PT-141

1025.18

1024.524292

6Y24O4F92S

G - Genito urinary system and sex hormones

379

-1.21

white powder

1.43

230

1.679

Currently there are no reports of overdoses of bremelanotide. Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure. In the event of an overdose, supportive measures should be used to address the associated symptoms.

In preregistration clinical trials, serum enzyme elevations were reported in small numbers of bremelanotide treated patients but in a similar proportion of subjects receiving placebo. A single case of acute hepatitis arose in a patient who had received 10 injections of bremelanotide over a one year period with marked elevations in serum aminotransferase levels, minimal increases in alkaline phosphatase, and mild jaundice which resolved after discontinuation. There have been no instances of acute liver failure or chronic liver injury attributed to bremelanotide, but the total clinical experience with this drug has been limited. Thus, acute liver injury from bremelanotide may occur but is rare.

Bremelanotide is 21% protein bound in serum.

Bremelanotide is indicated to treat premenopausal women with hypoactive sexual desire disorder that is not due to a medical or psychiatric condition, problems with the relationship, or the effects of a medication or drug.

Bremelanotide is a parenterally administered melanocortin receptor agonist that is used to treat female hypoactive sexual desire disorder. Bremelanotide has been reported to cause mild serum enzyme elevations during therapy and has been implicated in rare instances of clinically apparent acute liver injury.

Female Hypoactive Sexual Desire Disorder Agents

Bremelanotide is a melanocortin receptor agonist injected 45 minutes before anticipated sexual activity. Agonism of the melanocortin receptor MC1R also leads to increased melanin expression. Patients taking bremelanotide may also experience nausea, headache, and vomiting.

Bremelanotide has a T_max or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable. The C_max is 72.8ng/mL and the AUC is 276hr\*ng/mL.|64.8% of a radiolabelled dose is excreted in the urine and 22.8% of the dose is recovered in the feces.|The mean volume of distribution of bremelanotide is 25.0±5.8L.|The mean clearance of bremelanotide is 6.5±1.0L/hr.

Bremelanotide is a 7 amino acid and so its metabolism consists of multiple hydrolysis reactions.

The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).

Bremelanotide is an agonist of many melanocortin receptors which in order of potency are MC1R, MC4R, MC3R, MC5R, and MC2R. The mechanism by which agonism of these receptors translates to an improvement in hypoactive sexual desire disorder is currently unknown, however MC4R receptors are present in many areas of the central nervous system. MC3R and MC4R are found in the hypothalamus and are involved in food intake and energy homeostasis. One theory is that bremelanotide stimulates dopamine in the medial preoptic area, which is involved in the sexual behaviour of a number of organisms.

bremelanotide