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| Clinical data | |
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| Other names | DNS; Nalbuphine sebacate; Sebacoyldinalbuphine; SDN; Sebacoyl dinalbuphine ester; SDE; LT-1001 |
| Routes of administration | Intramuscular injection |
| Drug class | Opioidanalgesic |
| Pharmacokinetic data | |
| Bioavailability | •IMTooltip Intramuscular injection: 85.4% (relative tonalbuphine)[1] |
| Metabolism | Hydrolysis[2] |
| Metabolites | Nalbuphine[1] |
| Eliminationhalf-life | •DNS: 83.2 hours (mean absorption time: 145.2 hours)[1] •Nalbuphine: 4.0 hours |
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| CAS Number | |
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| Chemical and physical data | |
| Formula | C52H68N2O10 |
| Molar mass | 881.120 g·mol−1 |
| 3D model (JSmol) | |
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Dinalbuphine sebacate (DNS), also known asnalbuphine sebacate or assebacoyl dinalbuphine ester (SDE) and sold under the brand nameNaldebain, is a non-controlledopioidanalgesic which is used as a 7-day long-actinginjection in the treatment of moderate to severepostoperative pain.[3][4][5]
The compound is adiester ofnalbuphine (Nubain) joined via asebacic acid linker, and acts as a long-lastingprodrug of nalbuphine via slowhydrolysis.[5][2][6] It was developed to extend theduration of action of nalbuphine, which has a short duration and requires frequent injections.[7][5][2][1] Whereas nalbuphine must be injected every 4 to 6 hours, a single injection of DNS lasts for up to 7 to 10 days.[5]
It was invented by Professor Oliver Yoa-Pu Hu (National Defense Medical Center) and codeveloped with Lumosa Therapeutics. Naldebain received market approvals fromTaiwan FDA in March 2017,Health Sciences Authority ofSingapore in December 2020, theMinistry of Public Health of Thailand in December 2021, the Drug Control Authority of Malaysia in 2022, State Service of Ukraine on Medicines and Drugs Control and Brunei Darussalam Medicines Control Authority (BDMCA) in 2023.[3][4] Development is ongoing in theUnited States, China, Korea, and the Philippines.[8]
Naldebain is indicated for the relief of moderate to severe acute postsurgical pain, administered intramuscularly. The product is available in single-use vials; 2 mL single use vial (75 mg/mL) for IM injection is packaged in a carton.[8]
Nalbuphine, and hence DNS, acts as amixed agonist/antagonistopioid modulator, or more specifically as a moderate-efficacypartial agonist orantagonist of theμ-opioid receptor and as a high-efficacypartial agonist of theκ-opioid receptor.[5][9][10][11][12]
The release mechanism of dinalbuphine sebacate (DNS) upon IM injection is as follows:[13]
