Identification

Generic Name
Pexelizumab
DrugBank Accession Number
DB04949
Background

Pexelizumab is a humanized monoclonal antibody used as an immunosuppressive drug. It is being investigated by Alexion Pharmaceuticals.

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
>h5g1.1 scFv
MADIQMTQSPSSLSASVGDRVTITCGASENIYGALNWYQRKPGKAPKLLIYGATNLADGV
PSRFSGSGSGTDYTLTISSLQPEDFATYYCQNVLNTPLTFGQGTKVEIKRTGGGGSGGGG
SGGGGSQVQLVQSGAEVEKPGASVKKVSCKASGYIFSNYWIQWVRQAPGQGLEWMGEILP
GSGSTEYAQKFQGRVTMTADTSTSTAYMELSSLRSEDTAVYYCARYFFGSSPNYWYFDVW
GQGTLVTVSS
>h5g1.1VHC + F | Heavy Chain Variable Region
QVQLVQSGAEVKKPGASVKVSCKASGYIFSNYWIQWVRQAPGQGLEWMGEILPGSGSTEY
AQKFQGRVTMTADTSTSTAYMELSSLRSEDTAVYYCARYFFGSSPNWYFVWGQGT
>h5g1.1VHC + F | Light Chain Variable Region
DIQMTQSPSLSASVGDRVTITCGASENIYGALNWYQRKPGKAPKLLIYGATNLADGVPSR
FSGSGSGTDYTLTISSLQPEDFATYYCQNVLNTPLTFGQGTKVEIK
Download FASTA Format
Synonyms
  • 5G1.1-sc
  • h5G1.1-scFv
  • Pexelizumab

Pharmacology

Indication

For the treatment of inflammation during cardiac surgery.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Myocardial injury and dysfunction in acute infarction and during cardiac surgery with cardiopulmonary bypass (CPB) are associated with an undesirable systemic inflammatory response, in which the complement cascade plays a major role. In animal models C5 inhibition has been found to significantly reduce myocardial infarct size and decrease cellular necrosis and apoptosis. Pexelizumab is a humanized, monoclonal, single-chain antibody fragment that inhibits C5, thereby blocking its cleavage into active forms.

Mechanism of action

Although inflammation is a normal response, continued exposure to foreign surfaces, toxic antigens, and tissue injury results in pathologic local and systemic inflammation (SIRS). This response involves multiple humoral and cellular components, including the coagulation (Factor XII, thrombin, Proteins C and S, platelets) and complement systems, cytokines (TNF-alpha, interleukins), leukocytes, monocytes, adhesion molecules (ICAM-1), and endothelial cells, among others. The complement system is a group of glycoproteins, which, when activated, results in the formation of C3-convertase, which converts C3 to C3a and C3b. C3a cleaves C5 to C5a and C5b. C5b, in conjunction with C6, C7, C8, and C9, forms the membrane attack or terminal complement complex (TCC) C5b-9. Both C5a and C5b-9 activate, promote, and amplify inflammatory components, and likely play central roles in the development of SIRS, tissue injury, reperfusion injury, and apoptosis. Pexelizumab, a recombinant humanized single chain monoclonal antibody to C5, blocks the conversion of C5 to C5a and C5b-9.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

7.0 hours to 14.5 hours.

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Pexelizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Pexelizumab.
AducanumabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Aducanumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pexelizumab.
AlirocumabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Alirocumab.
AmivantamabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Amivantamab.
AnifrolumabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Anifrolumab.
AnsuvimabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Ansuvimab.
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Anthrax immune globulin human.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Pexelizumab is combined with Antilymphocyte immunoglobulin (horse).
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Food Interactions
Not Available

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
CHZ6OLQ3UU
CAS number
219685-93-5

References

General References
  1. Fitch JC, Rollins S, Matis L, Alford B, Aranki S, Collard CD, Dewar M, Elefteriades J, Hines R, Kopf G, Kraker P, Li L, O'Hara R, Rinder C, Rinder H, Shaw R, Smith B, Stahl G, Shernan SK: Pharmacology and biological efficacy of a recombinant, humanized, single-chain antibody C5 complement inhibitor in patients undergoing coronary artery bypass graft surgery with cardiopulmonary bypass. Circulation. 1999 Dec 21-28;100(25):2499-506. [Article]
  2. Armstrong PW, Mahaffey KW, Chang WC, Weaver WD, Hochman JS, Theroux P, Rollins S, Todaro TG, Granger CB: Concerning the mechanism of pexelizumab's benefit in acute myocardial infarction. Am Heart J. 2006 Apr;151(4):787-90. [Article]
  3. Granger CB, Mahaffey KW, Weaver WD, Theroux P, Hochman JS, Filloon TG, Rollins S, Todaro TG, Nicolau JC, Ruzyllo W, Armstrong PW: Pexelizumab, an anti-C5 complement antibody, as adjunctive therapy to primary percutaneous coronary intervention in acute myocardial infarction: the COMplement inhibition in Myocardial infarction treated with Angioplasty (COMMA) trial. Circulation. 2003 Sep 9;108(10):1184-90. Epub 2003 Aug 18. [Article]
  4. Fleisig AJ, Verrier ED: Pexelizumab -- a C5 complement inhibitor for use in both acute myocardial infarction and cardiac surgery with cardiopulmonary bypass. Expert Opin Biol Ther. 2005 Jun;5(6):833-9. [Article]
  5. Haverich A, Shernan SK, Levy JH, Chen JC, Carrier M, Taylor KM, Van de Werf F, Newman MF, Adams PX, Todaro TG, van der Laan M, Verrier ED: Pexelizumab reduces death and myocardial infarction in higher risk cardiac surgical patients. Ann Thorac Surg. 2006 Aug;82(2):486-92. [Article]
  6. Thomas TC, Rollins SA, Rother RP, Giannoni MA, Hartman SL, Elliott EA, Nye SH, Matis LA, Squinto SP, Evans MJ: Inhibition of complement activity by humanized anti-C5 antibody and single-chain Fv. Mol Immunol. 1996 Dec;33(17-18):1389-401. [Article]
PubChem Substance
347909855
Wikipedia
Pexelizumab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedPreventionCardiopulmonarybypass / Coronary Artery Bypass Grafting (CABG)1
3CompletedTreatmentAcute Myocardial Infarction (AMI)1
3CompletedTreatmentCoronary Artery Disease (CAD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Drug created at October 21, 2007 22:23 / Updated at February 21, 2021 18:51