mPGES-1 drives inflammation

Microsomal prostaglandin E synthase (mPGES-1) is an enzyme generally present at low levels in the human body. It stimulates production of prostaglandin E2 (PGE2), a potent biological messenger that has a pronounced impact on inflammation. During inflammation the levels of mPGES-1 are upregulated, causing excessive levels of PGE2, which drive the inflammatory symptoms. 

Endometriosis – a painful disease that causes great suffering to millions of women

Endometriosis is a chronic inflammatory disease affecting women of childbearing age worldwide. The condition is widespread, but many sufferers have to wait a long time to receive a correct diagnosis. Today, approximately 10 percent of all women of childbearing age live with endometriosis. In the US and the five largest Western European countries alone – Germany, Italy, Spain, the UK and France – this corresponds to approximately 16 million patients. In Sweden, approximately 200,000 women live with endometriosis, of which 10 percent or more are teenagers. Endometriosis seriously affects many women’s everyday life over many years, and the disease also has a large general impact on society. There is an urgent need for new effective treatments.

Common disease symptoms are severe pain and reduced fertility

The cause of endometriosis has not been established, but according to a common theory, the disease is thought to arise during menstruation when the body rejects the cells that make up the outermost layer of the uterine lining. Some of these cells then incorrectly go backwards through the fallopian tubes, towards the ovaries and the pelvic and abdominal cavities. Here the cells attach to the underlying tissue and give rise to endometriotic lesions.

The most common symptom is severe pain associated with menstruation. A majority of patients describe also experiencing severe pain in connection with ovulation; pain during intercourse or when going to the toilet is also common. The intense pain causes major limitations in everyday life and negatively affects the quality of life, especially as the pain can become chronic over time. The disease also affects mental health through depression and extreme fatigue. In the long term, the lesions may cause abdominal adhesions that can complicate future surgery.

Around 30-50 percent of women with endometriosis suffer from reduced fertility. Often, the disease is first confirmed in connection with an infertility investigation.

Endometrial lesions may appear in various locations across the pelvic and abdominal cavities.

Illustration by Hic et nunc / CC BY-SA 3.0
Conventional treatments lack precision and often cause unwelcome side effects

Despite great efforts currently being made to understand endometriosis better, the general disease knowledge within the healthcare system is relatively low, and the time to diagnosis may be long. Gynecological examination with ultrasound or magnetic resonance imaging (MRI) can be helpful in the diagnosis of endometriosis, but a definitive diagnosis requires tissue samples obtained via laparoscopy.

There is currently no cure for endometriosis. Available treatments are various types of hormone-regulating or pain-relieving drugs. Hormone regulation has proven effective for symptom relief and treatment and is frequently achieved with regular hormonal contraceptives. However, these can have side effects. Anti-inflammatory drugs (NSAIDs) are often used to counteract the pain and reduce the inflammation, but with long-term treatment there is a risk of gastritis. Another form of treatment is surgery, usually in the form of laparoscopic procedures to remove the endometriosis lesions. However, new lesions often appear within a few years and may require repeated interventions. The need for effective treatments with high precision is therefore still great.

Further reading

Learn more about Gesynta Pharma

Gesynta Pharma bases its R&D on groundbreaking research from the Karolinska Institutet.

Our executive team and board of directors hold vast experience in drug development, commercialization and company scale-up.

Endometriosis is a chronic, inflammatory, estrogen-dependent disease affecting millions of women worldwide.

Our lead drug candidate GS-248 is currently under evaluation in a phase 2 study.