March is Endometriosis Awareness Month which is aimed at increasing awareness of the debilitating condition that affects more than six million women in the U.S and an estimated 176 million worldwide. That equates to about 1 in 10 women who suffer from endometriosis. An extremely painful condition, endometriosis is further confounded by a general lack of awareness, which results in an average diagnosis of the disease taking more than seven years to achieve. To make matters worse, medical experts say endometriosis is the biggest cause of infertility in women. This is why one of the goals of the annual awareness campaign is to urge patients to seek out an earlier diagnosis and start treatment sooner.
This we know: Endometriosis is an estrogen-dependent, chronic, inflammatory disease characterized by the appearance and growth of endometrial cells or tissues in locations outside the uterus. There is no cure for endometriosis, and the associated pain is currently managed with oral contraceptives, progestins, nonsteroidal anti-inflammatory drugs (NSAIDs) and opioids. GnRH agonists are the most effective approved treatment option for endometriosis with leuprolide being the most widely used agent in this class of drug.
While effective, leuprolide has significant limitations in both convenience and tolerability which are largely attributed to its depot injection delivery method (Lupron Depot®). A depot injection is a slow-release, slow-acting form of administrating a medication. It is usually given in a carrier liquid that releases the medication slowly so it lasts in the body longer. In the case of Lupron Depot ®, it is given in a one month or a three month dose and is considered the current standard of care for endometriosis.
The problem with it, however, is that leuprolide is sometimes not tolerated by the patient and any side effects caused by the injections will last in the body for the duration of the dose given, i.e., one month or three months.
This is where Enteris BioPharma can help. Enteris develops innovative drug products built around its proprietary oral delivery technology, Peptelligence® which enables the company to develop oral dosing options to drugs that are usually administered via injection. In the case of endometriosis, Enteris is developing a daily oral tablet formulation of leuprolide called Ovarest®.
In a recent Phase 2a study, Ovarest® was found to enable significant suppression of estradiol (E2), demonstrating a measurable pharmacodynamic effect that is tightly correlated with efficacy in endometriosis. Importantly, Ovarest® not only offers the convenience of a pill, but also a rapid reversibility in the event of adverse side effects.
These properties are potential game changers for endometriosis patients. If approved by the U.S. FDA, Ovarest® would enable women to administer the medication as they would a standard tablet, eliminating the need to receive injections at a doctor’s office. Additionally, in the event of an adverse reaction to leuprolide, a patient would no longer have to endure the side effects for an extended period as is currently the case with a depot injection. All that would be required to reverse the side effects is for the woman to stop taking the tablets.
Recognizing that an oral treatment for endometriosis has the potential to meet several patient and prescriber needs, Enteris is excited to advance the development of Ovarest® into a Phase 2b trial with the hope and intent that positive data outcomes will translate into a viable treatment option for endometriosis sufferers. While we can never truly know what the future will hold, Enteris is optimistic that we will be able to provide endometriosis sufferers with a significant treatment option. But until we get there, Enteris recognizes the efforts by the various advocacy groups and associations that work tirelessly throughout the year to call attention to this disease.