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Drs. Elliott and Chan report no financial relationships relevant to this field of study.
The FDA has approved the first oral glucagon-like peptide-1 (GLP-1) receptor agonist for the treatment of type 2 diabetes mellitus (T2D). Semaglutide is a GLP-1 analog that has been marketed as an injectable since December 2017 (Ozempic). In the oral form, semaglutide is coformulated with an absorption enhancer, salcaprozate sodium (SNAC), to permit once-daily oral dosing. The FDA granted priority review. The drug will be marketed as Rybelsus.
INDICATIONS
Semaglutide is indicated as adjunct to diet and exercise to improve glycemic control in adults with T2D. 1
DOSAGE
The starting dose is 3 mg once daily for 30 days. 1 After 30 days, increase the dose to 7 mg once daily. The dose may be increased to 14 mg once daily after 30 days (if additional glycemic control is needed). The dose should be taken (with no more than 4 oz of plain water) at least 30 minutes before the first food, beverage, or other oral medications of the day. Semaglutide is available as 3 mg, 7 mg, and 14 mg tablets.
POTENTIAL ADVANTAGES
Oral semaglutide is the first oral GLP-1 receptor agonist to be approved. It can be transitioned to subcutaneous injection easily (7 mg or 14 mg to 0.5 mg). 1
POTENTIAL DISADVANTAGES
Oral semaglutide has low bioavailability (0.4%-1%), and requires optimal conditions for absorption. The oral form is dosed 7 to 14 times the subcutaneous dose on a mg basis and given daily instead of weekly. The drug should be taken on an empty stomach upon awakening with a sip of water (no more than 4 oz). Food should be eaten 30-60 minutes after taking oral semaglutide. The exposure of oral semaglutide decreases with increase in body weight (e.g., 129 kg vs. 56 kg)....