resomelagon

Action and Spectrum

Actions and Spectrum: 

Actions: 

Resomelagon exhibits dual pharmacological effects in cells. In HEK293A cells, concentrations from 0 to 1000 μM rapidly induce melanocortin signal transduction, triggering ERK1/2 phosphorylation and Ca2+ mobilization within 8 minutes. Simultaneously, at 1 nM for 30 minutes in peritoneal macrophages, Resomelagon demonstrates anti-inflammatory properties by inhibiting TNF-α release and impeding efferocytosis. These findings underscore Resomelagon’s potential to activate melanocortin signaling pathways and mitigate inflammatory responses, highlighting its relevance for therapeutic interventions targeting inflammatory conditions. 

Spectrum: 

Resomelagon appears to exhibit dual pharmacological actions, notably promoting melanocortin signal transduction and demonstrating anti-inflammatory effects, as indicated in earlier responses. The promotion of melanocortin signal transduction involves actions like ERK1/2 phosphorylation and Ca2+ mobilization, while its anti-inflammatory properties include inhibiting the release of TNF-α and hindering efferocytosis. However, for a comprehensive understanding of its broader spectrum of activity, including interactions with various molecular targets and potential applications in different disease contexts, it is essential to consult more recent scientific literature, delve into clinical studies, or obtain information from the pharmaceutical company responsible for the development of Resomelagon. 

Resomelagon is currently in the developmental stages with a focus on treating a range of systemic inflammatory diseases, including systemic lupus erythematosus, psoriatic arthritis, nephrotic syndrome, rheumatoid arthritis, peritonitis, inflammatory bowel diseases, multiple sclerosis, and acute respiratory distress syndrome (ARDS) associated with COVID-19. The drug candidate is administered orally, making it a convenient option for patients. Chemically, Resomelagon is a phenyl pyrrole aminoguanidine derivative known as AP-1189, and it exhibits potent anti-inflammatory properties. Its mechanism of action involves acting as a positive allosteric modulator (PAM) of the melanocortin receptors, suggesting a targeted approach to regulating these receptors to mitigate inflammatory responses. As research and development progress, Resomelagon holds promise as a potential therapeutic intervention for a diverse range of inflammatory conditions, offering hope for improved treatment options in the future. 

Drug Interaction

Adverse Reaction

Actions and Spectrum:  

Resomelagon has anti-inflammatory properties which inhibits TNF-α release and impedes efferocytosis.  

Black Box Warning

Black box warning  

None  

Contraindication / Caution

Contraindication/Caution:  

Contraindications  

• Hypersensitivity  

Cautions  

• Renal impairment  
• Hepatic impairment  
• Pregnancy   

Pregnancy / Lactation

Pregnancy Warnings: 

Pregnancy category: N/A 

Lactation: Excretion of the drug into the human breast milk is unknown 

Pregnancy categories: 

• Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester. 
• Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology:  

Resomelagon activates melanocortin signaling pathways and mitigating inflammatory responses which shows its significance in therapeutic interventions targeting inflammatory conditions.  

Pharmacodynamics:  

Limited information is available.  

Pharmacokinetics:  

Limited information is available on ADME.  

Adminstartion

Administration:  

The route of administration is not fully known.  

Patient Information Leaflet

Patient information leaflet  

Generic Name: resomelagon  

Why do we use resomelagon?  

Resomelagon is under the investigation stage for the treatment of inflammatory diseases including systemic lupus erythematosus, psoriatic arthritis, nephrotic syndrome, rheumatoid arthritis, peritonitis, and inflammatory bowel diseases.