Apremilast, a replacement for Methotrexate?

Apremilast, a replacement for Methotrexate?

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It’s always nice to have a new medication for a difficult-to-treat disease.

Psoriatic arthritis can be a frustrating disease to control effectively (read My Lack of Options with Psoriatic Arthritis).

Australian rheumatologists have had an opportunity to use Apremilast (Otezla). The medication is not reimbursed by our government bodies but Celgene, the pharmaceutical company made it available (in limited numbers over a limited time period) via a patient familiarisation program.

Apremilast works by blocking an enzyme called phosphodiesterase 4. This then reduces the amount of a protein called cyclic AMP being broken down by the enzyme. Cyclic AMP tends to be anti-inflammatory, so keeping it at higher levels helps to decrease some pro-inflammatory cytokines (eg tumour necrosis factor and interleukin 6) and increases other anti-inflammatory cytokines (eg interleukin 10).

It’s the 1st new oral disease-modifying agent for Psoriasis and Psoriatic Arthritis in decades.

I’m using it in 8 patients currently and my early thoughts is that it has been quite useful. 

  • It’s oral, and some patients really prefer this over injections.
  • It’s well tolerated. A few patients have had gastrointestinal side effects such as loose bowel motions, nausea and bloating but the symptoms were mild and improved over time. None of my patients have needed to stop the medication to date for these symptoms. 
  • It seems effective. All my patients qualified to use Apremilast because they either could not tolerate Methotrexate or the Methotrexate was not helping. Skin manifestations have improved, joints seems to have improved in a more delayed fashion, and the jury is still out for dactylitis and enthesitis in my patients.
  • It is not as effective as TNF inhibitor medication. The onset of effect seems slower and not as pronounced.
  • There’s less need to monitor various blood tests as Apremilast does not seem to cause significant lab abnormalities. 

So how would I use this medication?

Well, at this stage, and I qualify this opinion by stating that I am still a babe in the woods in terms of experience with it, I would like to use this as an alternative to Methotrexate in psoriatic arthritis. 

While rheumatologists are very comfortable using Methotrexate, some patients prefer not to be on Methotrexate and Apremilast would seem a good choice - apart from its high cost.

Because of its high cost, easy access to Apremilast as the first line treatment is unlikely to happen (until patents run out). 

So I hope I get to use it just as I have been given the opportunity to. 

In those, where Methotrexate has failed, either due to side effects or due to lack of effect.

I wonder what your experience of the medication has been? 

Image accessed from http://www.otezla.net/psoriatic-arthritis/ on 25/3/16

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