Chemistry:KL-50
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KL-50 (also known as RR-004 by its developer Pharminox Limited) is a drug candidate designed to treat glioblastoma. It functions by alkylating DNA yielding O6-(2-fluoroethyl)guanine which causes DNA interstrand crosslinks. Half of the cancers are unable to repair the DNA damage.[1][2][3][4]
The KL-50 molecule was patented by Pharminox Limited in 2013, detailing its potential use in treating MMR-/MGMT- gliomas.[5]
References
- ↑ Huseman, Eric; Lo, Anna; Fedorova, Olga; Elia, James; Gueble, Susan; Lin, Kingson; Sundaram, Ranjini; Burgenske, Danielle et al. (2023). "Mechanism of Action of KL-50, a Novel Imidazotetrazine for the Treatment of Drug-Resistant Brain Cancers". ChemRxiv. doi:10.26434/chemrxiv-2023-zwj94.
- ↑ Huseman, Eric D.; Lo, Anna; Fedorova, Olga; Elia, James L.; Gueble, Susan E.; Lin, Kingson; Sundaram, Ranjini K.; Oh, Joonseok et al. (30 May 2024). "Mechanism of Action of KL-50, a Candidate Imidazotetrazine for the Treatment of Drug-Resistant Brain Cancers". Journal of the American Chemical Society 146 (27): 18241–18252. doi:10.1021/jacs.3c06483. PMID 38815248. Bibcode: 2024JAChS.14618241H.
- ↑ "Slow and steady action makes brain cancer drug candidate more selective" (in en). https://cen.acs.org/synthesis/medicinal-chemistry/Slow-steady-action-makes-brain-cancer-drug-candidate-more-selective/102/web/2024/06.
- ↑ Leslie, Mitch (2 November 2022). "New Strategy May Thwart Glioblastoma Resistance". Cancer Discovery 12 (11): 2488–2489. doi:10.1158/2159-8290.CD-NB2022-0055.
- ↑ US patent application 2013338104
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