Murepavadin

Research use only, not for human use.

Murepavadin (POL7080) is a highly potent, specific, macrocycle Pseudomonas antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa.

Murepavadin (POL7080) is a highly potent, specific, macrocycle Pseudomonas antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa.Bacterial Infection Phase 3 Clinical.

Murepavadin has activity against P. aeruginosa with MIC50 and MIC90 values both of 0.12 mg/L.Murepavadin inhibits megalin-mediated uptake of gentamicin in vitro with an IC50 value of 5.84 μM.

Murepavadin (s.c.; 0-100 mg/kg) is active in pre-clinical animal models including infections with XDR isolates. Animal Model:murine models of P. aeruginosa infectionDosage:0-100 mg/kg Administration:Subcutaneous, q24h or q12h Result:Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection.Animal Model:Mouse, rat, rabbit, and monkey Dosage:0-5 mg/kg Administration:Intraperitoneal or subcutaneous, single Result:Followed a two-compartment model following intravenous administration and decline of plasma concentrations.Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) .Had high bioavailability (67.79%) after subcutaneous (s.c.) administration in rats but had low oral bioavailability (<0.01%).Had a linear relationship between ELF AUC and unbound plasma AUC in mouse.

POL7080 | POL 7080

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

944252-63-5

1553.837

C73H112N22O16

>98% (HPLC)

——

CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)N1)CC4=CNC5=CC=CC=C54)C(C)O)CO)C)CCN)CCN)CC6=CNC7=CC=CC=C76)CCN)CCN)CCCN)CCN

cyclo[Ala-Ser-D-Pro-Pro-Thr-Trp-Ile-Dab-Orn-D-Dab-Dab-Trp-Dab-Dab]

(-20℃)

With Ice Pack

≥ 2 years