MEDI-5884
MEDI-5884 (REG-101) is a humanized IgG4Pκ neutralizing monoclonal antibody targeting endothelial lipase (EL), with an IC50 of 1.3 nM and 1.7 nM against human and cynomolgus monkey EL, respectively; its Kd values for human and cynomolgus monkey EL are 4.1 nM and 1.6 nM, respectively. MEDI-5884 increases plasma levels of HDL-C, apolipoprotein A1 (ApoA1) and phospholipids, while causing a slight increase in LDL-C and apolipoprotein B (ApoB) levels. MEDI-5884 can be used in research related to cardiovascular diseases, coronary heart disease, coronary atherosclerosis and stable coronary artery disease.
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- CAS No.: 2643310-75-0
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Human
Endothelial lipase
MEDI-5884 (0.5-30 mg/kg; s.c.; single dose) neutralizes endogenous endothelial lipase in cynomolgus monkeys, producing dose-dependent, sustained elevations in HDL-C, ApoA1, and phospholipids, with a twofold HDL-C increase maintained for 2 months at the 30 mg/kg dose[1].
MEDI-5884 (10 mg/kg; s.c.; two doses on day 28 and day 42) elevates HDL-C in cynomolgus monkeys pretreated with a PCSK9 inhibitor, while the associated LDL-C increase is mitigated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (8-week-old male, adenoviral overexpression of human endothelial lipase to reduce endogenous HDL-C)[1]
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Dosage:30 mg/kg
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Administration:s.c.; single dose
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Result:Prevented further reduction in HDL-C and restored HDL-C nearly to baseline concentrations (baseline ~100 mg/dl, day 4 after Ad-hEL ~50 mg/dl, day 5 after treatment ~75 mg/dl).
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Animal Model:Macaca fascicularis (2 to 3 years old, male, 2.4 to 3.0 kg)[1]
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Dosage:0.5 mg/kg; 6 mg/kg; 30 mg/kg
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Administration:s.c.; single dose
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Result:Increased plasma HDL-C, ApoA1, and phospholipids in a dose-dependent manner.
Achieved an approximate twofold increase in HDL-C within 2 weeks at 30 mg/kg, which persisted for 2 months.
Produced similar maximum HDL-C increase at 6 mg/kg, with HDL-C returning to baseline by study end.
Resulted in smaller HDL-C increase at 0.5 mg/kg, which returned to baseline within 3 weeks.
Caused smaller magnitude, dose-dependent increases in LDL-C and ApoB, with no clear effect on triglycerides.
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Animal Model:Macaca fascicularis (2 to 3 years old, male, 2.4 to 3.0 kg, pretreated with PCSK9 inhibitor to lower LDL-C)[1]
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Dosage:10 mg/kg
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Administration:s.c.; two doses on day 28 and day 42
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Result:Maintained ability to raise HDL-C to a similar degree as seen in monkeys without PCSK9 inhibitor pretreatment.
Blunted the magnitude of LDL-C increase relative to MEDI-5884 alone.
Changed ApoA1 and ApoB matching patterns of HDL-C and LDL-C, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 2643310-75-0
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SMILES
N/A
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Synonyms
REG-101
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Le Lay JE, et al. Blocking endothelial lipase with monoclonal antibody MEDI5884 durably increases high density lipoprotein in nonhuman primates and in a phase 1 trial. Science translational medicine. 2021 Apr 21;13(590):eabb0602. [Content Brief]
[2]. Ruff CT, et al. LEGACY: Phase 2a Trial to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamic Effects of the Anti-EL (Endothelial Lipase) Antibody MEDI5884 in Patients With Stable Coronary Artery Disease. Arteriosclerosis, thrombosis, and vascular biology. 2021 Dec;41(12):3005-3014. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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