Zosurabalpin Explained

Drug Name:	Zosurabalpin
C:	43
H:	50
N:	8
O:	5
S:	1
Iupac Name:	4-[(11S,14S,17S)-14-(4-aminobutyl)-11-(3-aminopropyl)-17-(1H-indol-3-ylmethyl)-16-methyl-12,15,18-trioxo-2-thia-4,10,13,16,19-pentazatricyclo[19.4.0.0<sup>3,8</sup>]pentacosa-1(25),3(8),4,6,21,23-hexaen-22-yl]benzoic acid
Synonyms:	N^2.2.2.1,3-anhydro(N^2-[(2-([2-(aminomethyl)-4'-carboxy[1,1'-biphenyl]-3-yl]sulfanyl)pyridin-3-yl)methyl]-L-ornithyl-L-lysyl-N-methyl-L-tryptophan
Cas Number:	2379336-76-0
Pubchem:	148636827
Unii:	5Y6W5N1U0S
Smiles:	CN1[C@H](C(=O)NCC2=C(C=CC=C2SC3=C(CN[C@H](C(=O)N[C@H](C1=O)CCCCN)CCCN)C=CC=N3)C4=CC=C(C=C4)C(=O)O)CC5=CNC6=CC=CC=C65
Stdinchi:	1S/C43H50N8O5S/c1-51-37(23-30-25-47-34-12-3-2-10-32(30)34)40(53)49-26-33-31(27-16-18-28(19-17-27)43(55)56)11-6-15-38(33)57-41-29(9-8-22-46-41)24-48-35(14-7-21-45)39(52)50-36(42(51)54)13-4-5-20-44/h2-3,6,8-12,15-19,22,25,35-37,47-48H,4-5,7,13-14,20-21,23-24,26,44-45H2,1H3,(H,49,53)(H,50,52)(H,55,56)/t35-,36-,37-/m0/s1
Stdinchikey:	NJFUXFYUHIHHOJ-FSEITFBQSA-N

Zosurabalpin (RG6006, Abx-MCP, Ro7223280) is an experimental antibiotic developed in a collaboration between the pharmaceutical company Roche and scientists from Harvard University, for the treatment of carbapenem-resistant Acinetobacter baumannii (CRAB). It targets a lipopolysaccharide transporter.^[1] It works by recognizing a composite binding site made up of both the Lpt transporter and its LPS substrate.^[2] The chemical family to which it belongs was first disclosed in 2019, but the particular structure of RG6006 remained confidential until publication of the testing results in 2023.^{[3] [4] [5]}

See also

• Clovibactin
• Novobiocin
• Teixobactin

Notes and References

1. Zampaloni C, Mattei P, Bleicher K, Winther L, Thäte C, Bucher C, Adam JM, Alanine A, Amrein KE, Baidin V, Bieniossek C, Bissantz C, Boess F, Cantrill C, Clairfeuille T, Dey F, Di Giorgio P, du Castel P, Dylus D, Dzygiel P, Felici A, García-Alcalde F, Haldimann A, Leipner M, Leyn S, Louvel S, Misson P, Osterman A, Pahil K, Rigo S, Schäublin A, Scharf S, Schmitz P, Stoll T, Trauner A, Zoffmann S, Kahne D, Young JA, Lobritz MA, Bradley KA . 6 . A novel antibiotic class targeting the lipopolysaccharide transporter . Nature . 625. 7995. January 2024 . 566–571 . 38172634 . 10.1038/s41586-023-06873-0 . free . 10794144 .
2. Pahil KS, Gilman MS, Baidin V, Clairfeuille T, Mattei P, Bieniossek C, Dey F, Muri D, Baettig R, Lobritz M, Bradley K, Kruse AC, Kahne D . 6 . A new antibiotic traps lipopolysaccharide in its intermembrane transporter . Nature . 572–577 . January 2024 . 625 . 7995 . 38172635 . 10.1038/s41586-023-06799-7 . free . 10794137 .
3. US . 20190321440A1 . Peptide macrocycles against acinetobacter baumannii. . Bleicher K, Cheang D, Di Giorgio P, Hu T, Jenny C, Mattei P, Schmitz P, Stoll T . Hoffmann La Roche Inc. . 21 November 2023 .
4. Book: Erbetti I, Ferrari L, Ortombina A, Savoia P, Felici A, Bissantz C, Zampaloni C . 2109. In vitro and in vivo Killing Kinetics of Zosurabalpin (RG6006) Against Acinetobacter baumannii. . Open Forum Infectious Diseases . December 2023 . 10 . Suppl 2 . Oxford University Press . 10.1093/ofid/ofad500.1733 .
5. Theuretzbacher U . Evaluating the innovative potential of the global antibacterial pipeline . Clinical Microbiology and Infection. October 2023 . 37805036 . 10.1016/j.cmi.2023.09.024 . 263722286 .