brensocatib

Action and Spectrum

Action and Spectrum

Action:

A reversible inhibitor of dipeptidyl peptidase 1 (DPP-1), brensocatib targets an enzyme that plays a key role in the activation of neutrophil serine proteases (NSPs) including neutrophil elastase during neutrophil maturation in the bone marrow.
In cell-based studies, inhibition of DPP-1 by brensocatib leads to decreased activity of NSPs such as neutrophil elastase, cathepsin G, and proteinase 3.

Drug Interaction

Adverse Reaction

Frequency not defined

1-10%

Hyperkeratosis (1-3%)

Dry skin (3-4%)

Hypertension (2-5%)

Rash (4-6%)

Headache (7-9%)

>10%

Upper respiratory tract infection (27–29%)

Black Box Warning

None

Contraindication / Caution

Contraindication/Caution:

Dermatologic reactions

Drug interactions

Gingival and periodontal reactions

Pregnancy / Lactation

Pregnancy Warnings:

Pregnancy category: N/A

Lactation: Excretion in human breastmilk is unknown

Pregnancy categories:

Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.

Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.

Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.

Category N: There is no data available for the drug under this category.

Pharmacology

Pharmacology:

A reversible inhibitor of dipeptidyl peptidase 1 (DPP-1), brensocatib targets an enzyme that plays a key role in the activation of neutrophil serine proteases (NSPs) including neutrophil elastase during neutrophil maturation in the bone marrow.
In cell-based studies, inhibition of DPP-1 by brensocatib leads to decreased activity of NSPs such as neutrophil elastase, cathepsin G, and proteinase 3.

Pharmacokinetics:

Absorption

The drug has an oral absorption of >80%, with peak plasma levels occurring between 1 to 1.4 hours after administration.

Distribution

The drug is 87.2% bound to plasma proteins and has a volume of distribution ranging from 126 to 138 L.

Metabolism

It is primarily metabolized by the CYP3A enzyme, with minor contributions from CYP2C8 and CYP2D6.

Elimination and excretion

The elimination half-life ranges from 25 to 39 hours, and the clearance rate is between 6.4 and 10.7 L/hour. Excretion occurs through both urine and feces, with 54.2% of the dose recovered in urine (22.8% unchanged) and 28.3% recovered in feces (2.4% unchanged).

Adminstartion

Administration:

For oral administration, the medication may be taken with or without food. If a dose is missed, it should be taken at the regular scheduled time on the following day. A double dose should not be taken to compensate for a missed dose.

Patient Information Leaflet

Patient information leaflet

Generic Name: brensocatib

Why do we use brensocatib?

Brensocatib received U.S. Food and Drug Administration approval on August 12, 2025, for the treatment of non-cystic fibrosis bronchiectasis in adults and adolescents aged 12 years and older. It is the first and only FDA-approved therapy specifically developed for this chronic lung disease, which is characterized by irreversible dilation of the bronchi, resulting in mucus accumulation, recurrent respiratory infections, and persistent inflammation.