A Multi-center, Randomized, Double-Blind, Parallel-group, Vehicle-Controlled Study to Evaluate the Safety, Efficacy and Pharmacokinetics of DFD-25 (Zileuton Ointment), 1.25% and 5%, in Subjects with Moderate to Severe Atopic Dermatitis (AD) Over a 4 Week Treatment Period

Start Date02 Dec 2019

Sponsor / Collaborator-

NCT03571620

/ CompletedPhase 2

A Multicenter, Randomized, Phase 2, Double-blind, Vehicle-controlled, Parallel Group Comparison Study to Evaluate the Safety and Efficacy of Q301 Cream in Adolescents and Adults With Mild to Moderate Atopic Dermatitis

This is a randomized, double-blind, vehicle-controlled, parallel-group comparison study to evaluate the safety and efficacy of Q301 Cream vs. vehicle in adolescent and adult subjects with mild to moderate AD. Study drug (Q301 Cream or vehicle) will be administered topically twice a day for 8 consecutive weeks.

Start Date21 Jun 2018

Sponsor / Collaborator

Qurient Co., Ltd.

NCT02348203

/ CompletedPhase 2IIT

Clinical Study of the Effect of Combined Treatment of Aspirin and Zileuton on Biomarkers of Tobacco-Related Carcinogenesis in Current Smokers

This randomized phase II trial studies the effects of aspirin and zileuton on genes related to tobacco use in current smokers. Aspirin and zileuton may interfere with genes related to tobacco use and may be useful in preventing lung cancer in current smokers.

Start Date13 Jan 2016

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Zileuton

100 Translational Medicine associated with Zileuton

100 Patents (Medical) associated with Zileuton

672

Literatures (Medical) associated with Zileuton

31 Dec 2025·REDOX REPORT

Synergistic effects of AgNPs and zileuton on PCOS via ferroptosis and inflammation mitigation

Article

Author: Shatat, Doaa ; Atef, Marwa Mohamed ; Awad, Marwa Mahmoud ; Ibrahim, Rowida Raafat ; Farghal, Eman E. ; Motawea, Shaimaa M. ; El hanafy, Hend Ahmed ; Elesawy, Rasha ; Eltokhy, Amira K. ; El-Deeb, Omnia Safwat ; El-shaer, Rehab Ahmed Ahmed ; Ismail, Radwa ; Hafez, Yasser Mostafa

BACKGROUND:

The most prevalent endocrine disorder affecting women is PCOS. Programmed death of ovarian cells has yet to be elucidated. Ferroptosis is a kind of iron-dependent necrosis featured by significantly Fe⁺²-dependent lipid peroxidation. The ongoing study aimed to reinforce fertility by combining therapy with AgNPs and (Zileuton) in PCOS rats' model.

METHODS:

The study included 75 adult female rats divided into 5 groups; control, PCOS, PCOS treated with AgNPs, PCOS treated with Zileuton, and PCOS group treated with AgNPs and Zileuton. The study investigated the anti-ferroptotic, anti-inflammatory, antioxidant, antiapoptotic, histopathological and immunohistochemical examinations of COX-2 and VEGF.

RESULTS:

The combination of AgNPs and Zileuton showed significant reduction of inflammatory mediators (IL-6, TNF-α, NFk-B) compared with diseased group (P-value < 0.05), regression of ferroptosis marks (Panx1 and TLR4 expression, Fe⁺² levels) compared with diseased group (P-value < 0.05), depression of apoptotic marker caspase 3 level compared with diseased animals (P-value < 0.05), depression of MDA level, elevation of HO-1, GPx4 activity, and reduction of Cox2 and VEGF as compared with the diseased, AgNPs or zileuton-treated groups (P-value < 0.05).

CONCLUSION:

The study showed that the combination of AgNPs and zileuton guards against, inflammation, apoptosis, and ferroptosis in PCO.

01 Dec 2025·TOXICOLOGY AND APPLIED PHARMACOLOGY

Exploration of zileuton protective mechanisms against vancomycin-associated nephrotoxicity

Article

Author: Hudson, Cole S ; Nigo, Masayuki ; Vuong, Linh T ; Hu, Ming ; Tam, Vincent H ; Truong, Luan D ; Sheikh-Hamad, David ; Smith, James E ; Sun, Rongjin

Vancomycin is one of the most commonly used parenteral antibiotics for treating drug-resistant bacterial infections, however, it is hindered by nephrotoxicity. We previously demonstrated that zileuton could delay the onset of vancomycin-associated nephrotoxicity in rats. Here, we sought to understand the mechanism(s) of zileuton renal protection. Sprague-Dawley rats were administered vancomycin (200 mg/kg) and zileuton (1 and 4 mg/kg) daily for 10 days. After 3 days, kidneys were collected from select animals for histopathological analysis of renal injury. Single-dose vancomycin serum pharmacokinetics and renal tissue spatial distribution with adjuvant zileuton were evaluated. In vitro, proximal tubular cells were exposed to vancomycin and zileuton; cell viability, vancomycin accumulation, ROS levels, and p62/KEAP1 and ferroptosis-related protein levels were measured. Vancomycin was associated with increased serum creatinine and proximal tubule injury in rats including tubular cell necrosis, cytoplasmic vacuolization, interstitial edema, and mononuclear inflammatory cell infiltration. Adjuvant zileuton reduced renal injury and serum creatinine elevation without altering vancomycin serum pharmacokinetics or renal tissue distribution. In vitro, vancomycin exposure resulted in cellular injury, increased ROS, and significantly decreased HO-1 levels. Concomitant zileuton reduced cellular injury, decreased ROS, and rescued HO-1 levels. These preliminary findings indicate that zileuton may be protective against vancomycin-associated renal injury potentially by rescuing HO-1 levels and reducing oxidative stress in proximal tubular cells. Attenuation of nephrotoxicity would allow the optimal clinical use of vancomycin to treat drug-resistant bacterial infections, which could reduce patient harm and hospitalization costs.

31 Aug 2025·FASEB JOURNAL

Modulation of Neutrophil Recruitment and Inflammatory Signaling in Acute Respiratory Distress Syndrome by Leukotriene Inhibitors Montelukast and Zileuton

Article

Author: Heck‐Swain, Ka‐Lin ; Fuhr, Anika ; Koeppen, Michael ; Kleinmaier, Carolin ; Biedritzky, Anna ; Ngamsri, Kristian‐Christos ; Gamper‐Tsigaras, Jutta ; Konrad, Franziska ; Zhang, Yi

ABSTRACT:

Acute respiratory distress syndrome (ARDS) is characterized by excessive neutrophil‐driven inflammation and remains a leading cause of mortality in critical care. Leukotriene‐modifying agents, such as montelukast (a CysLTR1 antagonist) and zileuton (a 5‐lipoxygenase inhibitor), are approved for chronic inflammatory lung diseases, but their role in ARDS is unclear. We investigated the effects of montelukast and zileuton in a murine model of lipopolysaccharide (LPS)‐induced ARDS, supported by in vitro assays using human neutrophils. Mice were treated with either drug 1 h post‐injury. Neutrophil recruitment, cytokine release, and inflammatory signaling were assessed by immunohistochemistry, flow cytometry, ELISA, and qPCR. Neutrophil chemotaxis and signaling responses were evaluated in vitro. Both montelukast and zileuton significantly reduced neutrophil infiltration into lung tissue and bronchoalveolar lavage fluid (p < 0.01), suppressed expression of adhesion molecules (PSGL‐1, L‐selectin, LFA‐1), and decreased levels of TNF‐α, CXCL2, IL‐1β, and IL‐6 in BAL fluid (p < 0.05). In vitro, both drugs impaired neutrophil chemotaxis and reduced CysLTR1 and ERK1/2 expression following inflammatory stimulation. These findings indicate that leukotriene pathway inhibition limits neutrophil recruitment and activation in ARDS by modulating receptor expression and ERK1/2 signaling. Montelukast and zileuton may offer a targeted strategy to attenuate hyperinflammation in ARDS.

News (Medical) associated with Zileuton

15 May 2025

·www.globenewswire.com

Amneal Receives U.S. FDA Approval for Brekiya® (dihydroergotamine mesylate) injection for the Acute Treatment of Migraine and Cluster Headaches in Adults

Brekiya® becomes the first and only DHE autoinjector that allows patients to self-administer the same medication used in hospitals in a ready-to-use form Product will be available for appropriate patients in the second half of 2025 BRIDGEWATER, N.J., May 15, 2025 (GLOBE NEWSWIRE) -- Amneal Pharmaceuticals, Inc. (Nasdaq: AMRX) (“Amneal” or the “Company”) today announced that the U.S. Food and Drug Administration (FDA) has approved Brekiya® (dihydroergotamine mesylate) injection, the first and only dihydroergotamine (DHE) autoinjector for the acute treatment of migraine with or without aura and the acute treatment of cluster headaches in adults.1,2 Brekiya autoinjector provides patients with the potential for sustained* pain relief† in a convenient, self-administered form.1,3,4 It contains the same medication (DHE) used in hospitals, now in a ready-to-use device.1,5 Brekiya autoinjector does not require refrigeration, assembly, or priming of the device.1 Patients can deliver one dose subcutaneously into the middle of the thigh.1 This may be beneficial for patients who respond inadequately to oral therapies due to lack of efficacy, experience nausea or vomiting during attacks, have gastroparesis, or delay dosing until too late into the attack.1,5,6 “We are thrilled to offer the first and only ready-to-use autoinjector for patients suffering from acute migraine and cluster headaches. Physicians are familiar with DHE, which is an effective and well-established therapy that provides sustained relief for headaches. Our single-dose autoinjector represents an innovative therapeutic option for patients that allows for quick self-administration of the medication during these painful attacks without visiting the emergency room,” said Joe Renda, Senior Vice President, Chief Commercial Officer – Specialty. DHE is commonly administered in emergency rooms, urgent care facilities, and headache clinics intravenously. DHE can be used at any point during a migraine attack, and may protect patients from headache recurrence.1,3,4 Approximately 39 million Americans are living with migraine7, and up to one million with cluster headache.8 Also, headache is the fourth most common reason for emergency department visits, and accounts for 3% of all emergency room visits in the United States.9 There are limited treatment options available for cluster headache, and Brekiya autoinjector represents a new treatment option for this underserved population.2 Do not take Brekiya autoinjector with strong CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics. See additional Important Safety Information below. IndicationBrekiya autoinjector is a prescription medicine used for the acute treatment of migraine with or without aura and acute cluster headaches in adults. Brekiya autoinjector is not used to prevent migraine or used to treat other types of headaches such as hemiplegic migraines (that make you unable to move on one side of your body) or basilar migraines (rare form of migraine with aura). It is not known if Brekiya autoinjector is safe and effective in children. IMPORTANT SAFETY INFORMATIONSerious or potentially life-threatening reductions in blood flow to the brain or extremities due to interactions between dihydroergotamine (the active ingredient in Brekiya autoinjector) with strong CYP3A4 inhibitors (such as protease inhibitors and macrolide antibiotics) have been reported rarely. As a result, these medications should not be taken together. Do not use Brekiya autoinjector if you: are taking medicines known as strong CYP3A4 inhibitors, such as: ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, ketoconazole, or itraconazole.have heart problems or a history of heart problems, or uncontrolled high blood pressure.have narrowing of blood vessels in your legs, arms, stomach, or kidneys (peripheral vascular disease).have sepsis, had vascular surgery, severe liver or kidney problems.are allergic to dihydroergotamine, ergot alkaloids, latex, or any of the ingredients in Brekiya autoinjector.have taken any of the following medicines in the last 24 hours: sumatriptan, frovatriptan, ergotamine or ergotamine-type medicines, almotriptan, naratriptan, zolmitriptan, eletriptan, or rizatriptanhave taken any medicines that constrict your blood vessels or raise your blood pressure. Before you take Brekiya autoinjector, tell your healthcare provider about all your medical conditions, including if you: have high blood pressure, liver problems, or kidney problems.have risk factors for heart disease, such as: high blood pressure, high cholesterol levels, smoke, are overweight, diabetes, family history of heart disease.are pregnant or plan to become pregnant. Brekiya autoinjector may cause preterm labor. Brekiya autoinjector should be avoided during pregnancy. Talk to your healthcare provider right away if you are pregnant or want to become pregnant.are breastfeeding or plan to breastfeed. Brekiya autoinjector may reduce breast milk supply and pass into your breast milk. Brekiya autoinjector may be harmful to your baby. Do not breastfeed your baby while taking Brekiya autoinjector and for 3 days after you use Brekiya autoinjector. Talk with your healthcare provider about the best way to feed your baby if you take Brekiya autoinjector. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take: sumatriptan, ergot-type medicine, saquinavir, nefazodone, fluconazole, grapefruit juice, zileuton, nicotine, propranolol or other medicines that can lower your heart rate, any medicines that can increase your blood pressure, selective serotonin reuptake inhibitors. These are not all of the medicines that could affect how Brekiya autoinjector works. Your healthcare provider can tell you if it is safe to take Brekiya autoinjector with other medicines. How should I use Brekiya autoinjector? Certain people should take their first dose of Brekiya autoinjector in their healthcare provider’s office or in another medical setting.Brekiya autoinjector is for injection under the skin (subcutaneous) only.Use Brekiya autoinjector exactly as your healthcare provider tells you to use it.Each autoinjector contains one dose (1 mg).If your headache comes back after the first complete dose, you may give yourself up to 2 more doses as needed. Wait at least one hour between doses.Do not inject more than 3 doses (3 mg) of Brekiya autoinjector in a 24-hour period or 6 doses (6 mg) in a 1-week (7 day) period. What are the possible side effects of Brekiya autoinjector?Brekiya autoinjector can cause serious side effects, including: Heart attack and other heart problems. Heart problems may lead to death. Stop taking Brekiya autoinjector and get emergency medical help right away if you have any symptoms of a heart attack, such as: numbness or tingling in your fingers and toes, muscle pain or cramps in your arms and legs, weakness in your legs, temporary speeding or slowing of your heart rate, or swelling or itching. Brekiya autoinjector is not for people with risk factors for heart disease unless a heart exam is done and shows no problem. Stroke. Stop using Brekiya autoinjector and get emergency medical help right away if you have any of the symptoms of a stroke.Changes in color or sensation in your fingers and toes (Raynaud’s syndrome).Stomach and intestinal problems.Increased blood pressure.Medicine overuse headache. Some people who use too much Brekiya autoinjector may make their headaches worse. If your headaches get worse, your healthcare provider may decide to stop your treatment with Brekiya autoinjector.Preterm labor.Tissue changes (fibrotic complications). Inflammation and fiber-like tissue that is not normal (fibrosis) can occur around the lungs and stomach. Tell your healthcare provider if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of Brekiya autoinjector. Call your healthcare provider for medical advice about side effects. How should I store Brekiya autoinjector? Store at room temperature between 68°F to 77°F (20°C to 25°C). Do not refrigerate or freeze.Protect Brekiya autoinjector from light.Keep Brekiya autoinjector in the original pack until ready to use. To report SUSPECTED ADVERSE REACTIONS, contact Amneal Specialty, a division of Amneal Pharmaceuticals LLC at 1-877-835-5472, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Please see full Prescribing Information, including Boxed Warning, Medication Guide, and Instructions for Use at Brekiya.com. *Sustained represents a duration of approximately 24-72 hours2,3†Cluster headache results reported using IV administration.4 References: Brekiya [package insert]. Bridgewater, NJ: Amneal Pharmaceuticals LLC; 2025.Data on File. Amneal Pharmaceuticals LLC.Winner P, Ricalde O, Le Force B, Saper J, Margul B. Arch Neurol. 1996;53(2):180-184.Mather PJ, Silberstein SD, Schulman EA, Hopkins MM. Headache. 1991;31(8):525-532.Silberstein SD, Shrewsbury SB, Hoekman J. Headache. 2020;60(1):40-57. doi:10.1111/head.13700Aurora SK, Papapetropoulos S, Kori SH, Kedar A, Abell TL. Cephalalgia. 2013;33(6):408-415.https://migraineresearchfoundation.org/about-migraine/migraine-facts/https://americanmigrainefoundation.org/resource-library/cluster-headache-2/Phelan, M, Thompson NR, Zubair A et al. Emergency department utilization among patients who receive outpatient specialty care for headache: A retrospective cohort study analysis. Headache. 2023;63:472–483. Brekiya is a registered trademark of Amneal Pharmaceuticals LLC. About AmnealAmneal Pharmaceuticals, Inc. (Nasdaq: AMRX), headquartered in Bridgewater, NJ, is a global biopharmaceutical company. We make healthy possible through the development, manufacturing, and distribution of a diverse portfolio of over 280 pharmaceuticals, primarily within the United States. In its Affordable Medicines segment, the Company is expanding across a broad range of complex product categories and therapeutic areas, including injectables and biosimilars. In its Specialty segment, Amneal has a growing portfolio of branded pharmaceuticals focused primarily on central nervous system and endocrine disorders. Through its AvKARE segment, the Company is a distributor of pharmaceuticals and other products for the U.S. federal government, retail, and institutional markets. For more information, please visit www.amneal.com and follow us on LinkedIn. Cautionary Statement on Forward-Looking StatementsCertain statements contained herein, regarding matters that are not historical facts, may be forward-looking statements (as defined in the U.S. Private Securities Litigation Reform Act of 1995). Such forward-looking statements include statements regarding management’s intentions, plans, beliefs, expectations, financial results, or forecasts for the future, including among other things: discussions of future operations; expected or estimated operating results and financial performance; and statements regarding our positioning, including our ability to drive sustainable long-term growth, and other non-historical statements. Words such as “plans,” “expects,” “will,” “anticipates,” “estimates,” and similar words, or the negatives thereof, are intended to identify estimates and forward-looking statements. The forward-looking statements contained herein are also subject generally to other risks and uncertainties that are described from time to time in the Company’s filings with the Securities and Exchange Commission, including under Item 1A, “Risk Factors” in the Company’s most recent Annual Report on Form 10-K and in its subsequent reports on Forms 10-Q and 8-K. Forward-looking statements included herein speak only as of the date hereof and we undertake no obligation to revise or update such statements to reflect the occurrence of events or circumstances after the date hereof. Investor Contact Anthony DiMeoVP, Investor Relations anthony.dimeo@amneal.comMedia ContactBrandon SkopSr. Director, Corporate CommunicationsBrandon.skop@amneal.com PP-PRS-DHE-US-0001 05/2025

Drug Approval

19 Sep 2023

·synapse.patsnap.com

Targeting 5-lipoxygenase - Leukotriene inhibitor

Leukotrienes are a group of inflammatory mediators produced by the metabolism of arachidonic acid (AA) through the 5-lipoxygenase (5-LO) pathway, featuring a conjugated triene structure of a 20-carbon unsaturated acid. They are classified into six types - A, B, C, D, E, F, based on their substituents. Among these, LTC4, LTD4, and LTE4 all contain cysteinyl at C-6, collectively referred to as cysteinyl leukotrienes (CysLTs). Leukotrienes can be produced by cells after various immunological or non-immunological stimuli, through autocrine or paracrine mechanisms. These stimuli include antigens, immune complexes, complements, cytokines, osmotic pressure, and environmental pollutants. Once leukotrienes bind with specific G-protein coupled receptors (GPCRs) on the cell surface, they activate Gq proteins leading to an increase in intracellular calcium concentrations, and activating Gi proteins causing a decrease in cAMP, both of which can trigger a cascade of kinase protein signal transduction, inducing intracellular transcription responses and cell movement, thereby widely participating in the body's immune response. Currently, anti-leukotriene drugs are primarily divided into two categories: the first are leukotriene receptor antagonists, which inhibit tissue responses to leukotrienes by blocking leukotriene receptors, including Montelukast, Zafirlukast, and Pranlukast; the second one are leukotriene synthesis inhibitors, which inhibit the activity of the key enzyme 5-LO in the leukotriene synthesis pathway, thereby inhibiting the synthesis of cysteinyl leukotrienes and LTB4. Leukotriene Competitive LandscapeAccording to the data provided by Patsnap Synapse-Global Drug Intelligence Database: the following figure shows that as of 18 Sep 2023, there are a total of 142 5-LOX drugs worldwide, from 105 organizations, covering 60 indications, and conducting 52 clinical trials. 👇Please click on the picture link below for free registration or login directly if you have freemium accounts, you can browse the latest research progress on drugs , indications, organizations, clinical trials, clinical results, and drug patents related to this target. 5-LOX, or 5-lipoxygenase, is an enzyme that plays a crucial role in the human body's inflammatory response. It is responsible for the conversion of arachidonic acid into leukotrienes, which are potent mediators of inflammation. These leukotrienes are involved in various physiological processes, including immune response, allergic reactions, and the development of certain diseases such as asthma and arthritis. Due to its involvement in inflammation, 5-LOX has become an attractive target for pharmaceutical research, with the aim of developing drugs that can modulate its activity and potentially alleviate inflammatory conditions. Drugs under this target have been approved for indications such as asthma. Small molecule drugs are progressing most rapidly, with one approved and six in preclinical development. The United States is the leading country in terms of drug development for target 5-LOX, followed by Australia, Israel, and the European Union. China has made progress in preclinical development for this target. The current competitive landscape for target 5-LOX is characterized by a diverse range of companies and drug types. The presence of biosimilars indicates intense competition around the innovative drugs. Further research and development are needed to explore the potential of target 5-LOX in various indications and to expand its market presence globally. Leukotriene Pathway Inhibitor: ZileutonZileuton is a Leukotriene pathway inhibitor, classified as a 5-lipoxygenase inhibitor, used for the treatment of asthma and allergic rhinitis. Zileuton is associated with rare drug-induced liver disease and is considered contraindicated in patients with active liver disease. The 5- lipoxygenase is responsible for the conversion of arachidonic acid into leukotriene A4, leukotriene A4 is an effective mediator of the inflammatory cascade reaction, playing a pivotal role in asthma and allergic rhinitis. Zileuton has been shown to improve the symptoms of asthma and allergic rhinitis and was approved for use in the United States in 1996. Current indications include the prophylaxis and chronic treatment of asthma in adults and children aged 12 and above. 👇Please click on the image below to directly access the latest data (R&D Status | Core Patent | Clinical Trial | Approval status in Global countries) of this drug. Given its approval for asthma, Zileuton is expected to have a positive impact on patients suffering from this condition. By targeting 5-LOX, the drug helps to reduce the production of leukotrienes, which are known to contribute to airway inflammation and bronchoconstriction in asthma patients. By inhibiting this pathway, Zileuton can potentially alleviate symptoms and improve lung function in individuals with asthma. In summary, Zileuton is a small molecule drug developed by Abbott Laboratories that targets 5-LOX and is indicated for the treatment of asthma. Its approval in 1996 in the United States signifies its efficacy and safety in managing this respiratory condition. As a therapeutic option, Zileuton has the potential to provide relief to asthma patients by reducing airway inflammation and constriction. Targeted 5-LOX Small Molecule Drugs:A-72694The drug A-72694 is a small molecule drug that targets 5-LOX, which stands for 5-lipoxygenase. It is primarily developed for the treatment of asthma, a respiratory disease that affects the immune system. The drug is currently in the preclinical phase, indicating that it is still undergoing laboratory testing and has not yet progressed to human clinical trials. A-72694 is being developed by Abbott Laboratories, a well-known pharmaceutical company with expertise in the field of biomedicine. The therapeutic areas of A-72694 include immune system diseases and respiratory diseases, with asthma being the active indication. This indicates that the drug is specifically designed to target and treat asthma, a chronic condition characterized by inflammation and narrowing of the airways. 👇Please click on the image below to directly access the latest data (R&D Status | Core Patent | Clinical Trial | Approval status in Global countries) of this drug. As a small molecule drug, A-72694 is likely to have a low molecular weight and can be easily synthesized in a laboratory setting. Small molecule drugs are typically orally administered and can easily penetrate cell membranes, allowing them to interact with specific targets within the body. Although the drug is still in the preclinical phase, it shows promise for the treatment of asthma by targeting 5-LOX. 5-LOX is an enzyme involved in the production of leukotrienes, which are inflammatory molecules that play a role in asthma pathogenesis. By inhibiting 5-LOX, A-72694 may help reduce inflammation and improve respiratory symptoms in asthma patients. In summary, A-72694 is a small molecule drug developed by Abbott Laboratories that targets 5-LOX for the treatment of asthma. It is currently in the preclinical phase, and further research and development are needed to determine its safety and efficacy in human clinical trials.

12 May 2023

·www.drugs.com

Get Relief With the Most Common Asthma Medications

FRIDAY, May 12, 2023 -- Receiving a diagnosis of asthma may be frightening, but learning what the treatment options are can help alleviate the anxiety that comes with diagnosis. Depending on the severity, certain asthma medications may help you manage your symptoms. Here, experts break down the most common long-term and quick-acting medications for asthma, how they work and potential side effects. Long-term medications These drugs are ones the patient takes daily as a means of controlling asthma and preventing asthma attacks. These can be in pill form or used as inhalers. Bronchodilators: Long-acting beta-2 agonists (LABA) relax the muscle bands around your airway (bronchi), making it easier to get air in and mucus out. These medications for asthma are taken twice a day through an inhaler and last up to 12 hours, according to the Cleveland Clinic . LABA medications should be given with a corticosteroid. (See combination medications below.) The main side effects of LABA medications are nervous or shaky feelings, hyperactivity, overexcitement, increased heart rate, upset stomach and trouble sleeping. Salmeterol (Serevent) Formoterol (Foradil) Long-acting muscarinic antagonists (LAMA) also relax the muscle bands around your airway, the National Heart, Lung, and Blood Institute (NHLBI) says. This asthma medication is used if the steroid/LABA combination doesn’t give enough relief. Do not use this medication if you have glaucoma or are at risk of urinary retention. Tiotropium bromide (Respimat) Theophylline. While not used often, theophylline can be useful in relaxing the airways and preventing reactions to irritants. It is taken as a pill and used for mild asthma symptoms. You may need to have blood tests drawn on a regular basis to make sure the level of medication is correct, the Mayo Clinic says. Side effects are the same as the other bronchodilators, but may also include chest pain or discomfort, dizziness, fainting, increase in urine volume or seizures. Theophylline (Theo-24, Theo-Dur, Slo-Bid, and others) Corticosteroids: Corticosteroids are steroids that reduce inflammation in the airways, according to the NHLBI. They may be taken as a pill, although very few patients are on the pill for long term. It is frequently used in an inhaler, often combined with a LABA. Side effects from the inhaled form are thrush (a mouth infection) and a hoarse voice. Inhaled corticosteroids include: Fluticasone (Flovent HFA, Arnuity Ellipta, others) Budesonide (Pulmicort Flexhaler) Mometasone (Asmanex Twisthaler) Beclomethasone (Qvar RediHaler) Ciclesonide (Alvesco) Combination asthma medications (Corticosteroid and LABA): Fluticasone and salmeterol (Advair) Budesonide and formoterol (Symbicort) Fluticasone and Vilanterol (Breo) Leukotriene modifiers reduce swelling and help keep your airways open for up to 24 hours. According to Mayo Clinic, these medications block the effects of leukotrienes, immune system chemicals that cause asthma symptoms. Side effects are uncommon, but may include nausea, headache, tiredness or diarrhea. Montelukast (Singulair) Zafirlukast (Accolate) Zileuton (Zyflo) Quick-acting asthma medications These are a group of medications that are used when a patient has a flare-up or an asthma attack. Inhaled short-acting beta2-agonists (SABAs) open the airways so air can flow through them during an asthma attack. They start working within 15 to 20 minutes and continue to work for 4 to 6 hours, according to the Cleveland Clinic. Side effects can include tremors, rapid heartbeat, allergic reactions, muscle pain, worsening breathing, dry mouth, headache, sore throat or trouble sleeping. Inhaled forms of SABA medications include: Albuterol (Ventolin) Levalbuterol (Xopenex) Albuterol and ipratropium bromide combination (DuoNeb) Corticosteroids. Oral corticosteroids are usually prescribed for short-term use to help a patient overcome a flare-up. This type of medication quickly reduces swelling and inflammation in the airways. Side effects include: Cataracts, osteoporosis, weight gain, high blood sugar, increased risk of infections, thinning bones and fractures, thin skin, bruising and slower wound healing, mood swings, depression and aggressive behavior. Prednisone (Deltasone, Prednicot, and others ) Methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol) Short-acting anticholinergic bronchodilators help open the airways quickly. This medicine may be less effective than SABAs, but it is an option for people who experience side effects with other medications, the Cleveland Clinic says. Side effects you may experience with these inhalers are dry throat, eyes and nose; unusual taste; nausea and vomiting; or temporary blurred vision if the medicine gets in your eyes. Ipratropium bromide (Atrovent) Tiotropium bromide (Spiriva Respimat) Corticosteroid reliever. In January 2023, the FDA approved Airsupra, which can be used as needed to prevent bronchoconstriction and asthma attacks. In a study conducted before the approval, the risk of severe asthma exacerbation was significantly lower with a fixed-dose combination of albuterol and budesonide than with as-needed use of albuterol alone. Most common side effects are headache, oral yeast infection, cough, and difficulty speaking. Airsupra (albuterol-budesonide) Posted May 2023

Drug Approval

100 Deals associated with Zileuton

External Link

KEGG	Wiki	ATC	Drug Bank
D00414	Zileuton	R	DB00744

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Asthma	United States	Chiesi USA, Inc	09 Dec 1996

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Mild Atopic Dermatitis	Phase 2	United States	Qurient Co., Ltd.	21 Jun 2018
Moderate Atopic Dermatitis	Phase 2	United States	Qurient Co., Ltd.	01 Apr 2015
Severe Atopic Dermatitis	Phase 2	United States	Qurient Co., Ltd.	01 Apr 2015
Asthma chronic	Phase 2	-	Critical Therapeutics, Inc.	01 Sep 2007
Acne Vulgaris	Phase 2	United States	Critical Therapeutics, Inc.	01 Nov 2004
Food Hypersensitivity	Preclinical	United States	Yale School of Medicine	07 Aug 2025

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02348203 (CTgov)	Phase 2	Carcinogenesis \| Tobacco Use Disorder	63	Laboratory Biomarker Analysis+Aspirin+Zileuton (Arm I (Aspirin, Zileuton))	eezizntrss(diksxfjqkv) = gawsuohnbp jxvhjbfrmd (zljtmdoxva, 2.89) View more	-	23 Mar 2020
				Laboratory Biomarker Analysis (Arm II (Double Placebo))	eezizntrss(diksxfjqkv) = jhptyuhqrt jxvhjbfrmd (zljtmdoxva, 2.26) View more
NCT01021215 (CTgov)	Phase 1/2	Tobacco Use Disorder	84	laboratory biomarker analysis+Zileuton (Arm I: Zileuton)	ywbrfptane(grrewydpen) = ajpmhlhcxp itlbovpmet (wyzisrtrko, plwscgsfap - yyezzjbvcg) View more	-	02 Apr 2015
				laboratory biomarker analysis+celecoxib+Zileuton (Arm II: Zileuton and Celecoxib)	ywbrfptane(grrewydpen) = zqzgxlusub itlbovpmet (wyzisrtrko, mthelxwdvo - taaevypths) View more
NCT01805687 (CTgov)	Phase 4	Asthma chronic	25	Zileuton extended release	jbcyqmnxxx(cmetccnrpj) = orftnvmlzy tnafjddxgm (tbgmjwrpvb, 0.706) View more	-	18 Aug 2014
NCT00467831 (CTgov)	Phase 1/2	Hermanski-Pudlak Syndrome \| Pulmonary Fibrosis \| Albinism With Hemorrhagic Diathesis and Pigmented Reticuloendothelial Cells	3	Pravastatin+Erythromycin+N-Acetyl Cysteine+Losartan+Zileuton	lmceuanray = lgbgodtufg yfbthewrlj (mnjfbdngba, uibqsuabjm - rkwvidmbty) View more	-	02 Aug 2013
NCT00493974 (Pubmed \| COPD)	Phase 3	Pulmonary Disease, Chronic Obstructive	119	Zileuton 600 mg	rividakhnf(ujyfokursy) = uzxazuipbi kkeyjueajw (hrzwpvruku ) View more	Negative	01 Feb 2011
				Placebo	rividakhnf(ujyfokursy) = lparpbwgsa kkeyjueajw (hrzwpvruku ) View more
NCT00493974 (LEUKO, CTgov)	Phase 3	Pulmonary Disease, Chronic Obstructive	119	Zileuton (Zileuton)	aswnuvqkaa(etizqzfdnm) = tsienzrqih esvvpuwdyi (cljiaxgrwd, 2.19) View more	-	03 Mar 2010
				Placebo (Placebo)	aswnuvqkaa(etizqzfdnm) = xzkmypopiv esvvpuwdyi (cljiaxgrwd, 3.06) View more
NCT00575861 (Pubmed \| Pulm Pharmacol Ther)	Phase 4	Moderate persistent asthma Add-on	22	Fluticasone 250μg/Salmeterol 50μg	qoefnxkxsj(gnkefymzfv) = uorsmgtmgf wfcqpjoqkk (pqavwbdkxq ) View more	-	01 Dec 2009
				Fluticasone 250μg/Salmeterol 50μg + Zileuton 600mg	qoefnxkxsj(gnkefymzfv) = aissmkzxfm wfcqpjoqkk (pqavwbdkxq ) View more

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