endometriosis

PF-02413873 is a competitive antagonist of nonsteroidal progesterone receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.

Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.

Norethindrone (Norethisterone) is a synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception.

Dienogest (STS 557) is an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive.

Norethindrone acetate (19-Norethindroneacetate) is an oestrogen with inhibitory effects on adolescent menstruation and hepatic adenomas and is often used in combination with progestins in the study of endometriosis.

PBRM (17β-HSD1-IN-2) is a selective covalent inhibitor of 17β-HSD1, used in breast cancer and endometriosis research.

Opigolix, a Gonadotropin-releasing hormone receptor antagonist, treats hormone-dependent conditions by inhibiting the actions of gonadotropin-releasing hormone (GnRH).

Gestrinone (R 2323) is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.

Norethynodrel (Lynestrol) is a synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and endometriosis. As a contraceptive, it has usually been administered in combination with MESTRANOL.

Nomegestrol (TX 066 free base) is an orally available, selective and potent full agonist of the progesterone receptor with potent anti-estrogenic, partial anti-androgenic and anti-gonadotropic activity.Nomegestrol is also a contraceptive progestin and is used in the study of endometriosis and meningiomas.

3-Acetyl-7-Hydroxycoumarin (Compound 2) is a highly selective inhibitor of 17-β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). At a concentration of 6 μM, it achieves 57% inhibition of 17β-HSD1. 3-Acetyl-7-Hydroxycoumarin shows potential for research into hormone-dependent conditions such as breast cancer and endometriosis.

Histrelin (Supprelin LA) acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. It is considered a GnRH agonist. Histrelin is used in the treatment of hormone-sensitive cancers of the prostate in men and uterine fibroids in women.

Linzagolix choline is an orally available non-peptide gonadotropin-releasing hormone (GnRH) antagonist. It can be used to study pain associated with uterine fibroids and endometriosis.

ENMD-1068 HCl (ENMD 1068) is a PAR-2 antagonist. ENMD-1068 HCl inhibits the development of endometriosis in a mouse model.

Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by Kissei Pharmaceutical and ObsEva for the treatment of uterine fibroids, endometriosis, and adenomyosis. As of December 2020, it is under review for approval for uterine fibroids, is in phase III clinical trials for endometriosis, and is in phase II clinical studies for adenomyosis.

Leuprolide (1-3) is a manufactured version of a hormone used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, and early puberty.

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Goserelin is a gonadotropin-releasing hormone (GnRH LHRH) deceptide-like agent that acts as a GnRH agonist. It is suitable for hormone therapy of prostate cancer, premenopausal and perimenopausal breast cancer, endometriosis.

Goserelin acetate （ICI-118630 acetate） is a naturally occurring decapeptide, a GnRH (gonadotropin releasing hormone) agonist that reduces the production of sex hormones (testosterone and estrogen) for the treatment of prostate cancer, breast cancer and endometriosis.

ENMD-1068 hydrochloride, a selective protease-activated receptor 2 (PAR2) antagonist, inhibits TGF-β1 Smad signaling, thereby reducing hepatic stellate cell activation and collagen expression. It also suppresses the proliferation of endometrial cells and triggers apoptosis in epithelial lesion cells. This compound is utilized in researching endometriosis and liver fibrosis [1] [2].

Steroid sulfatase 17β-HSD1-IN-4 (compound 37) is a potent dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase 17β-HSD1-IN-4 irreversibly inhibits hSTS activity (IC50= 63 nM) and has research value in endometriosis and other estrogen-dependent diseases.

Steroid sulfatase 17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 [17β-HSD1], useful in studying endometriosis and other estrogen-dependent diseases.

Steroid sulfatase-IN-4 (Compound 16) is an irreversible inhibitor of human steroid sulfatase (STS) with an IC50 of 25 nM, and can be used to study endometriosis.

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.