DDInter915 DDInter1329
Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. It is marketed in Europe as Onbrez and in America as Arcapta Neohaler. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
Severe acute pain occurs through nociceptive signalling involving both ascending and descending spinal pathways, in which nerve conductance is mediated in part by the action of opioid receptors.[A218041, A218046] Opioid receptors are seven-transmembrane G-protein-coupled receptors (GPCRs), of which the μ-opioid receptor subtype is predominantly targeted by and is responsible for the effects of opioid agonists.[A218031, A218046] However, due to the ability of some opioid agonists to bind to other targets, as well as activation of additional downstream pathways from opioid receptors such as those involving β-arrestin, the beneficial analgesic effects of opioids are coupled with severe adverse effects such as constipation and respiratory depression.[A218026, A218031, A218036, A218041, A218046] Oliceridine (formerly known as TRV130) is a "biased agonist" at the μ-opioid receptor by preferentially activating the G-protein pathway with minimal receptor phosphorylation and recruitment of β-arrestin.[A218026, A218031] By acting as a biased agonist, oliceridine provides comparable analgesia compared with traditional opioids such as [morphine] at a comparable or decreased risk of opioid-related adverse effects such as constipation and respiratory depression.[A218026, A218031, A218051, A218056, A218061, A218066, A218071, L15516] Oliceridine was first reported in 2013,[A218026, A218086] but was initially not approved by the FDA due to concerns raised by the Anesthetic and Analgesic Drug Products Advisory Committee. Oliceridine gained FDA approval on August 7, 2020, and is currently marketed by Trevena Inc as OLINVYK™.
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is treated by {v} (Compound) Dexamethasone
Dexamethasone {u} may lead to a major life threatening interaction when taken with {v} Oliceridine
Indacaterol {u} (Compound) binds {v} (Gene) ADRB1
ADRB1 {u} (Gene) is bound by {v} (Compound) Formoterol
Formoterol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is treated by {v} (Compound) Salbutamol
Salbutamol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol {u} (Compound) binds {v} (Gene) ABCB1
ABCB1 {u} (Gene) is bound by {v} (Compound) Clarithromycin
Clarithromycin {u} may lead to a major life threatening interaction when taken with {v} Oliceridine
Indacaterol {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Metronidazole
Metronidazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Oliceridine
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is upregulated by {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol {u} (Compound) is included by {v} (Pharmacologic Class) Adrenergic beta2-Agonists
Adrenergic beta2-Agonists {u} (Pharmacologic Class) includes {v} (Compound) Salbutamol
Salbutamol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Bosutinib
Bosutinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Metronidazole
Metronidazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Oliceridine
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is downregulated by {v} (Compound) Dasatinib
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is treated by Dexamethasone (Compound) and Dexamethasone may lead to a major life threatening interaction when taken with Oliceridine
Indacaterol (Compound) binds ADRB1 (Gene) and ADRB1 (Gene) is bound by Formoterol (Compound) and Formoterol may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is treated by Salbutamol (Compound) and Salbutamol may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Indacaterol (Compound) binds ABCB1 (Gene) and ABCB1 (Gene) is bound by Clarithromycin (Compound) and Clarithromycin may lead to a major life threatening interaction when taken with Oliceridine
Indacaterol (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Metronidazole (Compound) and Metronidazole may cause a minor interaction that can limit clinical effects when taken with Oliceridine
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is upregulated by Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Indacaterol (Compound) is included by Adrenergic beta2-Agonists (Pharmacologic Class) and Adrenergic beta2-Agonists (Pharmacologic Class) includes Salbutamol (Compound) and Salbutamol may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Bosutinib (Compound) and Bosutinib may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Metronidazole (Compound) and Metronidazole may cause a minor interaction that can limit clinical effects when taken with Oliceridine
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is downregulated by Dasatinib (Compound) and Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine