What is a PDE4 inhibitor?
A PDE4 inhibitor is a type of drug that blocks the degradative action of an enzyme called phosphodiesterase 4 (PDE4) on a molecule known as cyclic adenosine monophosphate (cAMP)1. PDE4 is the most prevalent phosphodiesterase in immune cells1.
Here’s a bit more detail:
- How They Work: PDE4 inhibitors prevent PDE4 from breaking down cAMP in cells2. This leads to an increase in cAMP levels, which in turn decreases the levels of calcium in the cell2. The result is vasodilation and smooth muscle relaxation in their target tissues2.
- Therapeutic Utility: PDE4 inhibitors are known to possess procognitive, wakefulness-promoting, neuroprotective, and anti-inflammatory effects1. They have been investigated as treatments for a diverse group of diseases, including central nervous system disorders such as major depressive disorder, anxiety disorders, schizophrenia, Parkinson’s disease, Alzheimer’s disease, multiple sclerosis, attention deficit-hyperactivity disorder, Huntington’s disease, stroke, autism and inflammatory conditions such as chronic obstructive pulmonary disease (COPD), asthma and rheumatoid arthritis1.
- Adverse Reactions: The most commonly reported side effects of PDE4 inhibitors are nausea, vomiting, and related general gastrointestinal side effects1.
- Applications: PDE4 inhibitors are used in the treatment of diseases like psoriasis and certain lung diseases by lowering and managing inflammation3. They also suppress the immune system, which reduces inflammation4.
Bing AI…
What is good about this PDE4 is that this Alto is a transdermal patch and so doesn’t affect the gastro side effects while being more effective in this study.
Yes, ALTO-101 is indeed a transdermal patch 13. It’s a novel PDE4 inhibitor being developed by Alto Neuroscience for the treatment of cognitive impairment associated with schizophrenia (CIAS)13.
The transdermal delivery system (TDS) of ALTO-101 has shown favorable tolerability and improved pharmacokinetics compared to oral administration13. The study demonstrated that ALTO-101, when administered through a transdermal delivery system, had a favorable tolerability and improved pharmacokinetics compared to oral administration13.
This means that the drug is delivered through the skin, which can offer several advantages such as improved patient compliance, continuous drug delivery, and fewer adverse events typically associated with PDE4 inhibitors13. The transdermal formulation of ALTO-101 is being developed in partnership with MEDRx22.