. Top 23 by shared-target count:

Molecule	Source	Status	Shared targets
NAFAMOSTAT	ChEMBL	Phase 3	PRSS1, TMPRSS2
OTAMIXABAN	ChEMBL	Phase 3	PRSS1, TMPRSS2
PENTAMIDINE	ChEMBL + PubChem	Phase 4 (approved)	TMPRSS2
TANNIC ACID	ChEMBL + PubChem	Phase 4 (approved)	TMPRSS2
ARGATROBAN	ChEMBL	Phase 4 (approved)	PRSS1
BEROTRALSTAT	ChEMBL	Phase 4 (approved)	PRSS1
DEBRISOQUIN	ChEMBL	Phase 4 (approved)	TMPRSS2
MELAGATRAN	ChEMBL	Phase 4 (approved)	PRSS1
SULFAGUANIDINE	ChEMBL	Phase 4 (approved)	PRSS1
DABIGATRAN	ChEMBL	Phase 3	PRSS1
GABEXATE	ChEMBL	Phase 3	TMPRSS2
MILVEXIAN	ChEMBL	Phase 3	PRSS1
PROPAMIDINE	ChEMBL	Phase 3	TMPRSS2
QUERCETIN	ChEMBL	Phase 3	PRSS1
RUTIN	ChEMBL	Phase 3	PRSS1
SILIBININ	ChEMBL	Phase 3	PRSS1
BAICALEIN	ChEMBL	Phase 2	PRSS1
DIMINAZENE	ChEMBL	Phase 2	TMPRSS2
EFEGATRAN	ChEMBL	Phase 2	PRSS1
SEPIMOSTAT	ChEMBL	Phase 2	PRSS1
Apixaban	PubChem	Approved	PRSS1
Bromhexine	PubChem	Approved	TMPRSS2
Carfilzomib	PubChem	Approved	PRSS1