XP-21279 is a sustained-release levodopa (L-DOPA) prodrug and hence a dopamine precursor and non-selective dopamine receptor agonist which was under development for the treatment of Parkinson's disease.[4][1][3] It is taken by mouth.[1][2][3]
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| Other names | XP21279 |
| Routes of administration | Oral[1][2][3] |
| Drug class | Dopamine precursor; Dopamine receptor agonist |
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| Chemical and physical data | |
| Formula | C19H21NO6 |
| Molar mass | 359.378 g·mol−1 |
| 3D model (JSmol) | |
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Pharmacology
editThe drug is said to add a five-carbon ester conjugate to levodopa that allows it to be actively transported by high-capacity nutrient transporters throughout the entire gastrointestinal tract.[2][3][5] Subsequently, it is rapidly converted into levodopa by carboxylesterases.[2][3][5] Levodopa itself can only be transported by a short section of the small intestine and hence XP-21279 allows more time for levodopa to be absorbed, in turn resulting in an increased duration and possibly reduced fluctuations in dopamine levels between levodopa doses.[1][2][3]
Clinical studies
editAs of June 2015, XP-21279 was in phase 2 clinical trials.[4] As of May 2022, there have been no further developmental updates.[4] It was reported in 2018 that development of the drug had been discontinued several years prior.[6] A 2019 review reported that results were conflicting in phase 2 trials and that this likely resulted in the discontinuation of the drug's development.[5]
Chemistry
editMany sources do not report the chemical structure of XP-21279, suggesting that its exact structure has not been disclosed.[7][8][9][6][10] However, one source appears to report its chemical structure.[11]
See also
editReferences
edit- ^ a b c d Hauser RA (2011). "Future treatments for Parkinson's disease: surfing the PD pipeline". The International Journal of Neuroscience. 121 Suppl 2: 53–62. doi:10.3109/00207454.2011.620195. PMID 22035030.
- ^ a b c d e Ondo W (October 2014). "IPX066 , a mixed immediate/sustained-release levodopa preparation for Parkinson's disease". Expert Opinion on Pharmacotherapy. 15 (14): 2081–2085. doi:10.1517/14656566.2014.950224. PMID 25146967.
- ^ a b c d e f Freitas ME, Ruiz-Lopez M, Fox SH (November 2016). "Novel Levodopa Formulations for Parkinson's Disease". CNS Drugs. 30 (11): 1079–1095. doi:10.1007/s40263-016-0386-8. PMID 27743318.
- ^ a b c "XP 21279". AdisInsight. Springer Nature Switzerland AG. 26 May 2022. Retrieved 27 September 2024.
- ^ a b c Hengartner D, Fernandez HH (February 2019). "The next chapter in symptomatic Parkinson disease treatments". Parkinsonism & Related Disorders. 59. Elsevier BV: 39–48. doi:10.1016/j.parkreldis.2019.01.002. PMID 30661840.
- ^ a b Cacciatore I, Ciulla M, Marinelli L, Eusepi P, Di Stefano A (April 2018). "Advances in prodrug design for Parkinson's disease". Expert Opinion on Drug Discovery. 13 (4): 295–305. doi:10.1080/17460441.2018.1429400. PMID 29361853.
- ^ "XP21279: Uses, Interactions, Mechanism of Action". DrugBank Online. 19 March 2008. Retrieved 27 September 2024.
- ^ "Delving into the Latest Updates on XP-21279 with Synapse". Synapse. 20 September 2024. Retrieved 27 September 2024.
- ^ "XP 21279". PubChem. Retrieved 27 September 2024.
- ^ Markovic M, Deodhar S, Machhi J, Yeapuri P, Saleh M, J Edagwa B, et al. (February 2022). "Prodrug Therapies for Infectious and Neurodegenerative Diseases". Pharmaceutics. 14 (3): 518. doi:10.3390/pharmaceutics14030518. PMC 8953076. PMID 35335894.
- ^ Haddad F, Sawalha M, Khawaja Y, Najjar A, Karaman R (December 2017). "Dopamine and Levodopa Prodrugs for the Treatment of Parkinson's Disease". Molecules. 23 (1): 40. doi:10.3390/molecules23010040. PMC 5943940. PMID 29295587.