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Elagolix | CAS No: 834153-87-6 | GMP-certified suppliers
A medication that manages moderate to severe pain associated with endometriosis by modulating hormonal pathways to reduce pelvic pain and related symptoms.
Therapeutic categories
Primary indications
- Elagolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the management of moderate to severe pain associated with endometriosis
Product Snapshot
- Elagolix is an oral small molecule available in capsule and tablet formulations
- It is primarily indicated for the management of moderate to severe pain associated with endometriosis
- Elagolix is approved for use in the US and Canada, with both approved and investigational statuses
Clinical Overview
Pharmacologically, elagolix binds competitively to GnRH receptors in the pituitary gland, inhibiting endogenous GnRH signaling. This results in a dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. Consequently, circulating concentrations of ovarian sex steroids, primarily estradiol and progesterone, are reduced. In clinical studies, elagolix demonstrated reductions in median estradiol to approximately 42 pg/mL with a 150 mg once daily dose and 12 pg/mL with a 200 mg twice daily regimen. The drug partially suppresses ovulation, with ovulation rates of approximately 50% and 32% at these respective dosing regimens during a three-cycle study in healthy women.
Elagolix’s absorption and metabolism involve cytochrome P450 enzymes, including CYP2C19, CYP2C8, CYP2D6, and CYP3A, with elagolix acting both as a substrate and inhibitor of various CYP isoforms and transporters such as P-glycoprotein and OATP1B1/SLCO1B1. Its modulation of these pathways can influence drug-drug interactions, which is a consideration in clinical use.
Safety evaluations have not demonstrated clinically relevant QTc prolongation even at supratherapeutic doses. Common adverse effects are related to hypoestrogenism and may include hot flushes and decreased bone mineral density with extended use. Safety monitoring recommendations emphasize limiting treatment duration and assessment of bone health.
In the context of pharmaceutical development and API sourcing, elagolix’s chemical classification as a gamma amino acid derivative demands attention to stereochemical purity and rigorous control of synthetic impurities. Given its CYP-mediated metabolism, API suppliers should ensure consistent batch-to-batch quality and stability, supported by comprehensive analytical characterization and compliance with regulatory standards for hormonal therapies.
Identification & chemistry
| Generic name | Elagolix |
|---|---|
| Molecule type | Small molecule |
| CAS | 834153-87-6 |
| UNII | 5B2546MB5Z |
| DrugBank ID | DB11979 |
Pharmacology
| Summary | Elagolix is an oral nonpeptide GnRH receptor antagonist that competitively inhibits pituitary GnRH receptors, resulting in dose-dependent suppression of LH and FSH secretion. This suppression decreases ovarian production of estradiol and progesterone, hormones that promote endometriosis lesion growth. The pharmacodynamic effect includes reduction of circulating estradiol levels, contributing to the management of endometriosis-associated pain. |
|---|---|
| Mechanism of action | Endometriosis develops when tissue that is similar to the kind that is normally located in the uterus starts to grow outside of the uterus [A35868, F801]. Such growth leads to various symptoms like pain during periods, pelvic pain between periods, and pain during sexual intercourse [A35868, F801]. The growths themselves are referred to as lesions and frequently develop on the ovaries, fallopian tubes, and other areas around the uterus, including the bowel or bladder [A35868, F801]. The growth of these lesions is dependent upon the estrogen hormone . Elagolix is an orally-administered, nonpeptide small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland [FDA Label, A35855, A35856, A35857]. Administration of elagolix results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones, estradiol and progesterone. |
| Pharmacodynamics | During a three menstrual cycle study in healthy women, an elagolix 150 mg once daily regimen and a 200 mg twice daily regimen resulted in an ovulation rate of about 50% and 32%, respectively. In Phase 3 trials in women with endometriosis, elagolix caused a dose-dependent reduction in median estradiol concentrations to approximately 42 pg/mL for the 150 mg once daily regimen and 12 pg/mL for the 200 mg twice daily regimen. Furthermore, the effect of elagolix on the QTc interval was investigated in a randomized, placebo- and positive-controlled, open-label, single-dose, crossover thorough QTc study in 48 healthy adult premenopausal women. Elagolix concentrations in subjects administered a single dose of 1200 mg was seventeen times higher than the concentration in subjects given elagolix 200 mg twice daily. Nevertheless, there was no clinically relevant prolongation of the QTc interval. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gonadotropin-releasing hormone receptor | Humans | antagonist |
ADME / PK
| Absorption | The Tmax of elagolix is reported as being 1.0 hours. The effect of a high-fat meal (relative to fasting) can result in a reduction of the AUC and Cmax by as much as 24% and 36%, respectively. |
|---|---|
| Half-life | The terminal phase elimination half-life of elagolix is recorded as being 4 to 6 hours. |
| Protein binding | The percentage bound to human plasma proteins for elagolix has been documented as 80%. |
| Metabolism | Elagolix is predominantly metabolized by the CYP3A family of isoenzymes despite participating in minor metabolic pathways with the CYP2D6, CYP2C8, and uridine glucuronosyl transferases (UGTs) enzymes as well. The primary metabolite of elagolix, referred to as NBI-61962 (R-(+)-4-{2-[5-(2-fluoro-3-hydroxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino}-butyrate) , is not believed to possess any significant biologic activity due to its low plasma exposure and an observed potency that is exceptionally less than the parent elagolix compound (Ki value of 3.5 compared to 0.9 nM) . |
| Route of elimination | The primary route of elimination of elagolix is via hepatic metabolism. |
| Volume of distribution | The apparent volume of distribution at steady state (Vdss/F) of elagolix is reported to be 1674 for a 150 mg daily regimen and 881 for a 200 mg twice daily regimen. |
| Clearance | The oral clearance (CL/F) of elagolix is 123 L/hr for a 150 mg once daily regimen and 144 L/hr for a 200 mg twice daily regimen. |
Formulation & handling
- Elagolix is a small molecule active pharmaceutical ingredient intended for oral administration in solid dosage forms.
- Due to very low water solubility and moderate lipophilicity (LogP 3.14), formulation strategies should address solubility enhancement.
- No special food restrictions are required for administration, but concurrent supplementation with calcium and vitamin D is recommended to mitigate bone mineral density loss.
Regulatory status
| Lifecycle | The API is marketed in the US and Canada, with key US patents expiring between January 2021 and September 2024, indicating the product is transitioning into a mature market phase with potential for generic competition. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Elagolix is marketed primarily in the US and Canada with multiple branded products indicating the presence of several originator companies. Patents expiring in 2021 and as late as mid-2024 suggest that some generic competition may exist or is approaching, primarily within the US market. There is limited information on presence in the EU or other regions. |
|---|
Safety
| Toxicity | In case of overdose, monitor the patient for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed. Common adverse reactions of elagolix include hot flush, headache, nausea, insomnia, mood alterations, amenorrhea, depression, anxiety, arthralgia, bone loss, changes in menstrual bleeding patterns, suicidal ideation and behavior, exacerbation of existing mood disorders, and/or hepatic transaminase elevations. The recommended duration of use for elagolix is up to 24 months for the 150 mg once daily dose and up to six months for the 200 mg twice daily dose, as it causes a dose-dependent decrease in bone mineral density (BMD). BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment. For women with moderate hepatic impairment, the recommended dosage is 150 mg once daily for up to six months. |
|---|
- Elagolix demonstrates dose-dependent hepatotoxicity
- Hepatic transaminase levels should be monitored during use
- Prolonged administration is associated with a reduction in bone mineral density, which may be partially irreversible
Elagolix is a type of Gonadotrophic
Gonadotrophic is a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that plays a crucial role in reproductive health. It includes a group of naturally occurring hormones known as gonadotropins, which are produced by the pituitary gland. These hormones, namely follicle-stimulating hormone (FSH) and luteinizing hormone (LH), regulate the reproductive processes in both males and females.
Gonadotrophic APIs are commonly used in various medical applications, particularly in the field of assisted reproductive technology (ART) and fertility treatments. They stimulate the development of ovarian follicles in females, promoting ovulation and enhancing the chances of successful conception. In males, these APIs stimulate the production of sperm cells and support the production of testosterone.
The pharmaceutical industry produces gonadotrophic APIs through advanced biotechnology techniques, such as recombinant DNA technology. This process involves the use of genetically engineered cells, typically from Chinese hamster ovary (CHO) cells, to produce highly pure and bioactive forms of FSH and LH.
Gonadotrophic APIs are typically formulated into injectable preparations, ensuring their efficient delivery and absorption into the bloodstream. These formulations are administered under the guidance of healthcare professionals and require precise dosing to achieve optimal therapeutic outcomes.
Overall, gonadotrophic APIs have revolutionized the field of reproductive medicine, providing effective solutions for infertility and hormonal imbalances. Their usage has helped countless individuals and couples to overcome fertility challenges and realize their dreams of starting a family.
Elagolix (Gonadotrophic), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
Elagolix API manufacturers & distributors
Compare qualified Elagolix API suppliers worldwide. We currently have 6 companies offering Elagolix API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, MSDS, USDMF | 229 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, FDA, GMP, MSDS | 64 products |
| Solfyn International LLP | Distributor | India | China | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS, USDMF | 24 products |
When sending a request, specify which Elagolix API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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