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GSK2586184, a JAK1 selective inhibitor, in two patients with ulcerative colitis

Leonie C S De Vries1,2, Valerie J Ludbrook3, Kirsty J Hicks3

  • 1Department of Gastroenterology and Hepatology, Academic Medical Center, Amsterdam, The Netherlands.

BMJ Case Reports
|August 10, 2017
PubMed

Insights

A selective JAK1 inhibitor, GSK2586184, showed promise for ulcerative colitis (UC) treatment by improving clinical and endoscopic outcomes. This agent was well tolerated in a small patient group, suggesting potential for safer UC therapy.

Area of Science:

  • Gastroenterology
  • Immunology
  • Pharmacology

Background:

  • Ulcerative colitis (UC) is a chronic inflammatory bowel disease.
  • Non-selective Janus kinase (JAK) inhibitors like tofacitinib are effective but carry risks like neutropenia and anemia due to JAK2 inhibition.
  • Selective JAK1 inhibition offers a potential strategy to mitigate these adverse events.

Observation:

  • A study investigated the safety and efficacy of GSK2586184, a selective JAK1 inhibitor, in patients with moderate-to-severe UC.
  • The trial was discontinued early due to safety concerns in a parallel study.
  • GSK2586184 was administered to two patients with UC.

Findings:

  • GSK2586184 was well tolerated in the two UC patients treated.
  • The selective JAK1 inhibitor induced clinical and endoscopic response.
  • Treatment led to decreased histology scores and fecal calprotectin levels upon early withdrawal.

Implications:

  • Selective JAK1 inhibition may offer a safer therapeutic approach for ulcerative colitis.
  • Further research into JAK1-selective agents could lead to improved UC management.
  • Early indicators suggest potential for improved safety profile compared to non-selective JAK inhibitors.
Keywords:
drugs: gastrointestinal systeminflammatory bowel disease

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