Molecular Weight(MW): 558.14
Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.
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Choose Selective ALK Inhibitors
|Description||Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.|
|Features||Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.|
LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells. 
|In vivo||LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg. |
Enzymatic kinase profiling description:All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement)
|In vitro||DMSO||20 mg/mL warmed (35.83 mM)|
|Ethanol||3 mg/mL (5.37 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02450903||Completed||Drug: LDK378||Non-Small-Cell Lung Cancer||Novartis Pharmaceuticals|Novartis||August 21 2015||Phase 2|
|NCT02276027||Recruiting||Drug: BYL719|Drug: INC280|Drug: LDK378|Drug: MEK162||Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma||Novartis Pharmaceuticals|Novartis||January 20 2015||Phase 2|
|NCT02040870||Completed||Drug: LDK378||Non-Small Cell Lung Cancer||Novartis Pharmaceuticals|Novartis||March 7 2014||Phase 1|Phase 2|
|NCT01950481||Completed||Drug: LDK378||Normal Hepatic Function|Impaired Hepatic Function||Novartis Pharmaceuticals|Novartis||January 2014||Phase 1|
|NCT01772797||Completed||Drug: LDK378|Drug: AUY922||Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer||Novartis Pharmaceuticals|Novartis||June 2013||Phase 1|
|NCT01685060||Completed||Drug: LDK378||Non-Small Cell Lung Cancer||Novartis Pharmaceuticals|Novartis||November 26 2012||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
how to reconstitute the inhibitor for oral administration to mice?
You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.