Elagolix
[CAS# 834153-87-6]

Identification

• Classification: API >> Hormone and endocrine-regulating drugs >> Gonadotropin
• Name: Elagolix
• Synonyms: 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]butanoic acid
• Molecular Formula: C₃₂H₃₀F₅N₃O₅
• Molecular Weight: 631.59
• CAS Registry Number: 834153-87-6
• EC Number: 824-769-4
• SMILES: CC1=C(C(=O)N(C(=O)N1CC2=C(C=CC=C2F)C(F)(F)F)C[C@@H](C3=CC=CC=C3)NCCCC(=O)O)C4=C(C(=CC=C4)OC)F

Properties

• Density: 1.350 mg/mL

Safety Data

• Hazard Symbols: GHS08 Danger
• Risk Statements: H360-H361
• Safety Statements: P203-P280-P318-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Reproductive toxicity	Repr.	1B	H360
Reproductive toxicity	Repr.	2	H361

Discovery and Applications

Elagolix is a chemical substance developed as a medication to treat various conditions related to reproductive health, particularly endometriosis and uterine fibroids. It is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist, designed to reduce the levels of estrogen in the body by inhibiting the GnRH receptors. This results in a decrease in the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are essential for the production of estrogen and progesterone. By reducing estrogen levels, Elagolix helps to control the symptoms associated with conditions like endometriosis and uterine fibroids.

The discovery of Elagolix was driven by the need for more effective treatments for endometriosis, a condition in which tissue similar to the lining of the uterus grows outside of it, leading to pain, infertility, and other complications. Traditional treatments for endometriosis often involved surgical intervention or hormonal therapies with significant side effects. Elagolix was developed as an alternative that would provide effective symptom relief with fewer adverse effects.

Endometriosis affects millions of women worldwide, and Elagolix has been shown in clinical trials to significantly reduce pelvic pain and other related symptoms. By lowering estrogen levels, Elagolix works to shrink the endometrial tissue, alleviating pain and improving the quality of life for affected women. It is typically used in patients who have moderate to severe endometriosis and is taken orally, offering a convenient and non-invasive treatment option.

In addition to its use in endometriosis, Elagolix is also approved for the treatment of uterine fibroids. Uterine fibroids are non-cancerous growths that develop in the uterus and can cause heavy bleeding, pelvic pain, and other symptoms. By reducing estrogen levels, Elagolix helps to shrink fibroids and reduce the associated symptoms. It is particularly beneficial for women who are not candidates for surgery or who seek to avoid surgical interventions.

Elagolix is typically administered once daily, and its use is generally limited to six months due to the potential for bone density loss with long-term use. To mitigate this, patients may be prescribed additional medications, such as hormone replacement therapy, to protect bone health during treatment. Despite its effectiveness, the drug may cause side effects such as hot flashes, headaches, and mood changes, although these are generally mild and manageable.

The development of Elagolix represents a significant advancement in the treatment of gynecological conditions. By providing a non-surgical option for women with endometriosis and uterine fibroids, Elagolix offers an effective alternative that improves the quality of life for many patients. Ongoing research continues to explore its full potential, including its use in other hormone-related disorders.

In conclusion, Elagolix has become a key treatment option for managing endometriosis and uterine fibroids. Its unique mechanism of action and ability to target the underlying hormonal imbalance make it a valuable tool in reproductive health, offering a non-invasive and effective treatment alternative for women worldwide.

References

2024. Unraveling the complexity of amorphous solid as direct ingredient for conventional oral solid dosage form: The story of Elagolix Sodium. International Journal of Pharmaceutics, 666(1).
DOI: 10.1016/j.ijpharm.2024.124656

2023. Elagolix Sodium Salt and Its Synthetic Intermediates: A Spectroscopic, Crystallographic, and Conformational Study. Molecules (Basel, Switzerland), 28(9).
DOI: 10.3390/molecules28093861

2023. Efficacy and safety of oral gonadotropin-releasing hormone antagonists in moderate-to-severe endometriosis-associated pain: a systematic review and network meta-analysis. Archives of Gynecology and Obstetrics, 307(2).
DOI: 10.1007/s00404-022-06862-0