Oral to subcutaneous methotrexate dose-conversion strategy for rheumatoid arthritis

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Oral to subcutaneous methotrexate dose-conversion strategy for rheumatoid arthritis

Both the American College of Rheumatology (ACR) and European League Against Rheumatism (EULAR) guidelines propose the use of methotrexate (MTX) for rheumatoid arthritis (RA) treatment if there is no contraindication. MTX belongs to the class of antimetabolites drugs which acts by slowing or stopping the growth of cancer cells and repressing the immune system.

It is known to be a bedrock of RA therapy, although absorption saturation undermines its oral bioavailability. The need for guidance on successful dose-conversion methods arises due to the differences in the relative BA of oral versus subcutaneous (SC) MTX.  The study mentioned here was performed to distinguish MTX pharmacokinetics profiles as a consequence of MTX administration via three distinct treatment administrations: oral, SC, MTX administered via an auto-injector (MTXAI) into the abdomen (MTXAIab) and the thigh (MTXAIth). A dose-conversion method based on the BA of MTX from oral and SC administration was initiated in this paper.

Subcutaneous administration supplemented higher exposure of MTX than the same dose given orally. The dose-proportional exposure was seen with SC MTX unlike the exposure restrictions of oral MTX.


BMC musculoskeletal

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The original title of the article:

Rheumatoid arthritis treatment: Oral to subcutaneous methotrexate dose-conversion strategy


Markus Hildebrandt et al.

Therapeutic, Methotrexate, Rheumatoid Arthritis, Joints, Antimetabolites, Efficacy, Subcutaneously
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