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]
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| Identifiers | |
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3D model (JSmol)
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| Properties | |
| C7H7FN6O2 | |
| Molar mass | 226.171 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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The KL-50 molecule was patented by Pharminox Limited in 2013, detailing its potential use in treating MMR-/MGMT- gliomas.[5]
References
edit- ^ Huseman, Eric; Lo, Anna; Fedorova, Olga; Elia, James; Gueble, Susan; Lin, Kingson; Sundaram, Ranjini; Burgenske, Danielle; Oh, Joonseok; Liu, Jinchan; Menges, Fabian; Rees, Matthew; Ronan, Melissa; Roth, Jennifer; Batista, Victor; Crawford, Jason; Sarkaria, Jann; Pyle, Anna; Bindra, Ranjit; Herzon, Seth (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; Liu, Jinchan; Menges, Fabian; Rees, Matthew G.; Ronan, Melissa M.; Roth, Jennifer A.; Batista, Victor S.; Crawford, Jason M.; Pyle, Anna M.; Bindra, Ranjit S.; Herzon, Seth B. (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. PMC 11409917. PMID 38815248.
- ^ "Slow and steady action makes brain cancer drug candidate more selective". Chemical & Engineering News.
- ^ 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 application 2013338104