Dinalbuphine sebacate
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 | Opioid analgesic |
Pharmacokinetic data | |
Bioavailability | • IM : 85.4% (relative to nalbuphine)[1] |
Metabolism | Hydrolysis[2] |
Metabolites | Nalbuphine[1] |
Elimination half-life | • DNS: 83.2 hours (mean absorption time: 145.2 hours)[1] • Nalbuphine: 4.0 hours |
Identifiers | |
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JSmol) | |
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Dinalbuphine sebacate (DNS), also known as nalbuphine sebacate or as sebacoyl dinalbuphine ester (SDE) and sold under the brand name Naldebain, is a non-controlled
The compound is a
It was invented by professor Oliver Yoa-Pu Hu (National Defense Medical Center) and codeveloped with Lumosa Therapeutics. Naldebain received market approvals from Taiwan FDA in March 2017, Health Sciences Authority of Singapore in December 2020, the Ministry 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 the United States, China, Korea, and the Philippines.[8]
Medical uses
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]
Pharmacology
Pharmacodynamics
Nalbuphine, and hence DNS, acts as a
Pharmacokinetics
The release mechanism of dinalbuphine sebacate (DNS) upon IM injection is as follows:[13]
- Upon intramuscular injection, Naldebain first forms an oil depot in the muscle
- The oil depot gradually disperses as small droplets in the surrounding tissues
- The prodrug dinalbuphine sebacate gradually diffuses out from the droplets, after which it gets hydrolyzed to the active ingredient nalbuphine via two different mechanisms:
- a small portion of the prodrug gets hydrolyzed by esterases to release the active ingredient, nalbuphine, in the surrounding tissue cells
- the majority of the prodrug enters the bloodstream through local tissue lymph drainage and gets hydrolyzed to nalbuphine in the blood
References
- ^ S2CID 10814898.
- ^ S2CID 13206545.
- ^ a b "Dinalbuphine sebacate - Lumosa Therapeutics". AdisInsight. Springer Nature Switzerland AG.
- ^ a b "Lumosa Therapeutics Partners with Camargo Pharmaceutical Services in the Development of Naldebain(R) in the US". www.prnewswire.com (Press release).
- ^ S2CID 21247898.
- PMID 11076077.
- PMID 23460034.
- ^ a b "Lumosa Therapeutics". www.lumosa.com.tw. Retrieved 2023-11-23.
- S2CID 25378355.
- PMID 2986929.
- ISBN 978-0-7817-8763-5.
- PMID 17407276.
- ^ "BarashLumosa Therapeutics". www.lumosa.com.tw. Retrieved 2020-12-18.