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9 Facts about Leflunomide

Medscape has published an informative review of leflunomide, drawn from Dr. Eric Ruderman’s recent lecture on the subject at the February RWCS meeting in Maui.

Leflunomide was FDA approved in 1998 for rheumatoid arthritis, roughly around the same time infliximab and etanercept were approved. While much excitement ensued for the TNF inhibitors, leflunomide has received "middle child [status] was underloved, underappreciated, and largely dismissed," said Dr. Eric M. Ruderman from Northwestern University. 

Some highpoints from this Medscape article and lecture: 

  1. Leflunomide won't replace biologics, "…but it should be in your toolkit"
  2. Leflunomide is highly effective in combination with methotrexate
  3. Leflunomide is as effective as methotrexate in ACR20 responses
  4. Side effects include diarrhea, nausea, rash, alopecia (reversible), and elevated liver function tests
  5. One of leflunomides clear benefits is in cost; very important in many countries
  6. It's important to monitor the WBC and LFTs (it has a very long half-life - plasma half-life is 15.5 days)
  7. Leflunomide is teratogenic 
  8. Despite the package insert, the 100 mg for 3 days loading dose is no longer used
  9. Leflunomide has been effective in active PsA and cutaneous psoriasis 

Join The Discussion

Bruce I Hoffman MD

| Mar 12, 2024 9:15 pm

Also useful in patients with decreased GFRvas not really rxcrestef

Saurav Suman

| Mar 13, 2024 1:42 pm

Has also been found effective in lupus nephritis in asian population. I use it as an add on therapy

Donald E Thomas Jr

| Mar 13, 2024 4:07 pm

Agree with Dr. Suman. There is actually quite a bit of Chinese literature on this.

Also, the danger during pregnancy has been questioned recently by a couple of studies. It will be interesting to see what our Reproductive Guidelines updates recommend when redone:

https://www.sciencedirect.com/science/article/pii/S0890623820301234
https://ard.bmj.com/content/77/4/500

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Disclosures
The author has no conflicts of interest to disclose related to this subject