Brensocatib is a dipeptidyl peptidase 1 (DPP1) inhibitor.1
Non-cystic Fibrosis Bronchiectasis
Brensocatib is used for the treatment of non-cystic fibrosis bronchiectasis (NCFB) in adults and pediatric patients 12 years of age and older.1
Safety and efficacy of brensocatib have been established in two randomized, double-blind, placebo-controlled, parallel-group trials (ASPEN and WILLOW).1, 2, 3
In the ASPEN trial, 1680 adult and 41 pediatric patients 12 years of age and older with NCFB received brensocatib 10 mg, brensocatib 25 mg, or placebo once daily for 52 weeks.1 All adult patients experienced ≥2 documented pulmonary exacerbations prior to screening in the past 12 months while pediatric patients experienced at least 1 exacerbation.1 The mean age of patients was 60 years old; 64% were female; 74% were White, 1% was Black or African American, 11% were Asian, and 30% were Hispanic or Latino.1 Among all patients in ASPEN, 29% experienced ≥3 pulmonary exacerbations in the prior 12 months; 30% were former smokers.1 The baseline mean percent predicted forced expiratory volume in 1 second (ppFEV1) of all patients included was 23; 35% of patients had sputum positive for Pseudomonas aeruginosa , and 19% received chronic macrolide therapy.1 The primary efficacy endpoint was the annualized rate of pulmonary exacerbations over the 52 week treatment period; exacerbations were defined as worsening of ≥3 of the following major symptoms over 48 hours: increased cough, increased sputum volume or change in sputum consistency, increased sputum purulence, increased breathlessness, decreased exercise tolerance, fatigue and/or malaise, and hemoptysis, prompting a healthcare provider to prescribe systemic antibiotics.1 Exacerbations were considered severe if IV antibiotics were required and/or resulted in hospitalization.1
The annualized rate of pulmonary exacerbations was 1.02 in the 10 mg brensocatib group, 1.04 in the 25 mg brensocatib group, and 1.29 in the placebo group.1, 2 The median time to first pulmonary exacerbation was 49 weeks, 50.7 weeks, and 36.71 weeks, respectively.1 The annualized rate of severe pulmonary exacerbations was 0.14 in both brensocatib groups, and 0.19 in the placebo group.1
In the WILLOW trial, 256 adult patients with NCFB and ≥2 documented pulmonary exacerbations prior to screening received brensocatib 10 mg, brensocatib 25 mg, or placebo once daily for 24 weeks.1 The mean age of patients was 64 years old; 68% were female; 88% were White, 2% were Black or African American, 9% were Asian, and 2% were Hispanic or Latino.1 Among all patients in WILLOW, 33% experienced ≥3 pulmonary exacerbations in the prior 12 months, and 34% were former smokers.1 Additionally, the baseline ppFEV1 was 24; 35% of patients had sputum positive for Pseudomonas aeruginosa , and 16% received chronic macrolide therapy.1 The primary efficacy endpoint was the time to first pulmonary exacerbation over 24 weeks.1
The time to first pulmonary exacerbation was longer for patients receiving brensocatib at both dosages compared to placebo.1 The adjusted hazard ratio in the comparison of brensocatib with placebo was 0.58 in the 10 mg group and 0.62 in the 25 mg group.1, 3
Brensocatib is administered orally as tablets with or without food.1
If a dose of brensocatib is missed, the next dose should be taken at the regularly scheduled time; the missed dose should not be taken.1
Store brensocatib tablets at 20-25ºC, excursions permitted between 15-30ºC.1 Store in the original container.1
Dosage of brensocatib monohydrate is expressed in terms of brensocatib.1
Non-cystic Fibrosis Bronchiectasis (NCFB)
The recommended dosage of brensocatib for the treatment of NCFB in adults and pediatric patients 12 years of age and older is 10 mg or 25 mg once daily.1
No dosage adjustment is recommended for geriatric patients or patients with hepatic or renal impairment.1, 4
Dermatologic Adverse Reactions
An increase in dermatologic adverse reactions, including rash, dry skin, and hyperkeratosis has been reported in patients receiving brensocatib.1
Monitor patients for development of new rashes or skin conditions and refer patients to a dermatologist for evaluation of new dermatologic findings.1
Gingival and Periodontal Adverse Reactions
An increase in gingival and periodontal adverse reactions has been reported in patients receiving brensocatib.1
Refer patients to dental care services for regular dental checkups while taking brensocatib.1 Advise patients to perform routine dental hygiene.1
The concomitant use of brensocatib and live attenuated vaccines has not been evaluated.1 It is unknown whether administration of live attenuated vaccines during treatment will affect the safety or effectiveness of these vaccines.1
Avoid the use of live attenuated vaccines in patients receiving brensocatib.1
There are no adequate data regarding use of brensocatib in pregnant women.1 In animal reproductive studies, use of brensocatib was associated with fetal malformations at maternal exposures 128 times the maximum recommended human dose (MRHD).1 Oral administration of brensocatib to pregnant rats demonstrated no adverse development effects at doses that produced maternal exposures up to 20 times the MRHD.1
It is not known whether brensocatib is distributed into human milk, or if the drug has any effects on the breastfed infant or on milk production.1
The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for brensocatib and any potential adverse effects on the breastfed child from brensocatib or from the underlying maternal condition.1
The safety and effectiveness of brensocatib have been established in pediatric patients ≥12 years of age.1 Use of brensocatib in pediatric patients ≥12 years of age for the treatment of non-cystic fibrosis bronchiectasis (NCFB) is supported by evidence from the ASPEN trial, which enrolled 41 pediatric patients aged ≥12 years, and pharmacokinetic data in pediatric patients aged 12 to 17 years.1
In clinical trials of brensocatib, 676 (51%) patients were ≥65 years of age and 201 (15%) patients were ≥75 years of age.1 No differences in safety or effectiveness were observed in geriatric patients compared to younger adult patients.1
No clinically significant differences in pharmacokinetics were observed in patients with mild, moderate, or severe hepatic impairment.1, 4
No clinically significant differences in pharmacokinetics were observed in patients with mild, moderate, or severe renal impairment.1, 4
The most common adverse reactions (incidence ≥2%) reported with brensocatib in clinical studies were upper respiratory tract infection, headache, rash, dry skin, hyperkeratosis, and hypertension.1
In vitro studies indicate that brensocatib is a substrate of cytochrome P-450 (CYP)3A.1 Brensocatib does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A.1 Brensocatib is a weak CYP3A inducer, but not an inducer of CYP1A2, CYP2B6, CYP2C8, CYP2C9, or CYP2C19.1
Brensocatib is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), but is not a substrate of multidrug and toxin extrusion transporter (MATE)1, MATE2-K, organic anion transporting polypeptide (OAT)1, OAT3, OATP1B1, OATP1B3, organic cation transporter (OCT)1, and OCT2.1 Brensocatib is an inhibitor of BCRP, OATP1B, MATE1, and MATE2-K, but is not an inhibitor of P-gp, OAT1, OCT2, OAT3, or OATP1B3.1
Drugs Affecting Hepatic Microsomal Enzymes
When the strong CYP3A4 inducer rifampin (600 mg once daily for 9 days) was administered concomitantly with brensocatib, peak plasma concentrations of brensocatib decreased by 15% and AUC decreased by 33%.1
Drugs Metabolized by Hepatic Microsomal Enzymes
No clinically significant differences in the pharmacokinetics of midazolam are predicted when midazolam (CYP3A4 sensitive substrate) is administered concomitantly with brensocatib.1
Drugs Affecting Hepatic Microsomal Enzymes and P-glycoprotein Transport System
When the strong CYP3A4 and P-gp inhibitor clarithromycin (500 mg twice daily for 6 days) was administered concomitantly with brensocatib, peak plasma concentrations of brensocatib increased by 68% and AUC increased by 55%.1
When the moderate CYP3A4 and P-gp inhibitor verapamil (240 mg once daily for 5 days) was administered concomitantly with brensocatib, peak plasma concentrations of brensocatib increased by 53% and AUC increased by 32%.1
Drugs Affecting Gastric Acidity
Concomitant administration of brensocatib with esomeprazole (40 mg daily for 4 days) did not affect systemic exposure to brensocatib.1
Brensocatib is a competitive, reversible inhibitor of dipeptidyl peptidase 1 (DPP1).1 DPP1 is responsible for activating pro-inflammatory neutrophil serine proteases (NSPs) during neutrophil maturation in bone marrow.1 Activated NSPs contribute to the development of neutrophil-driven inflammation in NCFB.1 In cell-based assays, inhibition of DPP1 by brensocatib decreases the activity of NSPs such as neutrophil elastase, cathepsin G, and proteinase 3.1 Inhibition of DPP1 and downstream NSPs results in a broad anti-inflammatory activity.4
In exploratory assays, brensocatib was associated with dose-dependent reductions in NSP activity.1 The oral bioavailability of brensocatib has not been studied in humans; however, based on data from a mass balance study in healthy patients, the oral absorption is >80%.1 Following a single dose of 10 mg or 25 mg brensocatib, the median (min, max) time to maximum plasma concentration is 1-1.4 hours (0.5, 3 hours).1 Brensocatib is 87.2% plasma protein bound.1 The elimination half-life is 25 to 39 hours.1 Brensocatib is primarily metabolized by CYP3A and to a lesser extent by CYP2C8 and CYP2D6.1 Following administration of a radio-labeled brensocatib dose, thiocyanate, a major circulating metabolite, was identified in plasma and accounted for 51% of the total radioactivity AUC.1 In patients with non-cystic fibrosis bronchiectasis (NCFB) receiving recommended doses of brensocatib, no clinically meaningful changes of plasma thiocyanate from baseline were observed.1 Following administration of brensocatib 1.6 times the highest recommended dose to healthy patients, brensocatib is 54.2% eliminated in the urine (22.8% unchanged) and 28.3% eliminated in feces (2.4% unchanged).1
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Brensocatib is available only from designated specialty pharmacies.5 Contact the manufacturer or consult the brensocatib website ([Web]) for more information.5
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets, film-coated | 10 mg | Brinsupri® | Insmed |
25 mg | Brinsupri® | Insmed |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions December 10, 2025. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
1. Insmed Incorporated. Brinsupri® (Brensocatib) ORAL prescribing information. 2025 Aug. [Web]
2. Chalmers JD, Burgel PR, Daley CL, et al. Phase 3 trial of the DPP-1 inhibitor brensocatib in bronchiectasis. N Engl J Med. 2025;392(16):1569-1581. doi:10.1056/NEJMoa2411664
3. Chalmers JD, Haworth CS, Metersky ML, et al. Phase 2 trial of the DPP-1 inhibitor brensocatib in bronchiectasis. N Engl J Med. 2020;383(22):2127-2137. doi:10.1056/NEJMoa2021713
4. US Food and Drug Administration. Center for Drug Evaluations and Research Application Number: 217673Orig1a000 Integrated Review. From the FDA website. Accessed 2025 Oct 20.
5. There is support along your treatment journey. From Brinsupri website. Accessed 2025 Oct 20. [Web]