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Relugolix | CAS No: 737789-87-6 | GMP-certified suppliers
A medication that supports treatment of advanced prostate cancer and, in combination regimens, helps manage heavy menstrual bleeding associated with uterine fibroids for global markets.
Therapeutic categories
Primary indications
- Relugolix is indicated for the treatment of adult patients with advanced prostate cancer
- In a combination product with [estradiol] and [norethindrone], relugolix is indicated for the once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women
Product Snapshot
- Relugolix is an oral small‑molecule API supplied as film‑coated tablets
- It is used for advanced prostate cancer and, in fixed‑dose combination with estradiol and norethindrone, for heavy menstrual bleeding associated with uterine fibroids
- It holds approvals in the US, EU, and Canada, with additional investigational programs ongoing
Clinical Overview
Relugolix inhibits pituitary GnRH receptors, rapidly reducing luteinizing hormone secretion and downstream testosterone production. Suppression of circulating testosterone is central to androgen deprivation therapy, a cornerstone of advanced prostate cancer management. Clinical data show that most patients achieve castrate testosterone levels within several days of initiation, with maintenance of suppression during continued daily dosing.
The compound belongs to the n‑phenylurea class of organic molecules and exhibits pharmacologic properties consistent with systemic hormonal agents. As an orally administered antagonist, relugolix provides an alternative to injectable GnRH receptor antagonists. It interacts with multiple drug‑metabolizing pathways, including CYP3A and CYP2C8, and is a substrate and inhibitor of several transporters such as P‑glycoprotein and BCRP. These characteristics necessitate evaluation of potential drug interactions in polypharmacy settings.
Absorption, distribution, metabolism, and excretion parameters support once‑daily administration, though steady maintenance of exposure is required to sustain testosterone suppression. Relugolix has been associated with QTc prolongation risk, consistent with the safety profile of androgen deprivation therapies. Caution is advised in patients with electrolyte abnormalities, pre‑existing cardiac disease, or coadministration of QT‑prolonging agents. Fetal toxicity has been observed in nonclinical studies, and effective contraception is recommended for males with partners who may become pregnant.
Relugolix is marketed under names including Orgovyx, Relumina, and within the combination product Myfembree.
For API procurement, suppliers should provide robust control of stereochemistry, impurity profiles, and particle‑size distribution, along with full regulatory documentation to support global filings and consistent manufacturing quality.
Identification & chemistry
| Generic name | Relugolix |
|---|---|
| Molecule type | Small molecule |
| CAS | 737789-87-6 |
| UNII | P76B05O5V6 |
| DrugBank ID | DB11853 |
Pharmacology
| Summary | Relugolix is an oral competitive antagonist of gonadotropin‑releasing hormone receptors that suppresses pituitary release of luteinizing hormone and subsequently reduces testosterone production. Its pharmacologic effect produces rapid and sustained androgen suppression, a key therapeutic strategy in prostate cancer and a component of combination therapy for hormone‑dependent gynecologic conditions. The drug’s activity reflects systemic modulation of the hypothalamic‑pituitary‑gonadal axis. |
|---|---|
| Mechanism of action | The pathogenesis and progression of prostate cancer appear driven, at least in part, by the effects of testosterone.Androgen deprivation has been demonstrated to result in cell death and tumor regression in many well-differentiated prostate cancer cell lines - for this reason, androgen deprivation therapy (ADT) has become a standard in the treatment of prostate cancer, particularly in advanced disease. Testosterone production in males is carried out in the Leydig cells of testes and is stimulated by luteinizing hormone (LH), which itself is produced in the pituitary gland following the binding of gonadotropin-releasing hormone (GnRH) to corresponding GnRH receptors.Relugolix is a competitive antagonist of these GnRH receptors, thereby decreasing the release of LH and, ultimately, testosterone. |
| Pharmacodynamics | Approximately 56% of patients achieved castrate-level testosterone concentrations (<50 ng/dL) by day 4 of therapy and 97% of patients maintain these levels through 48 weeks of therapy.Relugolix requires once-daily oral administration to maintain the desired testosterone concentrations. Androgen deprivation therapies may prolong the QTc interval and should therefore be used with caution in patients having a high baseline risk of QTc prolongation, such as those with electrolyte abnormalities, congestive heart failure, or using other medications known to prolong the QTc interval.Based on its mechanism of action and data from animal studies, relugolix may result in fetal harm if administered to pregnant females - male patients with female partners should be advised to use effective contraception throughout therapy and for 2 weeks following cessation of therapy to prevent inadvertent fetal exposure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gonadotropin-releasing hormone receptor | Humans | antagonist |
ADME / PK
| Absorption | The C<sub>max</sub> and AUC of orally-administered relugolix increase proportionally following single doses - in contrast, with repeat dosing the AUC remains proportional to the dose while the C<sub>max</sub> increases greater than proportionally to the dose.Following the administration of 120mg once daily, the steady-state AUC and C<sub>max</sub> of relugolix were 407 (± 168) ng.hr/mL and 70 (± 65) ng/mL, respectively. The absolute oral bioavailability of relugolix is approximately 12% and the median T<sub>max</sub> following oral administration is 2.25 hours. |
|---|---|
| Half-life | The average effective half-life of relugolix is 25 hours, while the average terminal elimination half-life is 60.8 hours. |
| Protein binding | Relugolix is 68-71% protein-bound in plasma, primarily to albumin and, to a lesser extent, α1-acid glycoprotein. |
| Metabolism | Relugolix is metabolized mainly by the CYP3A subfamily of P450 enzymes, with a smaller contribution by CYP2C8. |
| Route of elimination | Approximately 81% of an orally administered dose was recovered in the feces, of which 4.2% was unchanged parent drug, while 4.1% of the dose was recovered in the urine, of which 2.2% remained unchanged. |
| Clearance | The average renal clearance of relugolix is 8 L/h with a total clearance of 26.4 L/h. |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility, so formulation typically uses solid oral technologies that can support dissolution enhancement.
- Stable for standard solid‑dose handling; logP near 4 may favor lipid-based or polymeric solubilization approaches if higher bioavailability is required.
- Food has no meaningful impact on pharmacokinetics, allowing flexible administration without meal‑related formulation constraints.
Regulatory status
| Lifecycle | Several U.S. patents for the API have recently expired, while others extend protection into 2036–2037, indicating a transition phase with partial remaining exclusivity. With products marketed in Canada, the US, and the EU, the API is present in mature markets but not yet fully exposed to generic competition in the United States. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Relugolix is supplied by a small number of originator manufacturers responsible for both the standalone API and its combination or monotherapy branded products. These products have established commercial presence across the US, EU, and Canada. Several key US patents have recently expired in 2024, while others extend to 2036–2037, indicating that partial loss of exclusivity may allow early generic development activity, though full generic entry will depend on the longer‑dated protections. |
|---|
Safety
| Toxicity | Data regarding overdose of relugolix are unavailable. |
|---|
- Limited overdose data are available
- Employ controlled handling and dosing precision due to unknown high‑exposure toxicological profile
- As a GnRH receptor antagonist, relugolix can significantly suppress sex hormone pathways
Relugolix 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.
Relugolix (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.
Relugolix API manufacturers & distributors
Compare qualified Relugolix API suppliers worldwide. We currently have 5 companies offering Relugolix API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA | 762 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, MSDS | 66 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 140 products |
When sending a request, specify which Relugolix 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.).
Use the list above to find high-quality Relugolix API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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