Glucocorticoid Receptor Agonist Market: Competitive Landscape, Pipeline, and Market Analysis 2024

The glucocorticoid receptor (GR, or GCR), also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1), is the receptor to which cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response. GCR Agonist drugs act by binding the glucocorticoid agonist, which induces a conformational change in the glucocorticoid receptor, leading to its activation. This activated receptor-ligand complex is then translocated into the nucleus. In the nucleus, the activated glucocorticoid receptor binds to specific DNA sequences known as glucocorticoid response elements (GREs) located in the regulatory regions of target genes, and once bound to the GREs, the activated glucocorticoid receptor complex interacts with other proteins and transcriptional co-regulators resulting in the recruitment of transcriptional machinery and the modulation of gene expression which will lead to the upregulation or downregulation of specific target genes.

GCR Agonist treats asthma, respiratory tract diseases, lung diseases, digestive system diseases, dermatitis, rhinitis, autoimmune disorders, and skin diseases. Increased prevalence of respiratory tract infections and allergic rhinitis are the key drivers for the GCR agonist market. For instance, according to the Centers for Disease Control and Prevention 2021, around there were 4.6% of adults who have ever been diagnosed with COPD, emphysema, or chronic bronchitisThe introduction of newer products by market players may look for opportunities that greatly impact comprehensive research and development in GCR Agonist inhibitors. For instance, AstraZeneca launched Breztri Aerosphere to treat COPD. For instance, GSK’s GSK870086 Inhalation for the indication of Asthma is under the various stages of clinical studies.

Key Market Developments:

• In July 2020, AstraZeneca received FDA approval for the Breztri Aerosphere (Budesonide/Glycopyrrolate/Formoterol Fumarate) for the maintenance treatment of patients with chronic obstructive pulmonary disease.
• In September 2020, GlaxoSmithKline received FDA grant for the expanded indication of Trelegy Ellipta (Fluticasone Furoate/Umeclidinium/Vilanterol) for the maintenance treatment of asthma in adults.

Approved Drug Molecules and Brand Names for GCR Agonist: 

• Breztri Aerosphere (Budesonide/Glycopyrrolate/Formoterol Fumarate)
• Trelegy Ellipta (Fluticasone Furoate/Umeclidinium/Vilanterol)
• Breo Ellipta (Fluticasone Furoate And Vilanterol Inhalation Powder)
• Alvesco (Ciclesonide)
• Arnuity Ellipta (Fluticasone Furoate Inhalation Powder)
• Dulera (Mometasone Furoate + Formoterol Fumarate Dihydrate)

Drugs under the Pipeline for GCR Agonist:

• GSK870086 Inhalation
• AZD5423
• Budenofalk Granules (Budesonide Gastro-Resistant Granules)
• Tri-Luma (Fluocinolone /Hydroquinone/Tretinoin)
• Xhance (Fluticasone Propionate Intranasal Spray)
• Budesonide (MAP0010)
• Dexamethasone Sodium Phosphate-Loaded RBC (EDS-EP)
• Dexamethasone Sustained-Release (TLC599)
• Triamcinolone Acetonide + Anti-VEGF (CLS-1003)
• Jorveza (Budesonide Orodispersible Tablets)
• Synavive (Prednisolone
• Salbutamol
• Cortone (Cortisone Acetate)
• Neofordex (Dexamethasone Acetate High-Dose)
• Budesonide Inhalation (VR647)
• Dexamethasone Cyclodextrin Nanoparticle Ophthalmic Suspension (OCS-01)
• Aerospan (Flunisolide HFA)
• BI 653048
• HM15136
• Semdexa (Dexamethasone)
• Budesonide Inhalation Solution (AQ001S)
• Fluticasone Propionate Controlled Release (EP-104)
• Fluticasone
• Mometasone Fuorate (LYR-210)

Clinical Activity and Developments of GCR Agonist:

Up until July 2023, there will be about more than 70 companies with over 100 compounds that focus on various forms of respiratory diseases, and skin diseases. For these molecules, more than 1600 of clinical trials are being conducted and majority are in phase-2, phase-3 clinical trials by the players across the globe. For instance,

• In August 2022, Galderma has completed phase 4, an assessment of the atrophogenic potential of Tri-Luma (Fluocinolone /Hydroquinone/Tretinoin) triple combination cream using histology measures in the treatment of moderate to severe melasma.
• In March 2022, Taiwan Liposome Company has completed phase 3, randomized, double-blind, placebo- and active-controlled study to evaluate the efficacy and safety of TLC599 in patients with osteoarthritis of the knee.