endometriosis

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.

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.

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 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.

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.

Mifepristone (C-1073) is a progesterone-receptor (IC50=0.2 nM) and glucocorticoid-receptor antagonist (IC50=2.6 nM). Mifepristone is used to terminate pregnancy, treat uterine fibroids, and treat 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.

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).

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.

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.

Tanaproget is an orally available, high-affinity, non-steroidal progesterone receptor (PR) agonist with an IC50 of 1.7 nM for hPR. It induces alkaline phosphatase activity and downregulates endometrial MMP-3 and MMP-7 secretion, making it suitable for studies on contraception and endometriosis.

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.

GnRH-R antagonist-2 (Compound 44c) is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist, with IC50 values of 43 nM for rat and 88 nM for human GnRH-R. It is applicable in studies related to hormone-dependent diseases such as endometriosis, breast cancer, and prostate cancer^[1].

BAY-1128688 is a potent, orally bioavailable selective AKR1C3 inhibitor with an IC50 of less than 2 nM. It shows high selectivity for related AKR1C enzymes (1C1, 1C2, 1C4) and AKR1D1, with no significant activity on major nuclear hormone receptors. BAY-1128688 reduces endometriotic lesions in a marmoset model of endometriosis and is useful for research in endometriosis.

GnRH-R antagonist-3 (Compound 37) is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist with IC50 values of 94 nM for rat GnRH-R and 275 nM for human GnRH-R. It is utilized in research related to hormone-dependent diseases, such as endometriosis, breast cancer, and prostate cancer^[1].

Elagolix is an orally active, highly effective, selective non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRH receptor) with a dissociation constant (KD) of 54 pM, as well as an NFAT inhibitor, and is utilized in researching endometriosis-related pain.

BV6 TFA acts as an antagonist of the apoptosis inhibitory proteins (IAP) family members, cIAP1 and XIAP. It inhibits the proliferation of HCC193 cells, showing an IC50 value of 7.2 μM in an MTS assay. BV6 TFA can be utilized in studies relating to endometrial cancer and endometriosis.

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

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