Bhaskaran and Nair, Gynecol Obstet 2012, 2:3
DOI: 10.4172/2161-0932.1000e105
Editorial Open Access
Volume 2 • Issue 3 • 1000e105
Gynecol Obstet
ISSN:2161-0932 Gynecology an open access journal
Progestins/Antiprogestins: Role in Pathogenesis and Treatment for
Endometriosis
Shylesh S. Bhaskaran and Hareesh B. Nair*
Southwest National Primate Research Center, Texas Biomedical Research Institute, San Antonio TX 78227, USA
Abstract
Endometriosis is a painful gynecological condition in fertile age in which endometrial tissue, which is normally
found only in the inside lining of the uterus, develops outside the uterus and attaches to the pelvic foor, endometrium
or peritoneal cavity. Endometriosis causes abdominal pain, bleeding, irregular menstrual cycles with excessive pain,
infammatory responses and infertility. Retrogressive menstruation and invasion theories have been well studied in
the pathogenesis of endometriosis. The role of steroids including estrogen and gonadotropin releasing hormones has
been documented and major treatment strategies are based on steroid biology of endometriosis. Current treatment
strategies are only partly successful and focus solely on the late phase of the disease. The exact role of progesterone
in the initiation (initial phase) of endometriosis has not been well studied or has been overshadowed by the concept
of progesterone resistance that occurs in the late phase of endometriosis. In this review, we discuss the role of
progesterone and the potential use of antiprogestins or possible combination treatment strategies that may help to
combat initiation and progression of endometriosis.
*Corresponding author: Hareesh B. Nair, Southwest National Primate
Research Center, Texas Biomedical Research Institute 7620 NW Loop 410,
San Antonio TX 78227, USA, Tel: 210-258-9515; Fax: 210-258-9883; E-mail:
hnair@txbiomedgenetics.org
Received May 29, 2012; Accepted May 29, 2012; Published May 31, 2012
Citation: Bhaskaran SS, Nair HB (2012) Progestins/Antiprogestins: Role
in Pathogenesis and Treatment for Endometriosis. Gynecol Obstet 2:e105.
doi:10.4172/2161-0932.1000e105
Copyright: © 2012 Bhaskaran SS, et al. This is an open-access article distributed
under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the
original author and source are credited.
Keywords: Endometriosis; Progesterone; Antiprogestins; Focal
Adhesion Kinase (FAK); Personalized therapy
Endometriosis is a benign gynecological disease that afects about
10% of reproductive- age women. It is associated with pelvic pain and
is a signifcant cause of infertility [1]. Patients with endometriosis show
reduced rates of follicular growth, reduced functional ability of the pre-
ovulatory follicle, reduced fertilization rates, irregular pre-implantation
embryonic development, altered early luteal function, and reduced
implantation rates [2,3]. Classical treatments, including progestins,
antiestrogens and GnRH antagonists, ofen lead to undesirable
side efects and a compromised quality of life [4]. Endometriosis is
expensive to treat and complex to study because there are notable
delays in its diagnosis as well as variations in symptoms and disease
development in patients [5]. Also, at the time of clinical presentation,
most women already have established disease, making the initiation
ofendometriosis difcult to study. Te implantation hypothesis of
retrograde menstruation by Sampson [6] is the most widely accepted
theory of endometriosis. Although retrograde menstruation occurs in
all women, the reason thatonly 10% of women experience adhesion
and invasion of endometriotic epithelial and stromal cells on peritoneal
mesothelium remains elusive.
Only sparse reports are available regarding the molecular
signalling of endometrial pathogenesis leading to the initiation and
progression of endometriosis. A large body of scientifc evidence
suggests that estrogen and estrogen receptors (ERs) are involved in
the progression of endometriosis [7]. Although progestins are used to
treat endometriosis, the exact role of progesterone in the formation
(initiation) of endometriotic lesions is poorly understood. Te main
side efects of progestin therapies are interim bleeding, weight gain
and reduced libido. Oral contraceptives are generally well tolerated but
they are not as efective in reducing pain [8]. GnRH-antagonists are
highly efective, but they lead to a signifcant reduction in bone density
[9]. Progesterone is produced by the corpus luteum to maintain early
pregnancy. Low progesterone secretion in the luteal phase has been
associated with habitual abortion. Hence it is logical to hypothesize
that antiprogestins given in early pregnancy can act as abortifaciants
and could provide alternatives to surgical abortion.
Based on our laboratory experiments, progression of endometriosis
primarily depends on the levels of progesterone secretion by the
corpus luteum at the time of attachment of menstrual endometrial
epithelial/stromal cells to peritoneal mesothelium. Progesterone level
is maintained high enough to support the attachment and subsequent
invasion; then it drops dramatically afer 1-2 weeks. Tis window is
crucial for progesterone-induced proliferation and activation of
progesterone target genes to ease the cellular invasion of the attached
menstrual endometrial or stromal cells. Tus, endometriosis is a
pseudo-pregnancy state and the corpus luteum produces progesterone
to support and maintain the attached endometrial/stromal cells as if
they were a fertilized egg. In most clinical cases at the time of diagnosis
(2-6 months), the circulating as well as tissue levels of progesterone
are too low to be detected and ofen misunderstood as progesterone
resistance [10,11].
Another important factor in the context of the ideal profle of an
antiprogestin for endometriosis is its efect on the endometrium [12].
Te endometrium is under the well-balanced control of estrogens
and progestins. Estrogens lead to a marked proliferation of the
endometrium that might lead to endometrial hyperplasia if this efect
is not controlled through the antiestrogenic efect of progestins.
Sustained, persistent estrogenic stimulation in the absence of progestin
ultimately results in hyperplasia. Our results point to the fact that the
efect of estrogen is apparent only in the second phase of the disease
(unpublished data), since the frst wave of progesterone secretion by
the corpus luteum to support the pseudo egg is sufcient to initiate
the menstrual endometrial/stromal cell attachment on the peritoneal
mesothelium. Te treatment with a pure antiprogestin may therefore
inhibit menstrual endometrial/stromal cell attachment on peritoneal
mesothelium as well as the subsequent second wave of estrogen
induced proliferation.
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ISSN: 2161-0932
Gynecology & Obstetrics