Synopsis
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1. 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno(2,3-d)pyrimidin-6-yl)phenyl)-3-methoxyurea
2. Orgovyx
3. Tak 385
4. Tak-385
5. Tak385
1. 737789-87-6
2. Tak-385
3. Orgovyx
4. Tak 385
5. 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
6. Chembl1800159
7. P76b05o5v6
8. 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
9. Urea, N-(4-(1-((2,6-difluorophenyl)methyl)-5-((dimethylamino)methyl)-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno(2,3-d)pyrimidin-6-yl)phenyl)-n'-methoxy-
10. Relugolix [usan:inn]
11. Unii-p76b05o5v6
12. Tak385
13. Tak-385/tak385
14. Relugolix (jan/inn)
15. Relugolix [inn]
16. Relugolix [jan]
17. Relugolix(tak-385)
18. Relugolix [usan]
19. Relugolix [who-dd]
20. Schembl778416
21. Gtpl5586
22. Relugolix [orange Book]
23. C29h27f2n7o5s
24. Dtxsid40224167
25. Rvt-601
26. Amy27916
27. Bcp21587
28. Ex-a1083
29. Myfembree Component Relugolix
30. Tak-385; Rvt-601
31. Bdbm50347982
32. Mfcd25976856
33. S5808
34. Zinc43206033
35. Cs-5917
36. Db11853
37. Relugolix Component Of Myfembree
38. Sb16721
39. Ac-35863
40. Bs-18032
41. Hy-16474
42. N-(4-(1-((2,6-difluorophenyl)methyl)-5-((dimethylamino)methyl)-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno(2,3-d)pyrimidin-6-yl)phenyl)-n'-methoxyurea
43. D10888
44. A857822
45. Ryeqo (relugolix-estradiol-norethisterone Acetate)
46. Q21099000
47. 1-(4-(1-((2,6-difluorophenyl)methyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno(2,3-d)pyrimidin-6-yl)phenyl)-3-methoxyurea
48. 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-(dimethylaminomethyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[4,5-e]pyrimidin-6-yl]phenyl]-3-methoxyurea
49. 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea;relugolix
50. 1-{4-[1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea
Molecular Weight | 623.6 g/mol |
---|---|
Molecular Formula | C29H27F2N7O5S |
XLogP3 | 3.2 |
Hydrogen Bond Donor Count | 2 |
Hydrogen Bond Acceptor Count | 11 |
Rotatable Bond Count | 9 |
Exact Mass | 623.17624448 g/mol |
Monoisotopic Mass | 623.17624448 g/mol |
Topological Polar Surface Area | 158 Ų |
Heavy Atom Count | 44 |
Formal Charge | 0 |
Complexity | 1010 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 0 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
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.
Orgovyx is indicated for the treatment of adult patients with advanced hormone-sensitive prostate cancer .
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.
Androgen Antagonists
Compounds which inhibit or antagonize the biosynthesis or actions of androgens. (See all compounds classified as Androgen Antagonists.)
L02BX
L - Antineoplastic and immunomodulating agents
L02 - Endocrine therapy
L02B - Hormone antagonists and related agents
L02BX - Other hormone antagonists and related agents
L02BX04 - Relugolix
Absorption
The Cmax 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 Cmax increases greater than proportionally to the dose. Following the administration of 120mg once daily, the steady-state AUC and Cmax 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 Tmax following oral administration is 2.25 hours.
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.
Relugolix is metabolized mainly by the CYP3A subfamily of P450 enzymes, with a smaller contribution by CYP2C8.
The average effective half-life of relugolix is 25 hours, while the average terminal elimination half-life is 60.8 hours.
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.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 37795
Submission : 2022-12-23
Status : Active
Type : II
Metrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.
DRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.
GDUFA
DMF Review : Reviewed
Rev. Date : 2024-08-05
Pay. Date : 2024-07-10
DMF Number : 39507
Submission : 2024-03-20
Status : Active
Type : II
Medichem is a vertically integrated pharmaceutical company specializing in the development & manufacturing of APIs & FDFs.
NDC Package Code : 53296-0131
Start Marketing Date : 2024-08-02
End Marketing Date : 2025-12-31
Dosage Form (Strength) : POWDER (75kg/75kg)
Marketing Category : BULK INGREDIENT
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 39995
Submission : 2024-06-14
Status : Active
Type : II
TAPI, a leading global supplier of APIs, provides over 350 products and customized CDMO solutions for every stage of development.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 37365
Submission : 2022-09-06
Status : Active
Type : II
API Imports and Exports
Importing Country | Total Quantity (KGS) |
Average Price (USD/KGS) |
Number of Transactions |
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PharmaCompass offers a list of Relugolix API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Relugolix manufacturer or Relugolix supplier for your needs.
Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Relugolix manufacturer or Relugolix supplier.
PharmaCompass also assists you with knowing the Relugolix API Price utilized in the formulation of products. Relugolix API Price is not always fixed or binding as the Relugolix Price is obtained through a variety of data sources. The Relugolix Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.
A Relugolix manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Relugolix, including repackagers and relabelers. The FDA regulates Relugolix manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Relugolix API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.
click here to find a list of Relugolix manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.
A Relugolix supplier is an individual or a company that provides Relugolix active pharmaceutical ingredient (API) or Relugolix finished formulations upon request. The Relugolix suppliers may include Relugolix API manufacturers, exporters, distributors and traders.
click here to find a list of Relugolix suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.
A Relugolix DMF (Drug Master File) is a document detailing the whole manufacturing process of Relugolix active pharmaceutical ingredient (API) in detail. Different forms of Relugolix DMFs exist exist since differing nations have different regulations, such as Relugolix USDMF, ASMF (EDMF), JDMF, CDMF, etc.
A Relugolix DMF submitted to regulatory agencies in the US is known as a USDMF. Relugolix USDMF includes data on Relugolix's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Relugolix USDMF is kept confidential to protect the manufacturer’s intellectual property.
click here to find a list of Relugolix suppliers with USDMF on PharmaCompass.
National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Relugolix as an active pharmaceutical ingredient (API).
The FDA updates the NDC directory daily. The NDC numbers for Relugolix API and other APIs are published in this directory by the FDA.
The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.
Pharmaceutical companies that manufacture Relugolix as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.
The NDC directory also contains data on finished compounded human drug products that contain Relugolix and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Relugolix NDC to their finished compounded human drug products, they may choose to do so.
click here to find a list of Relugolix suppliers with NDC on PharmaCompass.
Relugolix Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.
GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).
PharmaCompass offers a list of Relugolix GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Relugolix GMP manufacturer or Relugolix GMP API supplier for your needs.
A Relugolix CoA (Certificate of Analysis) is a formal document that attests to Relugolix's compliance with Relugolix specifications and serves as a tool for batch-level quality control.
Relugolix CoA mostly includes findings from lab analyses of a specific batch. For each Relugolix CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.
Relugolix may be tested according to a variety of international standards, such as European Pharmacopoeia (Relugolix EP), Relugolix JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Relugolix USP).