Most New Asthma Medicines Just Reformulations?

We asthmatics are very thankful for all the medicinal options currently available to help us treat and control asthma. Still, most newer asthma medicines are just reformulations to improve existing treatments, resulting in new patents and higher prices?

According to Dictionary.com: reformulate means “to formulate in a different way; alter or revise.” For the sake of this article, I will focus on inhaled medicine. Reformulate could mean a tweak to the formula, adding a new propellant, or even combining two older formulas.

Think about this for a second. Epinephrine was discovered in 1901, and was readily available for inhalation by the 1930s. Okay, so this means asthma rescue medicine is not new.

Granted, the side effects of epinephrine were rather significant, including hypertension, a pounding heartbeat, jitteriness, and tremors. Plus the effects only lasted 1-1.5 hours. The inspired scientists to play with the molecule, tweaking it ever so slightly, to come up with a better rescue medicine. The first reformulation was introduced as isopreterenol (Isuprel) in 1948. It had the same rescue effect as epinephrine without the side effect of hypertension.

A new formula means a new patent, and a new patent means a higher price.

Granted, the side effects of isopreterenol were rather significant, including pounding heartbeat, jitteriness, and tremors. Plus, like epinephrine, the effects only lasted only 1-1.5 hours. This inspired scientists to play with the molecule, tweaking it ever so slightly, to come up with a better rescue medicine. Another reformulation was introduced as metraproterenol (Alupent) in 1973. It had the same rescue effect as isopreterenol, although its effects lasted 4-6 hours.

A new formula means a new patent, and a new patent means a higher price.

Granted, the side effects of metraproterenol were still rather significant, including a pounding heartbeat, jitteriness and tremors. This inspired researchers to continue the quest to find a safer rescue medicine. Another reformulation was introduced as albuterol (Ventolin) in 1982. It had the same rescue effect as metraproterenol without the strong cardiac effect.

A new formula means a new patent, and a new patent means a higher price.

Granted, while the side effects of albuterol were considered negligible, it could have some effect on the heart, and cause jitteriness and tremors. This inspired researchers to continue the quest to find a better asthma rescue medicine. Another reformulation was introduced as levalbuterol (Xopenex) in 1999. It had the same rescue effect as albuterol with even fewer side effects.

A new formula means a new patent, and a new patent means a higher price.

Get the picture.

Continued efforts  to tweak the formula lead to the introduction of salmeterol (Serevent) in 1994. This was the first long-acting bronchodilator (LABA), keeping airways open up to 12 hours. It offered yet another option for asthmatics. Hold on to this thought a moment.

Now, let’s move on to corticosteroids. They were introduced during the 1950s and found to reduce and control airway inflammation. The first inhaled corticosteroids were introduced as beclomethasone (Vanceril) in 1982 and then budesonide (Pulmicort). A daily regime of one of these helped asthmatics control and prevent asthma.

Granted, the effects of these only lasted four hours. So, the formula was tweaked again, resulting in fluticasone (Flovent) in 1996 and mometasone (Azmanex) in 2008. The effects lasted up to 12 hours, meaning only two doses per day.

A new formula means a new patent, and a new patent means a higher price.

Now, back to LABAs.  Asthma experts decided they should only be taken in conjunction with an inhaled corticosteroid to control asthma. So salmeterol and fluticasone were combined and rebranded as  Advair in 2000.

A new formula means a new patent, and a new patent means a higher price.

“Great idea,” thought the other pharmaceuticals. So, the LABA formoterol was combined with budesonide in a new inhaler device and called Symbicort in 2006. So, formoterol was combined with mometasone in a new inhaler device and called Dulera in 2010.

A new formula means a new patent, and a new patent means a higher price.

The patent for Advair was set to expire. No worry, because a new formulation of salmeterol resulted in vilanterol. It was combined with a new formulation of fluticasone, and Breo was introduced. The medicine required only one daily puff. Many similar combination inhalers are in the pipeline. You may even see triple inhalers soon.

A new formula means a new patent, and a new patent means a higher price.

The patents for beclomethasone and albuterol expired long ago, resulting in lower prices. No worry, the old propellant was banned by the EPA, and this allowed scientists to add a new propellant to the formula. Albuterol is the same old medicine. So is beclomethasone, although it’s formula was tweaked slightly so it lasts 12 hours. It was rebranded as Qvar.

A new formula means a new patent, and a new patent means a higher price.
We asthmatics are very thankful for all of these products to help us treat, prevent and control asthma — not so much the prices. We now wait for the next big discovery, the next major breakthrough that leads to another whole new line of medicines, preferably something that gets to the root cause of our disease. This may already be on the way. Stay tuned!

This article represents the opinions, thoughts, and experiences of the author; none of this content has been paid for by any advertiser. The Asthma.net team does not recommend or endorse any products or treatments discussed herein. Learn more about how we maintain editorial integrity here.

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