While oral delivery of peptides has historically been challenging due to their susceptibility to degradation in the digestive system, recent advances have led to several successful oral peptide products in the US market. Here's a list of some currently approved ones:
1. Rybelsus (semaglutide): This medication, approved in 2019, is an oral GLP-1 receptor agonist used to treat type 2 diabetes. It utilizes a proprietary formulation to enhance absorption and stability in the gut. It is formulated in tablet with strengths of 3 mg, 7 mg and 14 mg. It is also available as solutions for the subcutaneous route. Its applicant holder is Novo Nordisk Inc, and the application number for tablet dosage form is N213051. It is covered by 11 orange book patents.
2. Mycapssa (octreotide): Approved in 2020, Mycapssa is a sustained-release capsule containing octreotide, a somatostatin analog. It uses a "transient permeability enhancer" technology to facilitate intestinal absorption. There are multiple octreotide injectable products, and one oral DR capsule. The strength of this DR capsule is 20 mg base. Its applicant holder is Amryt Pharmaceuticals DAC, and its application number is N208232. It is covered by 10 orange book patents.
3. Lupkynis (voclosporin): This immunosuppressant medication, approved in 2021, features a microemulsion formulation that improves oral bioavailability. It's used for preventing rejection in kidney transplant recipients. Its applicant holder is Aurinia Pharmaceuticals. Inc, and application number is N213716. It has one strength, and it is 7.9 mg. This product is covered by 3 orange book patents - 7332472 (exp. in 2024), 10286036 (exp. in 2037) and 11622991 (exp. in 2037)
4. Bylyvay (odevixibat): Another 2021 approval, Bylyvay is a bile acid modulator administered orally for the treatment of progressive familial intrahepatic cholestasis (PFIC). Its specific formulation allows for effective absorption. Odevixibat is formulated into capsules and capsule pellets, and they have different strengths. The applicant is Albired AB, and its application number is N215498. The capsule version is protected by 11 orange book patents.
5. Trulance (plecanatide): Approved in 2017, Trulance is a first-in-class medication for chronic idiopathic constipation. It acts locally in the gut and is relatively resistant to enzymatic degradation. Pleoanatide is formulated in tablet with a strength of 3 mg. The applicant holder is Salix Pharmaceuticals Inc. and its application number is N208745. It is protected by 9 orange book patents.
6. Macrilen (macimorelin): Also approved in 2017, Macrilen is an oral medication used to treat secondary hypogonadism in males. Its specific formulation helps protect it from breakdown in the digestive system. Macimorelin acetate is formulated for oral solution. Its strength per pouch is 50 mg base. The applicant holder is Novo Nordisk Inc, and its application number is N205598. It is protected by 1 orange book patent, and it is 8192719.
7. Cyclosporin A: While technically not a new drug, Cyclosporin A in its Neoral® formulation, approved in 1995, deserves mentioning. This microemulsion-based solution represents a significant advancement in oral peptide delivery for immunosuppression. And it is available in capsules, emulsion (ophthalmic), injectable and solution dosage forms.
It's important to note that this list isn't exhaustive, and more oral peptide products are in development with the potential for future approval. Additionally, it's crucial to consult with a healthcare professional before taking any medication, including those mentioned above.
