Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Development Status

US Approved Rx

3

Other

1

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

Beta-2 adrenergic receptor

2

Glucocorticoid receptor

1

Progesterone receptor

1

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

3

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

2006

2

1990

1

Unknown

1

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Chronic obstructive pulmonary disease

2

Corticosteroid-responsive dermatoses

1

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Palliative

2

Primary

1

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Penetrant

1

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Sepracor

2

Glaxo Wellcome

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

4

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

4

EPA CompTox

4

FDA UNII

4

PUBCHEM

4

ChEMBL

3

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Principal Form

3

Salts, Hydrates, Esters, etc.

1

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 4 of 4 results

First page disabled
Previous page disabled
1
Next page disabled
Next page disabled

Arformoterol

F91H02EBWT

Export Data
Search for Structure

Status:

US Approved Rx (2021)

First approved in 2006

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Beta-2 adrenergic receptor

Conditions:

Chronic obstructive pulmonary disease

Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral canters and is being developed as an inhaled preparation for the treatm...

ent of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.

FLUTICASONE PROPIONATE

O2GMZ0LF5W

Export Data
Search for Structure

Status:

US Approved Rx (2000)

First approved in 1990

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Progesterone receptor

Glucocorticoid receptor

Conditions:

Corticosteroid-responsive dermatoses

Fluticasone propionate, a medium-potency synthetic corticosteroid, is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis, intranasally to manage symptoms of allergic and non-allergic rhinitis, and orally for the ...

treatment of asthma. Fluticasone proprionate is marketed under several different brand names such as Flonase®. Fluticasone propionate is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patients over 12 years old for symptomatic relief of seasonal allergic rhinitis. Fluticasone propionate binds to the glucocorticoid receptor. Unbound corticosteroids cross the membranes of cells such as mast cells and eosinophils, binding with high affinity to glucocorticoid receptors (GR). The results include alteration of transcription and protein synthesis, a decreased release of leukocytic acid hydrolases, reduction in fibroblast proliferation, prevention of macrophage accumulation at inflamed sites, reduction of collagen deposition, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability and subsequent edema, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. In the management of asthma, the glucocorticoid receptor complexes down-regulates proinflammatory mediators such as interleukin-(IL)-1, 3, and 5, and up-regulates anti-inflammatory mediators such as IkappaB [inhibitory molecule for nuclear factor kappaB1], IL-10, and IL-12. The antiinflammatory actions of corticosteroids are also thought to involve inhibition of cytosolic phospholipase A2 (through activation of lipocortin-1 (annexin)) which controls the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

N-(2-HYDROXY-5-((1S)-1-HYDROXY-2-(((1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL)AMINO)ETHYL)PHENYL)FORMAMIDE

ZP145530CI

Export Data
Search for Structure

Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Arformoterol Tartrate

5P8VJ2I235

Export Data
Search for Structure

Status:

US Approved Rx (2021)

First approved in 2006

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Beta-2 adrenergic receptor

Conditions:

Chronic obstructive pulmonary disease

Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral canters and is being developed as an inhaled preparation for the treatm...

ent of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1