Future Erectile Dysfunction Drugs: Uprima, Topiglan, Melanocostin, Activators, Gene Therapy

The Race for New Erectile Dysfunction Treatments

Erectile dysfunction is a hot topic among medical researchers and those seeking alternative treatments for this disorder affecting sexual activity. Most studies and clinicians seeking new ways to treat erectile dysfunction focus on alternative supplements, new or improved surgical implant devices, and potential drugs that may be approved by the Food and Drug Administration. In the future, there will likely be many options to currently prescribed medications and therapies, including some that may prove more effective, faster acting, more convenient and with fewer side effects.

At present, there are five prescribed medications available for treatment of erectile dysfunction. This is a competitive market for pharmaceutical companies, so it is easily assumed that all pharmaceutical giants are working now toward the next wonder pill for treatment of erectile dysfunction. Several drugs and types of therapy for erectile dysfunction are rumored to be close to FDA approval for market use, including the following:

• Uprima
• Topiglan
• Melanocortin Activators
• Gene Therapy

Uprima

In Europe, Uprima has been on the market for awhile and is considered as reliable of a treatment of erectile dysfunction as some of the prescription medications used widely by Americans. The European Commission, like its American counterpart the FDA, approved Uprima use as the first medication to treat impotence. Residents of the United States can legally purchase Uprima in adequate supplies for up to 90 days because it is not a controlled substance or prohibited by the FDA. Uprima does meet FDA Medication Import Policy guidelines and can be ordered from European pharmacies.

A chemical cousin to morphine, Uprima is a dopamine receptor simulator. It stimulates the hypothalamus of the brain, the region responsible for development of erections. Uprima works through the hypothalamus to allow more blood to flow through the penis by inhibiting smooth muscle contractions that would typically block that blood flow. Because blood engorgement is responsible for the rigidity of an erection, Uprima makes achieving an erection easier with more frequency.

Like other drugs for erectile dysfunction, Uprima does not act as an aphrodisiac or increase sexual desire. This drug enables erections to occur when the man is already sexually stimulated through touch and mental factors.

Uprima shows great promise in its ability to achieve reliable, rapid, strong erections. It has been shown to work two to three times faster than drugs available on the American market at this time, usually acting in about 15 to 20 minutes.

Much of this benefit is attributed to Uprima’s use sublingually, under the tongue in dissolving tablets. This is unlike major competitors, which are often taken as tablets that must enter the bloodstream through the gastrointestinal tract. Because Uprima dissolves under the tongue, it also can be taken on an empty stomach, after eating, or at any other time without being affected or results diminished.

The biggest reason why Uprima is available in Europe but not in the United States is that it has some minor side effects that are being investigated. Nausea is one common effect, as are headaches, vomiting and dizziness. The worst effect has been fainting, which is what presently restricts wide release of Uprima in the U.S. Researchers are working on a nasal spray form of Uprima that may alleviate the nausea reactions.

Uprima is similar to other presently available erectile dysfunction drugs in America, in that it is not recommended for use by those with heart problems or hypertension. Uprima was originally developed for treatment of Parkinson’s Disease. When patients started experiencing erections upon taking the medication, doctors realized that the drug had potential for treatment of erectile dysfunction patients.

Topiglan

Applied topically in gel form, Topiglan is a new treatment for erectile dysfunction that may soon be approved by the FDA for sale in the United States. Topiglan is a great option for anyone with erectile dysfunction who cannot take a pill or for those who may not have had success with other ED medications.

The most important ingredient in Topiglan is Alprostadil, also known as prostaglandin E1 or PGE1, which was first approved by the FDA in 1996. Along with PGE1, a substance that allows for rapid absorption of the gel is contained in Topiglan. This substance helps the drug work through the skin’s layers quickly to efficiently dilate penis blood vessels.

Because Topiglan is used on the skin as a gel or cream, it is quickly absorbed and results in a rigidly erect penis in mere minutes after application. Also because it is applied directly to the penis, Topiglan does not offer the risk of adversely interacting with other medications the erectile dysfunction patient may be taking. This is different than other ED drugs taken orally, which can cause problems in patients taking nitrates for heart problems. In being topically applied, even nitrate patients may be able to use Topiglan without harm.

Other people who may be able to use Topiglan without problems include those who suffer from hypertension or diabetes. Even erectile dysfunction patients with cardiovascular disease or bad circulation can enjoy the benefits of Topiglan.

With Topiglan, there is no need to wait for it to start taking effect. Effects are seen immediately because the drug does not have to be absorbed into the blood stream to work. Since spontaneity is the biggest sacrifice of erectile dysfunction treatments, Topiglan’s ability to deliver a quick erection immediately upon application puts reliable spontaneity back into erectile dysfunction patients’ sex lives.

Although the FDA has yet to approve Topiglan, there do not yet appear to be any major side effects or disadvantages associated with the treatment. That is, no side effects beyond slight redness, rash or itching. Still, if it is eventually approved for sale in the United States, Topiglan will most likely be available only by prescription.

Melanocortin Activators

Drugs that seem to act through the brain and the rest of the central nervous system to produce an erection are known as melanocortin activators. Drugs of this nature, also known as PT-141, have been tested in animals and show positive results. The earliest studies in human subjects have also shown that PT-141 can work for men with mentally caused erectile dysfunction, but not for physically derived erectile dysfunction. It is very early in the testing phases of melanocortin activators, and larger, more comprehensive studies are needed to learn more about how these drugs work and whether they are safe options for treatment of erectile dysfunction.

Gene Therapy

Gene therapy for erectile dysfunction, also called gene transfer or ion channel therapy, has resulted in positive impressions. Considered both well tolerated and safe following its first human studies at Wake Forest University School of Medicine’s Institute for Regenerative Medicine, gene transfer was tested in 11 men with erectile dysfunction.

In gene transfer for erectile dysfunction, small pieces of DNA are introduced to the nuclei of cells to encourage production of proteins that relax smooth muscle cells. These smooth muscle cells are found in the penis and hollow organs like the bladder. When smooth muscle cells in the penis are relaxed, the penis fills with blood and an erection results.

One advantage of gene therapy versus other types of treatments for erectile dysfunction is that one gene transfer treatment can provide results which last for months. Subjects in the Wake Forest study showed improvements for the entire 24 weeks of their study. In half of the subjects studied, erectile dysfunction was blamed upon their diabetes or heart disease. Both of those ailments are known to cause ED, as they restrict the body’s ability to relax smooth muscle cells.

The study was originally initiated to ensure gene transfer was safe and tolerable by erectile dysfunction patients. Not only did gene transfer prove this safety and tolerability, but it also indicated that even the highest doses of delivery provided significant erectile functional improvement.

For delivery of the gene transfer, DNA segments mixed into blood plasma were injected into the sides of the penis. The injection sites were specifically the corpus cavernosum, the spongy and elastic tissue along the length of each side of the penis. These corpus cavernosum fill with blood during an erection.

Patient responses to the study were measured against their sexual partners’ impressions. Both parties in each couple participating in the study provided favorable benefit and validation of the gene transfer impact.

There appear to be no side effects or safety concerns for gene transfer in erectile dysfunction subjects. Although this initial study was very successful, it was obviously conducted on a very small group as an initial test to ensure safety for humans. The next step before results can lead toward the lengthy FDA approval process is for a larger study, or series of studies, to be conducted on higher numbers of individuals affected by erectile dysfunction. Future tests will also explore use of oral erectile dysfunction drugs in conjunction with gene therapy. Even with optimum research and study results, gene transfer is a long time away from regulatory approval for use in patients in the United States.