Brinsupri (brensocatib)
Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Brensocatib is a dipeptidyl peptidase 1 (DPP1) inhibitor.
Brensocatib is a competitive, reversible inhibitor of dipeptidyl peptidase 1 (DPP1). DPP1 is responsible for activating pro-inflammatory neutrophil serine proteases (NSPs) during neutrophil maturation in bone marrow. Activated NSPs contribute to the development of neutrophil-driven inflammation in NCFB.
In cell-based assays, inhibition of DPP1 by brensocatib decreases the activity of NSPs such as neutrophil elastase, cathepsin G, and proteinase 3. Inhibition of DPP1 and downstream NSPs results in a broad anti-inflammatory activity.
In exploratory assays, brensocatib was associated with dose-dependent reductions in NSP activity. 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%. 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).
Brensocatib is 87.2% plasma protein bound. The elimination half-life is 25 to 39 hours. Brensocatib is primarily metabolized by CYP3A and to a lesser extent by CYP2C8 and CYP2D6.
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. In patients with non-cystic fibrosis bronchiectasis (NCFB) receiving recommended doses of brensocatib, no clinically meaningful changes of plasma thiocyanate from baseline were observed. 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).
USES: This medication is used to treat a serious chronic lung disease (non-cystic fibrosis bronchiectasis - NCFB). NCFB causes swelling of the airways and frequent worsening of symptoms (flare-ups) such as worsening cough, shortness of breath and increased sputum. Brensocatib works by blocking certain enzymes (neutrophil serine proteases).
Blocking them helps reduce swelling and the number of flare-ups.
Generic name: brensocatib
Therapeutic class: Respiratory Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Brinsupri
Indications
The following indications are listed for Brinsupri:
- Non-Cystic Fibrosis Bronchiectasis
Dosing
Dosage of brensocatib monohydrate is expressed in terms of brensocatib.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Brinsupri 10 Mg Tablet | Maintenance | Take 1 tablet (10 mg) by oral route once daily. |
| Brinsupri 25 Mg Tablet | Maintenance | Take 1 tablet (25 mg) by oral route once daily. |
No dosing information is available for this tab.
Drug interactions
In vitro studies indicate that brensocatib is a substrate of cytochrome P-450 (CYP)3A. Brensocatib does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A. Brensocatib is a weak CYP3A inducer, but not an inducer of CYP1A2, CYP2B6, CYP2C8, CYP2C9, or CYP2C19.
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. Brensocatib is an inhibitor of BCRP, OATP1B, MATE1, and MATE2-K, but is not an inhibitor of P-gp, OAT1, OCT2, OAT3, or OATP1B3.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Brensocatib/Live Vaccines
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Brensocatib may suppress the immune system by inhibiting dipeptidyl peptidase-1 (DPP-1). Brensocatib prevents the activation of neutrophil serine proteases (NSPs) during neutrophil maturation in the bone marrow.(1) Immunocompromised patients may be at increased risk for uninhibited replication after administration of live, attenuated vaccines. Immune response to vaccines may be decreased during periods of immunocompromise.(2)
CLINICAL EFFECTS: The expected serum antibody response may not be obtained. The vaccine may result in illness. Immune response to live vaccines may be decreased during periods of immunocompromise.(2)
PREDISPOSING FACTORS: Immunosuppressive diseases (e.g. hematologic malignancies, HIV disease), treatments (e.g. radiation) and drugs may all increase the magnitude of immunodeficiency.
PATIENT MANAGEMENT: The coadministration of live vaccines and brensocatib should be avoided.(1) The Centers for Disease Control (CDC) Advisory Committee on Immunization Practices (ACIP) states that live-virus and live-attenuated vaccines should not be administered to patients who are immunocompromised. The magnitude of immunocompromise and associated risks should be determined by a physician.(2)
DISCUSSION: Killed or inactivated vaccines do not pose a danger to immunocompromised patients.(2) The concomitant use of live attenuated vaccines and brensocatib has not been evaluated. Brensocatib may suppress the immune system by inhibiting dipeptidyl peptidase-1 (DPP-1).(1)
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
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.
There are no severe adverse reactions for this drug.
More Frequent
- Upper respiratory infection
Less Frequent
- Dry skin
- Gingival disorders
- Headache disorder
- Hyperkeratosis
- Hypertension
- Periodontitis
- Skin rash
Rare or Very Rare
- Abnormal hepatic function tests
- Alopecia
- Malignant neoplasm of skin
Precautions
No enhanced messaging available.
The safety and effectiveness of brensocatib have been established in pediatric patients >=12 years of age. 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.
There are no adequate data regarding use of brensocatib in pregnant women. In animal reproductive studies, use of brensocatib was associated with fetal malformations at maternal exposures 128 times the maximum recommended human dose (MRHD). Oral administration of brensocatib to pregnant rats demonstrated no adverse development effects at doses that produced maternal exposures up to 20 times the MRHD.
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.
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.
In clinical trials of brensocatib, 676 (51%) patients were >=65 years of age and 201 (15%) patients were >=75 years of age. No differences in safety or effectiveness were observed in geriatric patients compared to younger adult patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Non-cystic fibrosis bronchiectasis | ||
| J47 | ICD10CM | Bronchiectasis |
| J47.0 | ICD10CM | Bronchiectasis with acute lower respiratory infection |
| J47.1 | ICD10CM | Bronchiectasis with (acute) exacerbation |
| J47.9 | ICD10CM | Bronchiectasis, uncomplicated |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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