From the Guidelines
Bremelanotide (PT-141) is not well absorbed sublingually. The medication's large peptide structure prevents efficient absorption into the bloodstream when administered through mucous membranes like those under the tongue, resulting in minimal therapeutic effect 1. Although the provided study does not directly address bremelanotide, it discusses the absorption of other drugs sublingually, highlighting that highly lipophilic drugs like methadone, fentanyl, and buprenorphine are well absorbed sublingually, but this does not apply to all medications, especially large peptides like bremelanotide.
- Key points to consider:
- Bremelanotide's poor oral bioavailability and large peptide structure make it unsuitable for sublingual administration.
- The FDA-approved route for bremelanotide (Vyleesi) is subcutaneous injection, which allows the peptide to bypass first-pass metabolism in the liver and enter the bloodstream directly.
- Alternative routes like sublingual administration would likely result in unpredictable or negligible therapeutic effects.
- In real-life clinical practice, patients seeking to use bremelanotide should follow the prescribed subcutaneous injection method for reliable absorption and therapeutic effect, rather than attempting sublingual administration.
From the Research
Absorption of Bremelanotide (PT 141) Sublingually
- There is no direct evidence in the provided studies that specifically addresses the absorption of bremelanotide (PT 141) sublingually 2, 3, 4, 5, 6.
- However, study 3 discusses the concept and technologies for improvement of sublingual drug delivery, highlighting its potential for achieving high bioavailability and rapid onset of effect, but also notes the limitations and challenges associated with this route of administration.
- The primary studies on bremelanotide 2, 4, 5, 6 focus on its administration via subcutaneous injection or intranasal routes for the treatment of hypoactive sexual desire disorder (HSDD), without mentioning sublingual absorption.
- Given the information available, it appears that there are no research papers directly addressing the sublingual absorption of bremelanotide (PT 141) in the provided evidence.