Women’s health pipeline: profiling the GCPR target class

8th January 2019 (Last Updated August 9th, 2019 09:33)

Health disorders in women can be caused by many abnormalities in the body and represent a very broad therapy area. Drug development for women’s health disorders has lagged behind other therapy areas, and few new therapies have been approved in the past years.

Women’s health pipeline: profiling the GCPR target class
Marketed pharmacotherapeutic treatments for diseases affecting women typically focus on controlling risk factors and complications in infertility. Credit: Moscow Institute of Physics and Technology.

Health disorders in women can be caused by many abnormalities in the body and represent a very broad therapy area. Drug development for women’s health disorders has lagged behind other therapy areas, and few new therapies have been approved in the past years.

The marketed pharmacotherapeutic treatments for diseases affecting women typically focus on controlling the risk factors and complications in infertility. The G protein-coupled receptor (GPCR) target class makes up 29% of the women’s health pipeline by molecular target.

These include follicle stimulating hormone receptor (FSHR), gonadotrophin-releasing hormone receptor (GnRHR), and oxytocin receptor. The gonadotropin FSH regulates several essential reproductive processes, including gametogenesis, follicular development and ovulation and exerts its effect via activation of the FSHR receptor, a glycoprotein located in the plasma membrane of ovarian granulosa cells.

Developing treatments for women's health disorders

FSHR mutations and dysregulated FSH-FSHR signalling are associated with infertility and subfertility in women. GNRHR also represents a well-established target within the market.

GnRH is the primary regulator of female reproductive function. By binding to the GnRHR, GnRH induces the synthesis and release of FSH and LH gonadotrophins.

Although the GPCR target class is dominated by targets that are already established in the market, there are a small number of novel targets, including kiss-1 receptor and tachykinin receptor 3, both of which have been recognised as key regulators of reproductive function.

As this is still an emerging class of therapy, this can be expected, and it may take more time for the pipeline size to reflect the commercial dominance. However, despite the relatively small pipeline size, there are opportunities for growth within this group.

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