AI Article Synopsis
- The FDA has approved oral formulations of peptides like semaglutide for diabetes and octreotide for acromegaly, showing that specific formulations can enable oral delivery.
- An assessment of MYCAPSSA®, the oral octreotide formulation, highlights its competitive advantages over traditional depot injections and discusses the innovative Transient Permeation Enhancer (TPE®) technology used to improve intestinal absorption.
- Despite oral octreotide having a much lower bioavailability compared to subcutaneous injections, its twice-daily convenience may appeal to acromegaly patients over less frequent injection methods.
Article Abstract
Introduction: The FDA approval of oral semaglutide for type 2 diabetes (2019) and oral octreotide for acromegaly (2020) is evidence that selected niche peptides can be administered orally if formulated with selected intestinal permeation enhancers.
Areas Covered: We evaluated the oral octreotide formulation, MYCAPSSA® (Chiasma Pharmaceuticals, Needham, MA, USA). An outline of the current standard of care in acromegaly and the benefits of oral octreotide versus depot injections is provided. We discuss the Transient Permeation Enhancer (TPE®) technology used and detail the safety and efficacy data from animal models and clinical trials.
Expert Opinion: TPE® is an oily suspension of octreotide that includes a number of excipients that can transiently alter epithelial barrier integrity by opening of intestinal epithelial tight junctions arising from transcellular perturbation. Phase I studies using 20 mg octreotide capsules yielded a relative oral bioavailability of ~0.7% and primary endpoints were achieved in two Phase III studies. The oral octreotide dose required to achieve these endpoints was over 200 times that of the 0.1 mg immediate-release subcutaneous injection, a reminder of the difficulty in achieving oral absorption of macromolecules. Many acromegaly patients will prefer a convenient twice-daily oral formulation of octreotide compared to monthly depot injections.
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| http://dx.doi.org/10.1080/17425247.2021.1942838 | DOI Listing |
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Article Synopsis
- * The MPOWERED trial tested oral octreotide capsules (OOCs), and the PATHFNDR-1 trial evaluated paltusotine, showing both effectively maintain biochemical control in patients used to injectable SRLs.
- * A systematic review highlighted 12 relevant studies, indicating OOCs have confirmed long-term maintenance, while further research is needed for paltusotine and direct comparisons between the two oral options.
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