Brensocatib

Summary

Brensocatib (CHEMBL3900409) is a phase-3 clinical-stage small molecule targeting CTSC; indicated across 6 conditions including bronchiectasis and severe acute respiratory syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (CTSC)
• Indications: 6 conditions
• Clinical trials: 17
• Chemistry: 420.5 Da · C23H24N4O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3900409
Name	Brensocatib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	118253852
Molecular formula	C23H24N4O4
Molecular weight	420.5
InChIKey	AEXFXNFMSAAELR-RXVVDRJESA-N

SMILES: CN1C2=C(C=CC(=C2)C3=CC=C(C=C3)C[C@@H](C#N)NC(=O)[C@@H]4CNCCCO4)OC1=O

IUPAC name: (2S)-N-[(1S)-1-cyano-2-[4-(3-methyl-2-oxo-1,3-benzoxazol-5-yl)phenyl]ethyl]-1,4-oxazepane-2-carboxamide

Also known as: AZD 7986, Azd-7986, AZD-7986, Azd7986, AZD7986, Brensocatib, INS-1007, INS1007, BRENSOCATIB

Patent coverage: 142 distinct patent families (437 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 342 (78%) of the total. 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
CTSC	cathepsin C	Inhibition	8.4	0%	P53634

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Dipeptidyl peptidase 1, Dipeptidyl peptidase 1, Dipeptidyl peptidase 1, Dipeptidyl peptidase 1.

Bioactivity

ChEMBL activities: 26 potent at pChembl ≥ 5 of 26 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CTSC	8.6	Kd	2.51	nM	CHEMBL_ACT_16748655
CTSC	8.4	IC50	3.98	nM	CHEMBL_ACT_16748708
CTSC	8.4	IC50	3.98	nM	CHEMBL_ACT_16748722
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_27579074
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_27985589
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_28508966
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_29009333
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_29014682
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_29021555
CTSC	8.35	IC50	4.47	nM	CHEMBL_ACT_29025752
CTSC	7.99	IC50	10.3	nM	CHEMBL_ACT_23245774
CTSC	7.99	IC50	10.3	nM	CHEMBL_ACT_24917174
CTSC	7.98	IC50	10.43	nM	CHEMBL_ACT_29172066
CTSC	7.97	IC50	10.72	nM	CHEMBL_ACT_29172083
CTSC	7.82	IC50	15.2	nM	CHEMBL_ACT_23245848
CTSC	7.82	IC50	15.2	nM	CHEMBL_ACT_24917219
O97578	7.8	IC50	15.85	nM	CHEMBL_ACT_16748642
CTSC	7.71	IC50	19.4	nM	CHEMBL_ACT_23245700
CTSC	7.71	IC50	19.4	nM	CHEMBL_ACT_24917138
P80067	7.7	IC50	19.95	nM	CHEMBL_ACT_16748641
CTSC	7.67	IC50	21.27	nM	CHEMBL_ACT_29125411
P97821	7.6	IC50	25.12	nM	CHEMBL_ACT_16748640
CTSC	7.21	IC50	61.66	nM	CHEMBL_ACT_16748659
CTSC	6.94	IC50	114.8	nM	CHEMBL_ACT_16748663
CTSC	6.85	IC50	141.2	nM	CHEMBL_ACT_16748657
CTSC	6.68	IC50	208.9	nM	CHEMBL_ACT_16748661

Target pathways

Aggregated over 1 target gene(s): CTSC.

Top Reactome pathways

14 total, by targets touching each:

Pathway	Targets	Genes
Adaptive Immune System	1	CTSC
Innate Immune System	1	CTSC
Immune System	1	CTSC
ER to Golgi Anterograde Transport	1	CTSC
Membrane Trafficking	1	CTSC
COPII-mediated vesicle transport	1	CTSC
MHC class II antigen presentation	1	CTSC
Metabolism of proteins	1	CTSC
Asparagine N-linked glycosylation	1	CTSC
Vesicle-mediated transport	1	CTSC
Cargo concentration in the ER	1	CTSC
Post-translational protein modification	1	CTSC
Neutrophil degranulation	1	CTSC
Transport to the Golgi and subsequent modification	1	CTSC

Dominant GO biological processes

GO term	Targets
T cell mediated cytotoxicity	1
proteolysis	1
immune response	1
negative regulation of myelination	1
obsolete proteolysis involved in protein catabolic process	1
obsolete positive regulation of proteolysis involved in protein catabolic process	1
positive regulation of microglial cell activation	1
positive regulation of apoptotic signaling pathway	1
apoptotic process	1

Indications & clinical

Indications

6 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
bronchiectasis	3	MONDO:0004822	HP:0002110
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
cystic fibrosis	2	MONDO:0009061	MONDO:0009061
liver disorder	1	MONDO:0005154	EFO:0001421
kidney disorder	1	MONDO:0005240	EFO:0003086

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

Clinical trials

Total trials: 17.

Phase distribution

Phase	Trials
PHASE1	10
PHASE2	4
PHASE3	2
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04594369	PHASE3	COMPLETED	A Study to Assess the Efficacy, Safety, and Tolerability of Brensocatib in Participants With Non-Cystic Fibrosis Bronchiectasis
NCT04817332	PHASE3	COMPLETED	STOP-COVID19: Superiority Trial Of Protease Inhibition in COVID-19
NCT06685835	PHASE2	ACTIVE_NOT_RECRUITING	A Study of the Efficacy and Safety of Brensocatib in Adults With Moderate to Severe Hidradenitis Suppurativa (HS)
NCT03218917	PHASE2	COMPLETED	Assessment of INS1007 in Participants With Non-Cystic Fibrosis Bronchiectasis
NCT05090904	PHASE2	COMPLETED	A Study to Assess the Safety, Tolerability, and Pharmacokinetics of Brensocatib Tablets in Adults With Cystic Fibrosis
NCT06013241	PHASE2	COMPLETED	A Study of the Efficacy and Safety of Brensocatib in Participants With Chronic Rhinosinusitis Without Nasal Polyps (CRSsNP)
NCT02303574	PHASE1	COMPLETED	Single + Multiple Ascending Dose and Food Effect Study of AZD7986 in Healthy Volunteers, PK, PD and Safety Study
NCT02653872	PHASE1	COMPLETED	A Phase I Study to Assess PK of AZD7986 Alone & With Verapamil, Itraconazole or Diltiazem in Healthy Subjects
NCT05355935	PHASE1	COMPLETED	A Study to Investigate the Effects of Brensocatib on QT Interval in Healthy Participants
NCT05517525	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics (PK) and Safety of a Single Dose of Brensocatib in Participants With Normal Hepatic Function and Participants With Hepatic Impairment
NCT05673603	PHASE1	COMPLETED	A Study of Brensocatib Following a Single Oral Administration in Participants With or Without Renal Impairment
NCT05826574	PHASE1	COMPLETED	A Study to Assess Pharmacokinetics (PK) of Brensocatib Alone and With Multiple Doses of Rifampin or Esomeprozole in Healthy Participants
NCT05927597	PHASE1	COMPLETED	A Study of the Safety, Pharmacokinetics, and Pharmacodynamics of INS1007 in Healthy Japanese and Caucasian Participants
NCT05965570	PHASE1	COMPLETED	A Study to Investigate Effect of Clarithromycin, a Strong CYP3A4 Inhibitor, on Brensocatib Pharmacokinetics in Healthy Participants
NCT06178783	PHASE1	COMPLETED	A Study of the Palatability and Acceptability of Different Brensocatib Oral Liquid Formulations in Healthy Participants
NCT06344728	PHASE1	COMPLETED	A Study to Assess the Relative Bioavailability of Brensocatib Pediatric Oral Solution to Oral Tablets in Healthy Participants
NCT05344508	Not specified	APPROVED_FOR_MARKETING	An Expanded Access Study to Assess Brensocatib for Participants With Non-Cystic Fibrosis Bronchiectasis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

3 molecules share ≥1 primary target. Top 3 by shared-target count:

Molecule	Source	Status	Shared targets
OSIMERTINIB	ChEMBL + PubChem	Phase 4 (approved)	CTSC
CANERTINIB	ChEMBL	Phase 3	CTSC
Afatinib	PubChem	Approved	CTSC