Chemical Property of (2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoic acid
Chemical Property:
- PSA：0.00000
- LogP:0.00000
- XLogP3:3.3
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:8
- Rotatable Bond Count:13
- Exact Mass:641.37884898
- Heavy Atom Count:46
- Complexity:1080
- Purity/Quality:
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99% *data from raw suppliers
Eculizumab *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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Useful:
- Canonical SMILES:CCCCC(C(=O)O)N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C
- Isomeric SMILES:CCCC[C@H](C(=O)O)N(C(=O)[C@@H](CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)[C@H](CC(C)(C)C)NC(=O)N3[C@@H](CCC[C@@H]3C)C
- Recent EU Clinical Trials:A RANDOMIZED, OPEN-LABEL ECULIZUMAB AND RAVULIZUMAB CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF POZELIMAB AND CEMDISIRAN COMBINATION THERAPY IN PATIENTS WITH PAROXYSMAL NOCTURNAL HEMOGLOBINURIA WHO ARE CURRENTLY TREATED WITH ECULIZUMAB OR RAVULIZUMAB
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Description
Eculizumab, a fully humanized anti-C5 monoclonal antibody, was introduced for treating patients with PNH to reduce hemolysis. It is the first therapy
to be approved for this rare and life-threatening form of hemolytic anemia. PNH
is a clonal hematopoietic stem-cell disorder that is characterized by the
production of abnormal red blood cells (RBCs) with a deficiency of surface
proteins that protect the cells against attack by the body’s complement system.
Complement-mediated destruction of the susceptible RBCs results in intravascular
hemolysis, the primary clinical manifestation in all PNH patients.
Previously, patients with PNH have mainly been managed supportively, with
red cell transfusions as required, and treatments such as folate and iron
supplementation, anticoagulation for thrombotic disease, and the occasional use
of steroids during hemolytic crises. Allogenic stem cell transplantation is
currently the only curative option for PNH; however, it is associated with
significant morbidity and mortality. Eculizumab therapy is aimed at preventing
red cell lysis through blockade of complement activation process and the
production of the membrane attack complex. Eculizumab specifically binds to the
human complement protein C5 with high affinity (IC50 ＝ 2 nM) and inhibits its
cleavage to C5a and C5b, which is a key step in the pathway leading to the
membrane attack complex C5b-C9.Eculizumab has been granted orphan drug status from both the FDA and European regulatory agencies.The most serious adverse reaction associated with eculizumab therapy is meningococcal infections. Eculizumab is contraindicated in patients who are not vaccinated against Neisseria meningitidis or who have N. meningitidis infections. The most common adverse reactions with eculizumab include headache (44%), nasopharyngitis (23%), back pain (19%), and nausea (16%).
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Uses
Treatment of autoimmune disease such as rheumatoid arthritis, membranous nephritis, lupus nephritis, dermatomyositis, and autoimmune hemolytic anemias.
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Clinical Use
Recombinant monoclonal antibody:Paroxysmal nocturnal haemoglobinuria (PNH)Atypical haemolytic uraemic syndrome (aHUS)Refractory generalized myasthenia gravis (gMG) in
patients who are anti-acetylcholine receptor (AChR)
antibody-positive (MG)
