Bremelanotide Treatment Improves Sexual Function and Reduces Associated Distress Levels in Women

A recent randomized, double-blind, placebo-controlled phase IIb trial of bremelanotide for the treatment of female sexual dysfunction actually required two stages of analysis, both of which were presented in New York City on May 6, 2014, at the American Psychiatric Association’s 167th annual meeting.

Bremelanotide is a melanocortin-receptor-4 agonist that targets a receptor system in the central nervous system that is active in such areas as hair and skin pigmentation, sleep, and weight, as well as sexual arousal.

The first stage of research, explained Leonard R. DeRogatis, PhD, director of the Maryland Center for Sexual Health, was designing a more thorough questionnaire that would measure not just women’s sexual dysfunction, but also their distress at that lack of function. As he pointed out, “You can have all the symptoms of sexual dysfunction in the world, but if you have no desire, you can’t be given a diagnosis of distress.” Or, in lay terms, “Some menopausal women say, ‘Thank God that’s over.’”

Accordingly, his team of researchers added two items to the 13 existing questions on the FSDS-R, thus creating what he called the Female Sexual Distress Scale-Desire/Arousal/Orgasm.

The two new items ask women: “How often did you feel concerned by difficulties with sexual arousal?” and “How often did you feel frustrated by problems with orgasm?” over the past 30 days. There were a number of subtopics, such as “How often did you feel embarrassed about your sexual problems?” and “How often did you feel bothered by low sexual desire?"

Armed with the enhanced questionnaire, the study then enrolled approximately 725 premenopausal women in the 12-week study. Each of the participants was in a stable, monogamous relationship that had been ongoing for at least six months, and many of them were in long-term marriages, according to Anita H. Clayton, PhD, a professor of psychiatry and neurobehavioral sciences at the University of Virginia in Charlottesville. She said she did not know if any were lesbian relationships, but she said the results theoretically should be the same for both heterosexual and same-sex partnerships.

The participants had all been diagnosed with hypoactive sexual desire disorder, female sexual arousal disorder, or both conditions, for at least six months.

The study medication was self-administered at a dosage of 0.75 mg, 1.25 mg, or 1.75 mg, by subcutaneous injection usually in the abdominal area. According to Clayton, bremelanotide is effective for 24 hours, and it can be safely used as many as 16 times in a month.

In its most important results, using the new questionnaire, the trial found significant improvements at the highest dosage of bremelanotide in terms of frequency of desire, frequency of arousal, ease of arousal, continuation of arousal, and orgasm, compared with the cohort on placebo. For instance, the mean change in orgasms was a reported increase of 1 for the 1.75 mg dosage versus just 0.4 for the group on placebo. Frequency of desire was nearly double: a mean of 0.9 for the group on 1.75 mg of bremelanotide and 0.5 for the control group.

If they get approval from the Food and Drug Administration, the researchers hope to start phase III trials by the end of the year.

Source: http://www.hcplive.com

New Agent for Female Sexual Dysfunction Has Promise

The melanocortin-receptor-4-agonist bremelanotide seemed to cut back distress and increase satisfaction among premenopausal ladies with feminine sexual dysfunction, researchers rumored here.

In phase II clinical studies, a 1.75-mg hypodermic dose of the experimental bremelanotide result in a mean reduction of regarding 1.1 points in feminine Sexual Distress Scale-Desire/Arousal/Orgasm score compared with a mean reduction of regarding 0.6 points among placebo patients (P<0.001), said Sheryl Kingsberg, PhD, from Case Western Reserve University in Cleveland, and colleagues.

Combining the 1.25-mg dose and also the 1.75-mg dose, the reduction was regarding 0.9 points (P<0.01 versus placebo), Kingsberg unhappy at an advertisement presentation at the American College of Obstetricians and Gynecologists annual meeting.

"There aren't any approved medication for hypoactive sexual desire disorder in ladies," she told MedPage these days.

"Female sexual dysfunction could be a category of disorders that represent the foremost outstanding sexual disorders in ladies," she went on to clarify. "You could still have sex and it would be pleasurable, but it is about wanting sex."

In a companion study that specifically checked out hypoactive sexual desire disorder, David Portman, MD, director of the Columbus Center for Women's Health analysis in Ohio, said that treatment with bremelanotide resulted in ladies boosting the amount of satisfactory sexual events in a month.

The study by Kingsberg's cluster targeted on the analysis of how at-home, self-administered bremelanotide mitigated the strain hooked up to hypoactive sexual desire.

"The FDA needs that the treatment cut back stress on the feminine Sexual Distress Scale-Desire/Arousal/Orgasm," Kingsberg same. "We demonstrated a dose-dependent efficacy for bremelanotide to cut back the distress of feeling fazed by low sexual desire."

The 12-week study had 97 ladies who were randomised to received placebo, 87 ladies who were treated with a 0.75 mg dose of bremelanotide, that was a dose that wasn't more practical than placebo, 75e ladies who were treated with 0.25 mg of bremelanotide, and 74 ladies on a high dose of 0.75 mg. the ladies self-administered the drug on an as-needed basis.

Responder rates for satisfying sexual events were 37 for placebo, 38% for 0.75-mg dose, 48% for 1.25-mg dose, 55% for 1.75-mg dose, and 51 for one.25-mg and 0.75-mg pooled dose. Responder rates were 45%’ 49%, 60%, 69%, and 64%, severally, on the feminine Sexual Distress Scale-Desire/Arousal/Orgasm.

Patients taking bremelanotide reported more nausea, flushing, and headaches than those on placebo. About 5% of the placebo patients and 10% of the 1.75-mg dose of bremelanotide patients withdrew from the study because of adverse events, but the drug was generally well tolerated, Kingsberg said.

"Bremelanotide has finished its phase II studies and designs for phase III are now awaiting approval from the FDA," she said.

In the phase IIB, 24-week study by Portman's group, women self-administered the drug about 45 minutes prior to anticipate sexual activity. Of the 327 participants, the majority had either mixed hypoactive sexual desire disorder or female sexual arousal disorder with a primary diagnosis of hypoactive sexual desire disorder.

The mean change in sexual satisfying events with was increased by 0.3 events per month among the 76 placebo patients; by 0.7 events a month among the 62 women assigned to the 1.75-mg dose (P<0.05); and by 0.7 events per month in the 128 patients in the pooled 1.25-mg and 1.75-mg dose (P<0.05).

"In premenopausal hypoactive sexual desire disorder, subcutaneous bremelanotide yielded improvements across all key hypoactive sexual desire disorder measures with robust dose-dependence attaining statistical significance at 1.75 mg," the authors concluded.