Synopsis
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1. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide
2. S-297995
3. Symproic
1. 916072-89-4
2. S-297995
3. 03ksi6wlxh
4. S 297995
5. S-297,995
6. (4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-n-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide
7. Naldemedine [usan]
8. Unii-03ksi6wlxh
9. Naldemedine [usan:inn]
10. Naldemedine [mi]
11. Naldemedine [inn]
12. Naldemedine (usan/inn)
13. Naldemedine [who-dd]
14. Gtpl9150
15. Schembl9880572
16. Chembl2105755
17. Dtxsid501030350
18. Bdbm50503604
19. Db11691
20. Compound 9k [pmid: 30446313]
21. Hy-19627
22. Morphinan-7-carboxamide, 17-(cyclopropylmethyl)-6,7-didehydro-4,5-epoxy-3,6,14- Trihydroxy-n-(1-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl)-,(5alpha)-
23. Cs-0016072
24. J3.573.009e
25. D10188
26. Q6960846
27. 17-(cyclopropylmethyl)-6,7-didehydro-4,5a-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide
28. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide
Molecular Weight | 570.6 g/mol |
---|---|
Molecular Formula | C32H34N4O6 |
XLogP3 | 3.2 |
Hydrogen Bond Donor Count | 4 |
Hydrogen Bond Acceptor Count | 9 |
Rotatable Bond Count | 6 |
Exact Mass | 570.24783482 g/mol |
Monoisotopic Mass | 570.24783482 g/mol |
Topological Polar Surface Area | 141 Ų |
Heavy Atom Count | 42 |
Formal Charge | 0 |
Complexity | 1140 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 4 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
1 of 1 | |
---|---|
Drug Name | SYMPROIC |
Active Ingredient | NALDEMEDINE TOSYLATE |
Company | SHIONOGI INC (Application Number: N208854. Patents: 9108975, RE46365, RE46375) |
For the treatment of opioid-induced constipation.
FDA Label
Rizmoic is indicated for the treatment of opioid-induced constipation (OIC) in adult patients who have previously been treated with a laxative.
Naldemedine is an opioid receptor antagonist with restricted movement across the blood brain barrier. This allows it to antagonize the periperal effects of opioid drugs such as constipation without interfering with the effects on the central nervous system.
A06AH05
A - Alimentary tract and metabolism
A06 - Drugs for constipation
A06A - Drugs for constipation
A06AH - Peripheral opioid receptor antagonists
A06AH05 - Naldemedine
Absorption
Tmax is 0.75 h. Administration with a high-fat meal reduces Cmax by 35% and increases Tmax to 2.5 h.
Route of Elimination
57% of naldemedine is excreted in the urine with 16-18% as the parent compound and 35% is excreted in the feces.
Volume of Distribution
The apparent volume of disribution during the terminal phase is 155 L
Naldemedine is mainly metabolized to nor-naldemedine by CYP3A. Some metabolism to naldemedine-3-glucuronide occurs via UGT1A3. Both metabolites are acitive but less potent than naldemedine. The relative exposures of these metabolites are 9-13% and <3% for nor-naldemedine and naldemedine-3-glucuronide respectively. Naldemedine is also cleaved in the intestine to form benzamidine and naldemedine carboxylic acid.
The terminal elimination half life is 11 h.
Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors. The binding of opioid agonists to peripheral mu-opioid receptors slows the transit of feces through the intestine resulting in constipation. By antagonizing mu-opioid receptors, naldemedine inhibits this effect.
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PharmaCompass offers a list of Naldemedine 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 Naldemedine manufacturer or Naldemedine supplier for your needs.
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PharmaCompass also assists you with knowing the Naldemedine API Price utilized in the formulation of products. Naldemedine API Price is not always fixed or binding as the Naldemedine Price is obtained through a variety of data sources. The Naldemedine Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.
A nalmedine manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of nalmedine, including repackagers and relabelers. The FDA regulates nalmedine manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. nalmedine 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 nalmedine manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.
A nalmedine supplier is an individual or a company that provides nalmedine active pharmaceutical ingredient (API) or nalmedine finished formulations upon request. The nalmedine suppliers may include nalmedine API manufacturers, exporters, distributors and traders.
click here to find a list of nalmedine suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.
nalmedine 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 nalmedine 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 nalmedine GMP manufacturer or nalmedine GMP API supplier for your needs.
A nalmedine CoA (Certificate of Analysis) is a formal document that attests to nalmedine's compliance with nalmedine specifications and serves as a tool for batch-level quality control.
nalmedine CoA mostly includes findings from lab analyses of a specific batch. For each nalmedine 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.
nalmedine may be tested according to a variety of international standards, such as European Pharmacopoeia (nalmedine EP), nalmedine JP (Japanese Pharmacopeia) and the US Pharmacopoeia (nalmedine USP).