Cilastatin attenuates VAN-induced acute renal failure in vitro by decreasing apoptosis without affecting antibacterial activity. This effect could be related, at least in part, to the reduction in accumulation of the drug in cells. Therefore, cilastatin could represent a novel therapeutic approach in reducing VAN-induced renal damage without compromising bactericidal efficacy.
|Cell lines||Proximal Tubular Primary Cell|
|Preparation method||Cells were pretreated with VAN (0.6, 3, and 6 mg/mL) alone or in combination with cilastatin (200 μg/mL) before being trypsinized, washed twice with PBS, and incubated for 30 min in the dark in 100 μL buffer containing 5 μL fluorescein isothiocyanate- (FITC-) labeled annexin V and 5 μL PI for flow cytometry.|
|Incubation time||24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Protective Effects of Cilastatin against Vancomycin-Induced Nephrotoxicity.
Humanes B, et al. Biomed Res Int. 2015;2015:704382. PMID: 26504822.
Randomized phase 2 trial to evaluate the clinical efficacy of two high-dosage tigecycline regimens versus imipenem-cilastatin for treatment of hospital-acquired pneumonia.
Ramirez J, et al. Antimicrob Agents Chemother. 2013 Apr;57(4):1756-62. PMID: 23357775.
Humanized vascular endothelial growth factor (VEGF) antibody (bevacizumab; Avastin) is a highly effective monoclonal antibody against metastatic colorectal cancer and several other advanced late stage cancers.
MCC950 is a potent, selective NLRP3 inhibitor with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
MAK683, an epigenetic drug for nasopharyngeal carcinoma, which is more prevalent in China than elsewhere, has entered Phase I clinical trials.
MTX-211 is a enamide hydrate.
GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain.
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