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1. 4,5-epoxy-6-(3,6,9,12,15,18-hexaoxanonadec-1-yloxy)-3-methoxy-17-methylmorphinan-14-ol
2. Nktr-181
1. Oxycodegol
2. Oxycodegol [usan]
3. Nktr-181
4. J2wiv0jmml
5. Oxycodegol (usan)
6. 1211231-76-3
7. Oxicodegol
8. Loxicodegol [inn]
9. Unii-j2wiv0jmml
10. Oxycodegol [inn]
11. Loxicodegol (deleted Inn)
12. Loxicodegol [who-dd]
13. Nktr181
14. Gtpl10652
15. Who 9971
16. Db14146
17. Cs-0033429
18. D11424
19. (4r,4as,7s,7ar,12bs)-9-methoxy-7-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-ol
20. 4,5.alpha.-epoxy-6.alpha.-((2,5,8,11,14,17-hexaoxanonadecan-19-yl)oxy)-3-methoxy-17-methylmorphinan-14-ol
21. 4,5alpha-epoxy-6alpha-((2,5,8,11,14,17-hexaoxanonadecan-19-yl)oxy)-3-methoxy-17-methylmorphinan-14-ol
22. Morphinan-14-ol, 4,5-epoxy-6-(3,6,9,12,15,18-hexaoxanonadec-1-yloxy)-3-methoxy-17-methyl-, (5.alpha.,6.alpha.)-
| Molecular Weight | 595.7 g/mol |
|---|---|
| Molecular Formula | C31H49NO10 |
| XLogP3 | -1.1 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 11 |
| Rotatable Bond Count | 20 |
| Exact Mass | 595.33564676 g/mol |
| Monoisotopic Mass | 595.33564676 g/mol |
| Topological Polar Surface Area | 107 Ų |
| Heavy Atom Count | 42 |
| Formal Charge | 0 |
| Complexity | 808 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 5 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Loxicodegol was developed as an opioid analgesic with low abuse potential for use in treating chronic pain. An application has been filed for FDA approval of Loxicodegol for use in treating chronic lower back pain.
Loxicodegol displays full analgesic activity comparable to that of oxycodone, producing similar acetone-writhing test responses in mice and hot-plate test maximal latencies in rats. The safety profile of Loxicodegol is much improved from that of other opioid analgesics. The incidence of respiratory depression and sedation is reduced compared to oxycodone and morphine. Generalized pruritus occurred in 7.3% and 4.9% of subjects at 200mg and 400mg of Loxicodegol compared to 41.5% with 40mg oxycodone. Nausea occurred in 2.5%, 2.4%, and 7.3% with 100mg, 200mg, and 400mg of Loxecodegol compared to 29.3% with 40mg oxycodone. Lastly, vomiting occurred in 2.4% with both 200mg and 400mg Loxicodegol compared to 24.4% with 40mg oxycodone. Loxicodegol is much less addictive than other opioid analgesics. It produces a only a slight high at dosages of 400mg, peaking at scores only 25% that of oxycodone, with no difference compared to placebo at lower dosages. No differences have been noted between Loxicodegol and saline in self-administration or behavior reinforcement in monkeys or rats
Absorption
Loxicodegol has a Tmax of 1.8h and a bioavailability of 34% with oral administration. It enters the brain about 17-70 times more slowly than oxycodone. Loxicodegol is also a p-glycoprotein substrate further reducing its transport into the brain.
Volume of Distribution
Loxicodegol has a steady-state Vd of 4.19 L/kg.
Clearance
Loxicodegol has a clearance rate of 59.3 mL/min/kg.
Loxicodegol has a half-life of 4.53 h allowing for a longer duration of action.
Loxicodegol is a full agonist at the -opioid receptor. It also displays selectivity towards this subtype with an affinity of 237 nM compared to 4150 nM and >100000 nM for the - and -opioid receptors. The -opioid receptor is activated with an EC of 12.5 M. Activation of this receptor produces an inhibitory effect on neurotransmission through Gi/Go coupling. Opioid medications like Loxicodegol inhibit voltage gated Ca channel opening presynaptically on C fibres and activate inward-rectifying K channels post-synaptically on 2nd order neurons, leading to hyperpolarization. Together, these prevent the nociceptive signal from traveling up the spinal cord to the brain. In the brain, opioids work through a mechanism of inhibition of inhibition to allow regulatory neurons to suppress nociception.
ABOUT THIS PAGE
A Oxycodegol manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Oxycodegol, including repackagers and relabelers. The FDA regulates Oxycodegol manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Oxycodegol API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.
A Oxycodegol supplier is an individual or a company that provides Oxycodegol active pharmaceutical ingredient (API) or Oxycodegol finished formulations upon request. The Oxycodegol suppliers may include Oxycodegol API manufacturers, exporters, distributors and traders.
Oxycodegol 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 Oxycodegol 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 Oxycodegol GMP manufacturer or Oxycodegol GMP API supplier for your needs.
A Oxycodegol CoA (Certificate of Analysis) is a formal document that attests to Oxycodegol's compliance with Oxycodegol specifications and serves as a tool for batch-level quality control.
Oxycodegol CoA mostly includes findings from lab analyses of a specific batch. For each Oxycodegol 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.
Oxycodegol may be tested according to a variety of international standards, such as European Pharmacopoeia (Oxycodegol EP), Oxycodegol JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Oxycodegol USP).
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