Fluticasone furoate, sold under the brand name Flonase Sensimist among others, is a corticosteroid for the treatment of non-allergic and allergic rhinitis administered by a nasal spray. It is also available as an inhaled corticosteroid to help prevent and control symptoms of asthma. It is derived from cortisol. Unlike fluticasone propionate, which is only approved for children four years and older, fluticasone furoate is approved in children as young as two years of age when used for allergies. It was approved for medical use in the United States in April 2007, and in the European Union in November 2008. In 2021, fluticasone was the 23rd most commonly prescribed medication in the United States, with more than 25million prescriptions.

Medical uses

Fluticasone furoate is indicated for the treatment of the symptoms of allergic rhinitis, and asthma. Fluticasone Furoate is a corticosteroid medication primarily used to treat allergic rhinitis (hay fever) and non-allergic (perennial) rhinitis. It is also indicated for the treatment of nasal polyps in adults. Additionally, fluticasone furoate nasal spray may be prescribed for the management of symptoms associated with sinusitis. Always consult with a healthcare professional for accurate diagnosis and appropriate treatment options. Fluticasone furoate nasal spray is highly effective in relieving symptoms of allergic rhinitis, including nasal congestion, runny nose, sneezing, and nasal itching. It works by reducing inflammation in the nasal passages and decreasing the production of mucus. Fluticasone Furoate is used as a maintenance treatment for asthma in patients aged 12 years and older. It helps to reduce inflammation in the airways, which is a key component of asthma management. It helps to control symptoms such as wheezing, shortness of breath, chest tightness, and coughing, thereby improving the overall quality of life for individuals with asthma. Regular use of Fluticasone Furoate can reduce the frequency and severity of asthma exacerbations or attacks, helping to prevent serious episodes of breathing difficulty. When used as an inhaler, Fluticasone furoate helps to control asthma symptoms by reducing airway inflammation and preventing asthma attacks. It is often used as a maintenance treatment to provide long-term control of asthma symptoms and improve lung function.

Available forms

Side effects

Serious side effects of Fluticasone Furoate include: It's essential to use Fluticasone furoate as directed by a healthcare professional to maximize its benefits and minimize the risk of side effects. If you experience any concerning side effects while using Fluticasone furoate, it's important to consult your doctor for further evaluation and management.

Interactions

Fluticasone Furoate has serious interactions with the following drugs: Fluticasone Furoate has moderate interactions with at least 45 other drugs.

Toxicity

The toxicity of Fluticasone furoate is primarily associated with excessive or prolonged use, especially at high doses. While Fluticasone furoate is generally considered safe when used according to prescribed guidelines, long-term or improper use can lead to various adverse effects.

Pharmacology

Mechanism of action

The mechanism of action of Fluticasone furoate, like other corticosteroids, involves its binding to glucocorticoid receptors within cells.

Pharmacokinetics

The pharmacokinetics and metabolism of Fluticasone furoate involve its absorption, distribution, metabolism, and elimination from the body.

History

Fluticasone furoate or (FF) was discovered by researchers at GlaxoSmithKline, also known as (GSK), and Theravance, Inc. (NASDAQ: THRX). Research first began in 2006, however, its final phases of research began conclusion from the 6th December 2013 and into 2014. Dave Allen, Head, Respiratory Therapy Area Unit, R&D said, “We are pleased to see the results delivered by FF/VI in the treatment of asthma. We have undertaken a large and comprehensive clinical programme providing data on the efficacy and safety profile for FF/VI in asthma. With these additional data we will consider our next steps in relation to an asthma filing in the US.” on 6 December 2013. Dave Allen is responsible for the identification of novel differentiated medicines and their progression to registration and launch at GlaxoSmithKline (GSK). He leads a group of over 200 scientists and clinicians who exploit scientific innovations that have the potential to address the major unmet needs in diseases such as COPD, severe asthma, acute lung injury and idiopathic pulmonary fibrosis. Also noted in the 6th of December 2013 press release from GlaxoSmithKline (GSK), “There is an ongoing unmet medical need among patients with asthma,” said Rick E Winningham, Chief Executive Officer of Theravance. “This is an important outcome for FF/VI and we will continue working with GSK to determine how we can make this potential treatment available to appropriate patients who could benefit from a new asthma medicine.” Fluticasone furoate is most commonly known for its form combinations vilanterol trifenate, known as Fluticasone furoate/vilanterol (FF/VI) for its treatment of bronchospasms for COPD ( Chronic Obstructive Pulmonary Disease ). GlaxoSmithKline announced on 20 August 2014 that the Food and Drug Administration (FDA) as approved Arnuity™ Ellipta® (fluticasone furoate inhalation powder) for use in The United States of America, a once-daily inhaled corticosteroid (ICS) medicine for maintenance treatment of asthma as prophylactic therapy in patients aged 12 years and older. Arnuity is not indicated for relief of acute bronchospasm. GSK Australia and Theravance, Inc. (NASDAQ: THRX) announced today that the Therapeutic Goods Administration (TGA) has approved BREO® ELLIPTA® (fluticasone furoate/vilanterol [FF/VI]) on the 22nd April 2014, for the treatment of patients with asthma or chronic obstructive pulmonary disease (COPD) in Australia. FF/VI was approved by the FDA for sale as BREO® ELLIPTA® (fluticasone furoate/vilanterol [FF/VI]) on the 30th April 2015 for use in The United States of America, for the once-daily treatment of asthma in patients aged 18 years and older. Breo Ellipta is not indicated for the relief of acute bronchospasm.

Drug class

Fluticasone Furoate falls under the drug class of Corticosteroid. Corticosteroids are a class of steroid hormones produced naturally by the adrenal cortex, which is located on top of the kidneys. They play a crucial role in regulating various physiological processes in the body, including metabolism, immune response, and inflammation. Corticosteroids can also refer to synthetic drugs that mimic the actions of these natural hormones. There are two main types of corticosteroids: glucocorticoids and mineralocorticoids. Glucocorticoids, such as cortisol, are involved in regulating metabolism and suppressing inflammation. They have anti-inflammatory and immunosuppressive properties, making them useful in the treatment of conditions like asthma, arthritis, and autoimmune diseases. Mineralocorticoids, such as aldosterone, primarily regulate electrolyte and fluid balance in the body. Synthetic corticosteroids, like prednisone, dexamethasone, and fluticasone, are commonly used in medicine to reduce inflammation and suppress immune responses in conditions such as allergies, asthma, rheumatoid arthritis, and inflammatory bowel disease. They are available in various forms, including oral tablets, inhalers, creams, and injections, depending on the specific condition being treated and the desired route of administration.

Chemistry

Fluticasone furoate contains fluorine atoms at specific positions on the steroid nucleus. These fluorinated substituents enhance the molecule's potency and duration of action. The furoate ester group is attached at position 17 of the steroid nucleus. This ester group contributes to the molecule's lipophilicity, which affects its absorption and distribution in the body. Fluticasone furoate has a side chain attached at position 17 of the steroid nucleus. This side chain plays a crucial role in determining the molecule's selectivity and potency. Molecular Formula: C27H29F3O6S Molecular Weight : 538.6 g/mol

Reactivity

Fluticasone furoate, like other corticosteroids, exhibits specific chemical reactivity characteristics based on its structure. Based on its chemical structure, which includes a corticosteroid backbone with a fluorine substitution pattern, Fluticasone furoate might exhibit some reactivity typical of compounds with such structures, such as:

Synthesis

"a solution of Compound II in butanone with DMAP and tripropylamine is treated with furoyl chloride to obtain Compound III, which is then treated with N-methylpiperazine to de-fluoridize to obtain Compound IV. Compound IV is reacted with a fluoromethylating reagent to obtain the fluticasone furoate of Compound I".

Additional Information

Fluticasone furoate, sold under the brand name Flonase Sensimist among others, is a corticosteroid for the treatment of non-allergic and allergic rhinitis administered by a nasal spray. It is also available as an inhaled corticosteroid to help prevent and control symptoms of asthma. It is derived from cortisol. Unlike fluticasone propionate, which is only approved for children four years and older, fluticasone furoate is approved in children as young as two years of age when used for allergies. It was approved for medical use in the United States in April 2007, and in the European Union in November 2008. In 2021, fluticasone was the 23rd most commonly prescribed medication in the United States, with more than 25million prescriptions.

Society and culture

Brand names

In the US it is marketed by GlaxoSmithKline for asthma as Arnuity Ellipta and is only available with a prescription. It is sold over-the-counter for allergic rhinitis as Flonase Sensimist. The Veramyst brand name was discontinued in the US. The combination drugs fluticasone furoate/umeclidinium bromide/vilanterol, marketed as Trelegy Ellipta, and fluticasone furoate/vilanterol, marketed as Breo Ellipta (US, Canada, New Zealand) and Relvar Ellipta (EU, UK), are approved for use in the United States for long-term maintenance treatment of airflow obstruction in people with chronic obstructive pulmonary disease (COPD). They are also approved for the treatment of asthma. The combination fluticasone propionate/salmeterol (Advair Diskus) is indicated for the treatment of asthma and chronic obstructive pulmonary disease.