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Phase II Reactions: Methylation Reactions01:17

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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Drug Regulation01:25

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Drug regulation encompasses the management of drug usage by evaluating its safety and efficacy through assessments conducted by regulatory authorities. Regrettably, the history of drug regulation is marred by several catastrophic events. One such incident is the Elixir Sulfanilamide tragedy, in which the toxic compound diethyl glycol was included in a sweet-tasting medication, leading to numerous fatalities. This event prompted the enactment of the Food, Drug, and Cosmetic Act in 1938. Under...
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Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren...
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Carotegrast Methyl: First Approval.

Sohita Dhillon1

  • 1Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. dru@adis.com.

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Summary
This summary is machine-generated.

Carotegrast methyl is a new treatment for ulcerative colitis. This α4 integrin antagonist blocks inflammatory cell adhesion, offering a novel therapeutic option for moderate cases.

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Area of Science:

  • Gastroenterology
  • Immunology
  • Pharmacology

Background:

  • Ulcerative colitis (UC) is a chronic inflammatory bowel disease.
  • Current treatments for moderate UC, such as 5-aminosalicylic acid, have limitations for some patients.
  • Targeting inflammatory cell adhesion offers a potential therapeutic strategy.

Purpose of the Study:

  • To summarize the development milestones of carotegrast methyl.
  • To highlight the first approval of carotegrast methyl for moderate ulcerative colitis.

Main Methods:

  • Carotegrast methyl is a small-molecule α4 integrin antagonist.
  • Its active metabolite inhibits the interaction between integrins (α4β1, α4β7) and their ligands (VCAM-1, MAd-CAM-1).
  • This mechanism blocks inflammatory cell adhesion and extravasation.

Main Results:

  • Carotegrast methyl targets key adhesion molecules involved in UC pathogenesis.
  • The drug's mechanism of action reduces inflammatory cell infiltration into the gut.
  • Demonstrated efficacy in patients with moderate ulcerative colitis.

Conclusions:

  • Carotegrast methyl represents a significant advancement in UC treatment.
  • Its approval in Japan marks a milestone for patients with moderate UC.
  • This α4 integrin antagonist offers a targeted approach to managing ulcerative colitis.