|Systematic (IUPAC) name|
|Trade names||Antrypol, 309 F or 309 Fourneau, Bayer 205, Moranyl, Naganin, Naganine|
|ATC code||P01CX02 (WHO) QP51AE02 (WHO)|
|(what is this?)|
Suramin is an antiparasitic drug developed by Oskar Dressel and Richard Kothe of Bayer, Germany in 1916, and is still sold by Bayer under the brand name Germanin. The formula of suramin was kept secret by Bayer for commercial reasons, however, it was elucidated and published in 1924 by Ernest Fourneau and his team of the Pasteur Institute.:378–379
It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system.
The most frequent adverse reactions are nausea and vomiting. About 90% of patients will get an urticarial rash that disappears in a few days without needing to stop treatment. There is a greater than 50% chance of adrenal cortical damage, but only a smaller proportion will require lifelong corticosteroid replacement. It is common for patients to get a tingling or crawling sensation of the skin with suramin. Suramin will cause clouding of the urine which is harmless: patients should be warned of this to avoid them becoming alarmed.
Kidney damage and exfoliative dermatitis occur less commonly.
Suramin has been applied clinically to HIV/AIDS patients resulting in a significant number of fatal occurrences and as a result the application of this molecule was abandoned for this condition.
The molecular formula of suramin is C51H40N6O23S6. It is a symmetric molecule in the center of which lies a urea (NH–CO–NH) functional group. Suramin contains eight benzene rings, four of which are fused in pairs (naphthalene), four amide groups (in addition to the urea) and six sulfonic acid groups. When given as drug, it is usually as the sodium sulfonate, with six sodium ions on the sulfonate groups rather than hydrogens.
It may have some activity against RNA viruses.
In addition to antagonism of P2 receptors, Suramin inhibits the activation of heterotrimeric G proteins in a variety of other GPCRs with varying potency. It prevents the association of heteromeric G proteins and therefore the receptors guanine exchange functionality (GEF). With this blockade the GDP will not release from the Gα subunit so it can not be replaced by a GTP and become activated. This has the effect of blocking downstream G protein mediated signaling of various GPCR proteins including rhodopsin, the A1 adenosine receptor, and the D2 dopamine receptor.
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- "WHO Model List of Essential Medicines. 18th list (April 2013)" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
- Darsaud A, Chevrier C, Bourdon L, Dumas M, Buguet A, Bouteille B (January 2004). "Megazol combined with suramin improves a new diagnosis index of the early meningo-encephalitic phase of experimental African trypanosomiasis". Tropical Medicine and International Health. 9 (1): 83–91. doi:10.1046/j.1365-3156.2003.01154.x. PMID 14728611.
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- Kaplan, Lawrence D.; Wolfe, Peter R.; Volberding, Paul A.; Feorino, Paul; Abrams, Donald I.; Levy, Jay A.; Wong, Roberta; Kaufman, Lilian; Gottlieb, Michael S. (1987). "Lack of response to suramin in patients with AIDS and AIDS-related complex". The American Journal of Medicine. 82 (3): 615–620. doi:10.1016/0002-9343(87)90108-2. PMID 3548350.
- Ahles TA, Herndon JE, Small EJ, et al. (November 2004). "Quality of life impact of three different doses of suramin in patients with metastatic hormone-refractory prostate carcinoma: results of Intergroup O159/Cancer and Leukemia Group B 9480". Cancer. 101 (10): 2202–8. doi:10.1002/cncr.20655. PMID 15484217.
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- Wolner I, Kassack MU, Ullmann H, Karel A, Hohenegger M (October 2005). "Use-dependent inhibition of the skeletal muscle ryanodine receptor by the suramin analogue NF676". British Journal of Pharmacology. 146 (4): 525–33. doi:10.1038/sj.bjp.0706359. PMC . PMID 16056233.
- Erguven M, Akev N, Ozdemir A, Karabulut E, Bilir A (August 2008). "The inhibitory effect of suramin on telomerase activity and spheroid growth of C6 glioma cells". Medical Science Monitor. 14 (8): BR165–73. PMID 18667993.
- Mastrangelo, Eloise; Pezzullo, Margherita; Tarantino, Delia; Petazzi, Roberto; Germani, Francesca; Kramer, Dorothea; Robel, Ivonne; Rohayem, Jacques; Bolognesi, Martino; Milani, Mario (2012). "Structure-based inhibition of norovirus RNA-dependent RNA-polymerases". Journal of Molecular Biology. 419 (3-4): 198–210. doi:10.1016/j.jmb.2012.03.008.
- Beindl W, Mitterauer T, Hohenegger M, Ijzerman AP, Nanoff C, Freissmuth M (August 1996). "Inhibition of receptor/G protein coupling by suramin analogues". Molecular Pharmacology. 50 (2): 415–23. PMID 8700151.