| Identification | Back Directory | [Name]
SPR-741 | [CAS]
1179330-52-9 | [Synonyms]
NAB741
SPR-741
SPR741TFA
SPR741 (NAB741)
2-10-Polymyxin B1, N-acetyl-3-D-serine- | [Molecular Formula]
C44H73N13O13 | [MDL Number]
MFCD33029242 | [MOL File]
1179330-52-9.mol | [Molecular Weight]
992.15 |
| Hazard Information | Back Directory | [Uses]
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741[1][2]. | [in vivo]
SPR741 has the ability to permeabilize the outer membrane of Gram-negative bacteria, thus sensitizing them to hydrophobic antibiotics. SPR741 has a significantly safety profile of compared to that of polymyxin B, which suffers severe, dose-limiting nephrotoxicity in humans. In multiday rodent and nonhuman primate studies, polymyxin B exhibited nephrotoxicity at a far-lower exposure-normalized dose than SPR741[1]. | [References]
[1] Corbett D, et al. Potentiation of Antibiotic Activity by a Novel Cationic Peptide: Potency and Spectrum of Activity of SPR741. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00200-17. DOI:10.1128/AAC.00200-17
[2] Eckburg PB, et al. Safety, Tolerability, Pharmacokinetics, and Drug Interaction Potential of SPR741, an Intravenous Potentiator, after Single and Multiple Ascending Doses and When Combined with β-Lactam Antibiotics in Healthy Subjects. Antimicrob Agents Chemother. 2019 Aug 23;63(9). pii: e00892-19. DOI:10.1128/AAC.00892-19 |
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