Salbutamol, also known as albuterol and sold under the brand name Ventolin among others, is a medication that opens up the medium and large airways in the lungs. It is a short-acting β2 adrenergic receptor agonist that causes relaxation of airway smooth muscle. It is used to treat asthma, including asthma attacks and exercise-induced bronchoconstriction, as well as chronic obstructive pulmonary disease (COPD). It may also be used to treat high blood potassium levels. Salbutamol is usually used with an inhaler or nebulizer, but it is also available in a pill, liquid, and intravenous solution. Onset of action of the inhaled version is typically within 15 minutes and lasts for two to six hours.
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth muscle cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin. They are primarily used to treat asthma and other pulmonary disorders. Bronchodilators are considered an important treatment regime for chronic obstructive pulmonary disease (COPD) and are usually used in combination with short acting medications and long acting medications in a combined inhaler.
Isoprenaline, also known as isoproterenol and sold under the brand name Isuprel among others, is a sympathomimetic medication which is used in the treatment of acute bradycardia, heart block, and rarely for asthma, among other indications. It is used by injection into a vein, muscle, fat, or the heart, by inhalation, and in the past under the tongue or into the rectum.
Long-acting β adrenoceptor agonists (LABAs) are beta-adrenergic agonists usually prescribed for moderate-to-severe persistent asthma and chronic obstructive pulmonary disease (COPD).
Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Evidence is inconclusive regarding the efficacy of levosalbutamol versus salbutamol or salbutamol-levosalbutamol combinations, though levosalbutamol is believed to have a better safety profile due to its more selective binding to β2 receptors versus β1.
Ritodrine, sold under the brand name Yutopar, is a tocolytic drug used to stop premature labor. This drug has been removed from the US market, according to FDA Orange Book. It was available in oral tablets or as an injection and was typically used as the hydrochloride salt.
Lumiliximab is an IgG1k monoclonal antibody that targets CD23. It acts as an immunomodulator and was awarded orphan drug status and fast track designation by the FDA.
The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (HCRTR1, HCRTR2).
Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways and resulting in easier breathing. They are a class of sympathomimetic agents, each acting upon the beta adrenoceptors. In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands mimic the actions of both epinephrine- and norepinephrine- signaling, in the heart and lungs, and in smooth muscle tissue; epinephrine expresses the higher affinity. The activation of β1, β2 and β3 activates the enzyme, adenylate cyclase. This, in turn, leads to the activation of the secondary messenger cyclic adenosine monophosphate (cAMP); cAMP then activates protein kinase A (PKA) which phosphorylates target proteins, ultimately inducing smooth muscle relaxation and contraction of the cardiac tissue.
Bradanicline is a drug which was being developed by Targacept that acts as a partial agonist at the α7 subtype of the neural nicotinic acetylcholine receptors. It showed cognitive enhancing effects in animal studies, and was being developed through a collaboration between Targacept and AstraZeneca as a potential treatment for schizophrenia and attention deficit disorder. Phase I clinical trials were completed successfully, and it was in phase II trials.
Tralokinumab sold under the brand names Adtralza (EU/UK) and Adbry (US) among others, is a human monoclonal antibody used for the treatment of atopic dermatitis. Tralokinumab targets the cytokine interleukin 13.
Namilumab is a human monoclonal antibody that targets granulocyte macrophage-colony stimulating factor (GM-CSF)/colony stimulating factor 2 (CSF2) and is currently being researched for application in rheumatoid arthritis (RA) and psoriatic arthritis. Clinical trials investigating the therapeutic utility of Namilumab have include phase I and phase II clinical trials to establish the safety, tolerability and preliminary therapeutic utility of the antibody in plaque psoriasis and rheumatoid arthritis.
Olodaterol is an ultra-long-acting β adrenoreceptor agonist (ultra-LABA) used as an inhalation for treating people with chronic obstructive pulmonary disease (COPD). It is manufactured by Boehringer Ingelheim.
β2-adrenoceptor agonists are a group of drugs that act selectively on β2-receptors in the lungs causing bronchodilation. β2-agonists are used to treat asthma and COPD, diseases that cause obstruction in the airways. Prior to their discovery, the non-selective beta-agonist isoprenaline was used. The aim of the drug development through the years has been to minimise side effects, achieve selectivity and longer duration of action. The mechanism of action is well understood and has facilitated the development. The structure of the binding site and the nature of the binding is also well known, as is the structure activity relationship.
Sufotidine (INN, USAN, codenamed AH25352) is a long-acting competitive H2 receptor antagonist which was under development as an antiulcerant by Glaxo (now GlaxoSmithKline). It was planned to be a follow-up compound to ranitidine (Zantac). When taken in doses of 600 mg twice daily it induced virtually 24-hour gastric anacidity thus closely resembling the antisecretory effect of the proton pump inhibitor omeprazole. Its development was terminated in 1989 from phase III clinical trials based on the appearance of carcinoid tumors in long-term toxicity testing in rodents.
Carmoterol is a non-catechol experimental ultra-long-acting β adrenoreceptor agonist (ultra-LABA) that was in clinical trials before 2010 when it has been withdrawn from further development based on evidence that the compound does not possess a competitive profile.
PF-610355 is an inhalable ultra-long-acting β2 adrenoreceptor agonist (ultra-LABA) that was investigated as a treatment of asthma and COPD by Pfizer. It utilizes a sulfonamide agonist headgroup, that confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties minimized systemic exposure following inhalation and reduced systemically mediated adverse events. Its in vivo duration on action confirmed its potential for once-daily use in humans.
Ralmitaront is an investigational antipsychotic drug which is undergoing a clinical trial for the treatment of negative symptoms in schizophrenia and schizoaffective disorder. Another clinical trial targeting acute psychotic symptoms of schizophrenia has been terminated due to lack of efficacy. It is a partial agonist of the TAAR1. The medication is being developed by the pharmaceutical company Hoffmann-La Roche. Ralmitaront had completed phase 1 clinical trials.
Suntinorexton (INNTooltip International Nonproprietary Name; developmental code name TAK-861) is an experimental orexin receptor agonist. It acts as a selective agonist of the orexin OX2 receptor and was described in 2019 in a patent by Takeda Pharmaceutical Company. Suntinorexton superseded firazorexton (TAK-994) as a clinical drug candidate following evidence of hepatoxicity in humans. The drug has reached phase 3 clinical trials as of 2024. It is orally active and centrally penetrant.
Bedoradrine is a sympathomimetic and bronchodilator medication that was developed for the treatment of preterm labor, asthma, and chronic obstructive pulmonary disease (COPD) but was never marketed. It acts as an ultra-selective long-acting β2-adrenergic receptor agonist. The drug was intended for intravenous administration.
