Relugolix: a revolutionary advance in the treatment of hormone-dependent diseases with GnRH antagonists
Basic information
Product Name: Relugolix
Synonyms:
CAS: 737789-87-6
MF: C29H27F2N7O5S
MW: 623.63
Chemical Properties
Melting point: 228 °C (decomp)(Solv: ethyl acetate (141-78-6); tetrahydrofuran (109-99-9))
Density: 1.442±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
Solubility: DMSO:20.0(Max Conc. mg/mL);32.1(Max Conc. mM)
Ethanol: 1.0(Max Conc. mg/mL);1.6(Max Conc. mM)
Form: A crystalline solid
Pka: 13.17±0.70(Predicted)
Color: White to off-white
InChIKey: AOMXMOCNKJTRQP-UHFFFAOYSA-N
SMILES: N(C1=CC=C(C2SC3=C(C=2CN(C)C)C(=O)N(C2=NN=C(OC)C=C2)C(=O)N3CC2=C(F)C=CC=C2F)C=C1)C(NOC)=O
product description
The main areas of application of this drug include the treatment of sex hormone-dependent diseases, which are as follows:
Uterine fibroids: Relugolix has been shown to be safe and effective in the treatment of uterine fibroids in a Phase III clinical study. It is able to rapidly lower estrogen and progesterone levels in women by taking them orally once a day, thereby relieving painful symptoms associated with uterine fibrosis.
Endometriosis: In a phase II clinical study, Relugolix was shown to significantly reduce pain caused by endometriosis and improve patients' quality of life.
Prostate Cancer: Relugolix has also shown potential in a Phase II clinical study to reduce serum testosterone to castration levels and significantly reduce prostate-specific antigen (PSA), which is an important indicator for the treatment of prostate cancer.
In addition, Relugolix, as a GnRH antagonist, also has the potential to study sex hormone-dependent diseases, for example, through its high affinity and strong antagonistic activity to study the pathological mechanisms of related diseases.
It has IC50 values of 0.33 nM (for humans) and 0.32 nM (for monkeys), respectively, showing its potential efficacy in the treatment of the above diseases.
In summary, the application of Relugolix is mainly focused on the field of gynecology and urology, especially for the treatment of diseases such as uterine fibroids, endometriosis and prostate cancer. As an orally effective non-peptide GnRH antagonist, Relugolix offers a new option for the treatment of these diseases and has shown positive results in clinical studies.