Recommended

Golimumab In Unresponsive Ulcerative Colitis

Systematic Review Of Randomized Controlled Tria...

Long-term Efficacy And Safety Of Once-daily Mes...

Clinical Potential Of Naloxegol In The Manageme...

Targeted Therapy Of Short-bowel Syndrome With T...

0 votes
Long-term Efficacy And Safety Of Once-daily Mesalazine Granules For The Treatment Of Active Ulcerative Colitis
Author: Stephan Karl Böhm, Wolfgang Kruis
Publisher: Derivative Works
15 pages
One time payment: €0.00
Required subscription: Free
Type of publication: Article
ISBN/ISSN: 1178-7023
DOI: 10.2147/CEG.S35691
Follow this publisher

Share this publication:

Description:

Abstract: In 1977, 5-aminosalicylic acid (5-ASA) was discovered as a therapeutically active moiety of sulfasalazine (SASP) and was launched for topical and oral therapy of ulcerative colitis (UC) in 1984. As a first-step, delivery systems had to be developed to protect 5-ASA against absorption in the upper gastrointestinal tract, resulting in different and competing strategies (azo compounds, controlled release, and pH-dependent release). In a second step, at the beginning of the new century, coinciding with the expiration of patent protection for the first 5-ASA formulations, two component composite release mechanisms (pH-dependent and controlled release) were developed. Furthermore, the drug was formulated as granules instead of tablets, allowing higher unit strengths compared with tablets. Neither Salofalk Granu-Stix®, nor MMX 5-ASA, nor Pentasa® granules have initially been developed for once-daily (OD) dosing. A review of the achievements of 20 years of 5-ASA development has demonstrated that 5-ASA has equal efficacy compared with SASP at best, that there are no measurable differences in efficacy between various 5-ASA preparations, and that in a group of patients tolerating SASP, adverse event profiles of SASP and 5-ASA did not differ significantly, with SASP being the far cheaper substance. Therefore, drug adherence came into focus as a new goal for improving UC therapy. Although adherence is a complex and multifactorial construct, a simple dosing schedule may contribute to higher drug adherence and better efficacy of treatment. Simultaneously, the US 5-ASA market, estimated to be worth US$1.4 billion, is expected to grow continuously. Naturally, this very competitive market is not only driven by scientific progress but also by commercial interests. Thus, patents for minor changes to the formulation may serve as protection against drug companies trying to launch generic versions. Randomized controlled trials performed on OD dosing in induction of remission have demonstrated that OD administration of 5-ASA is as effective as conventional dosing in mild to moderate active UC. The three 5-ASA products MMX, Salofalk®, and Pentasa® employed in those studies so far have not shown differences in efficacy between OD and conventional dosing. No differences regarding safety outcomes have been detected between OD and conventional dosing, including incidence of adverse events, serious adverse events, or withdrawal from treatment due to an adverse event. Although the majority of patients prefer OD dosing to conventional dosing, it was not possible to detect differences in adherence between OD and multiple dose regimens in the clinical trial setting. Well-designed and controlled large-scale community-based studies are necessary to further investigate and prove the point of improved long-term adherence and treatment efficacy in OD dosing.

About the publisher:

We are a publishing house devoted to reuse CC-BY licensed published materials.

 

Using CC-BY licenses:

YOU ARE FREE TO:

  • Adapt — remix, transform, and build upon the material
  • for any purpose, even commercially.
  • The licensor cannot revoke these freedoms as long as you follow the license terms.

UNDER THE FOLLOWING TERMS:

  • No additional restrictions — You may not apply legal terms or technological measures that legally restrict others
    from doing anything the license permits.

NOTICES:

  • You do not have to comply with the license for elements of the material in the public domain or where your use is permitted by an applicable exception or limitation.
  • No warranties are given. The license may not give you all of the permissions necessary for your intended use. For example, other rights such as publicity, privacy, or moral rights may limit how you use the material.

Select a payment method