Generic Name
DrugBank Accession Number

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

Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Protein Chemical Formula
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Protein Average Weight
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>h5g1.1 scFv
>h5g1.1VHC + F | Heavy Chain Variable Region
>h5g1.1VHC + F | Light Chain Variable Region
Download FASTA Format
  • 5G1.1-sc
  • h5G1.1-scFv
  • Pexelizumab



For the treatment of inflammation during cardiac surgery.

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Contraindications & Blackbox Warnings
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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.


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Volume of distribution

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Protein binding

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Route of elimination

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7.0 hours to 14.5 hours.


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Adverse Effects
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Pharmacogenomic Effects/ADRs
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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.
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
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Drug Categories
Chemical TaxonomyProvided by Classyfire
Not Available
Organic Compounds
Super Class
Organic Acids
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Alternative Parents
Not Available
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Molecular Framework
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External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number


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

Clinical Trials

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


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