What is Ibudilast?

Ibudilast is an anti-inflammatory and neuroprotective agent. It is a neuroimmune modulator that selectively inhibits phosphodiesterase (PDE) and macrophage inhibitory factor (MIF). In Asia, where it’s clinically used, Ibudilast is marketed as Ketas. [R][R]

Ibudilast was originally developed in Japan in the 1980s for the treatment of bronchial asthma and post-stroke complications. It was later approved by Japan’s Pharmaceuticals and Medical Devices Agency (PMDA) to treat the abovementioned conditions. [R]

In the US and European Union, regulatory agencies (FDA and EMA) have granted orphan drug designation to Ibudilast for treating amyotrophic lateral sclerosis (ALS). The orphan designation is given to medicines that are intended for use against rare conditions. [R]

Clinical trials have reported that the potential benefits of Ibudilast extend beyond the above conditions. For instance, topical application of this small molecule substance improved subjective symptoms in patients with seasonal allergic conjunctivitis. [R]

How does Ibudilast Work?

Here are the proven effects of Ibudilast:

Anti-Inflammatory Effects

Ibudilast exerts its anti-inflammatory effects via the inhibition of the PDE enzyme and regulating the production of pro- and anti-inflammatory cytokines. Let’s take a comprehensive look at the anti-inflammatory effects of this substance: [R]

1) Inhibits phosphodiesterase enzyme

Ibudilast is a non-specific PDE inhibitor, meaning it inhibits the activity of the group of PDE enzymes. This sets it apart from other types of PDE inhibitors. Ones that are more selective in their action, such as cilostazol (PDE-3 inhibitor), roflumilast (PDE-4 inhibitor), and Icariin (PDE-5 inhibitor). [R]

2) Regulates production of pro- and anti-inflammatory cytokines

Ibudilast has also been shown to suppress the production of interleukin (IL)-1 beta and IL-6, which are pro-inflammatory cytokines. Aside from that, it has been found to increase the production of at least one anti-inflammatory cytokine (IL-10). [R]

Neuroprotective Effects

The neuroprotective effects of Ibudilast involve inhibiting nitric oxide synthesis and reducing reactive oxygen species. They also include the increase in the production of neurotrophic factors, such as nerve growth factor (NGF), glia-derived NF (GDNF), and neurotrophin (NT-4). [R]

1) Suppresses nitric oxide synthesis

A cell-based study reported that Ibudilast suppresses nitric oxide synthesis dose-dependently. Enhanced NO biosynthesis may contribute to platelet dysfunction in patients with chronic kidney failure. It may also lead to hemodialysis hypotension. [R][R]

2) Reduces reactive oxygen species

In the above study, Ibudilast administration reduced the levels of reactive oxygen species (ROS) in a dose-dependent manner. Excessive production and levels of ROS can disrupt multiple organs and body processes, ultimately disrupting the body’s normal physiology. [R][R]

3) Enhances production of neurotrophic factors

Another way Ibudilast exerts its neuroprotective effects is by increasing the production of neurotrophic factors in activated microglia. The neurotrophic factors include nerve growth factor (NFG), glia-derived neurotrophic factor (GDNF), and neurotrophin (NT-4). [R]

Ibudilast Research

What follows is a summary of the existing research on Ibudilast. The information given in this section is for educational purposes only. It doesn’t constitute medical advice. Speak to your treating doctor to know more about this macrophage migration inhibiting factor.

Ibudilast and Asthma

Ibudilast has been approved by Japan’s Pharmaceuticals and Medical Devices Agency (PMDA) for the treatment of bronchial asthma.

In a clinical trial involving 13 asthmatics, Ibudilast treatment (20 mg/day) significantly reduced the severity of asthma attacks and improved airway hypersensitivity. No serious adverse reactions were reported in the study. Most common adverse reactions were nausea and abdominal pain. [R]

Another open-label trial in 86 patients reported that Ibudilast treatment yielded clinical benefits at all dose levels. The efficacy outcome measured demonstrated that Ketas Ibudilast didn’t stop asthmatic attacks immediately. [R]

Ibudilast and Opioid Dependence

Data from a clinical study suggest that Ibudilast may be useful for treating opioid use disorders.

The study investigated the effects of Ibudilast on opioid-dependent male subjects. All the participants underwent in-patient detoxification with morphine. Afterward, they were given a placebo and Ibudilast (50 mg/day), followed by oxycodone administration. [R]

Under the 15 mg oxycodone condition, patients who were administered Ibudilast reported reduced ratings of drug liking. Heroin craving was also significantly reduced in the Ibudilast group versus placebo, and similar effects were observed for tobacco and cocaine craving. [R]

Ibudilast and Post Stroke Dizziness

Ibudilast is clinically used in Japan to treat dizziness caused by cerebrovascular disorders (i.e., cerebral infarction). [R]

A placebo-controlled clinical study investigated the hemodynamic effects of Ibudilast in 41 patients with non-insulin-dependent diabetes. Participants were either administered oral Ibudilast (10 mg) or a control. In the Ibudilast group, all the relevant parameters improved. [R]

An open-label trial reported the effects of Ibudilast (30 mg/day) on patients with chronic central vascular disease complaining of dizziness. All patients reported a resolution of dizziness at six months. [R]

Ibudilast and Multiple Sclerosis

According to a phase 2 trial involving patients with multiple sclerosis (MS), Ibudilast was associated with slower progression of brain atrophy than placebo. However, it was associated with higher rates of gastrointestinal side effects, such as vomiting, abdominal pain elevation, etc. [R]

A 2-year double-blind clinical study investigated the effects of Ibudilast (10 – 20 mg) in 297 patients with MS. At the highest dose, Ibudilast significant reduced percent brain volume loss, time to first relapse, disability progression, and probability of new lesions evolving to “black holes”. [R]

Ibudilast and Hay Fever

In a clinical trial involving 69 people with steroid-resistant Ibudilast, the efficacy and safety of loratadine were compared with Ibudilast. [R]

Results from the study show that Ibudilast can effectively alleviate the clinical symptoms and signs of steroid-resistant hay fever. This substance was found to exert a better curative effect than loratadine in improving clinical symptoms and signs. [R]

Ibudilast and Allergic Conjunctivitis

In Japan, Ibudilast is clinically used to treat allergic conjunctivitis. [R]

A clinical study assessed the effects of the topical application of Ibudilast on seasonal allergic conjunctivitis in patients wearing soft contact lenses (SCLs). Among the allergic symptoms, itching and dry sensation improved after the topical application of Ibudilast ophthalmic solution. [R]

FAQs

What are phosphodiesterase inhibitors?

Phosphodiesterase inhibitors are medications that block PDE enzymes to promote blood vessel dilation. This facilitates easy flow of blood through the expanded blood vessels. This action of phosphodiesterase inhibitors also helps lower blood pressure.

What are the side effects of Ibudilast?

In a clinical study of 238 patients affected with post-stroke dizziness, subjects treated with the Ibudilast group reported gastrointestinal distress, hepatic dysfunction, jaundice, and anorexia. In another study, gastrointestinal distress was among the common adverse reactions listed. [R]

Where to Buy Ibudilast Online?

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Summary

Ibudilast is a small molecule with anti-inflammatory and neuroprotective properties. It is used in Japan to treat bronchial asthma and cerebrovascular (brain and blood vessel) disorders, particularly the improvement of post-stroke dizziness.

In clinical trials, it has reduced opioid dependence and alleviated symptoms of hay fever, multiple sclerosis, and allergic conjunctivitis. PureRawz sells Ibudilast for laboratory and research purposes only.