C5a
Synonyms
Prepro-C5, CPAMD4, Complement C5, C3 And PZP-Like Alpha-2-Macroglobulin Domain-Containing Protein 4, C5D, Complement Component 5, C5a, Anaphylatoxin C5a Analog, C5a Anaphylatoxin, C5b, ECLZB, C5
Description
Activation of C5 by a C5 convertase initiates the spontaneous assembly of the late complement components, C5-C9, into the membrane attack complex. C5b has a transient binding site for C6. The C5b-C6 complex is the foundation upon which the lytic complex is assembled.Derived from proteolytic degradation of complement C5, C5 anaphylatoxin is a mediator of local inflammatory process. Binding to the receptor C5AR1 induces a variety of responses including intracellular calcium release, contraction of smooth muscle, increased vascular permeability, and histamine release from mast cells and basophilic leukocytes. C5a is also a potent chemokine which stimulates the locomotion of polymorphonuclear leukocytes and directs their migration toward sites of inflammation.
KO Status
RenMab: F0
Drug Information
Launched drugs: 2
Drugs in clinical trials: 17
Latest Research Phase: Approved
Drug Name
Code
Phase
Company
Indications
Clinical Trials
Ravulizumab
ALXN-1210, ALXN-1810
Approved
Alexion Pharmaceuticals Inc
Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Glomerulonephritis, IGA, Coronavirus Disease 2019 (COVID-19), Respiratory Distress Syndrome, Adult, Atypical Hemolytic Uremic Syndrome, Thrombotic Microangiopathies, Lupus Nephritis, Pneumonia, Viral, Neuromyelitis Optica, Acute Lung Injury, Amyotrophic Lateral Sclerosis
Eculizumab
5G1-1, HAL-1, LEX-98, h-5G1.1
Approved
Alexion Pharmaceuticals Inc
Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Atypical Hemolytic Uremic Syndrome, Delayed Graft Function, Neuromyelitis Optica, Asthma, Guillain-Barre Syndrome
Eculizumab biosimilar (CinnaGen)
Phase 3 Clinical
Cinnagen
Hemoglobinuria, Paroxysmal
Vilobelimab
IFX-1, CaCP-29
Phase 3 Clinical
Beijing Mabworks Biotech Co Ltd, Inflarx
Shock, Septic, Granulomatosis with Polyangiitis, Drug-Related Side Effects and Adverse Reactions, Pyoderma Gangrenosum, Microscopic Polyangiitis, Coronavirus Disease 2019 (COVID-19), Sepsis, Lung Diseases, Interstitial, Hidradenitis Suppurativa, Systemic Inflammatory Response Syndrome
Pozelimab
REGN-3918
Phase 3 Clinical
Regeneron Pharmaceuticals Inc
Hemoglobinuria, Paroxysmal
Crovalimab
SKY-59, RG-6107, CH-7092230, RO-7092230, RO-7112689, RO-7112689/
Phase 3 Clinical
F. Hoffmann-La Roche Ltd, Chugai Pharmaceutical Co Ltd
Hemoglobinuria, Paroxysmal, Atypical Hemolytic Uremic Syndrome, Anemia, Sickle Cell
BDB-001
BDB-001, BDB001, BDB 001
Phase 3 Clinical
Staidson(Beijing) Biopharmaceuticals Co Ltd
Solid tumours, Coronavirus Disease 2019 (COVID-19), Hidradenitis Suppurativa
Zilucoplan
RA-101495, RA-101495-SC
Phase 3 Clinical
Ra Pharma
Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Lupus Nephritis, Hemolytic-Uremic Syndrome
Nomacopan
EV-576, rVA576, rEV-576
Phase 3 Clinical
Evolutec
Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Arthritis, Rheumatoid, Sjogren's Syndrome, Autoimmune Diseases, Atypical Hemolytic Uremic Syndrome, Thrombotic Microangiopathies, Hemolytic-Uremic Syndrome, Pemphigoid, Bullous, Asthma, Inflammation, Guillain-Barre Syndrome, Keratoconjunctivitis
Eculizumab biosimilar (IBC GENERIUM)
Phase 3 Clinical
Ibc Generium
Hemoglobinuria, Paroxysmal, Atypical Hemolytic Uremic Syndrome
References
Title
Authors
Source
Complete cDNA sequence of human complement pro-C5. Evidence of truncated transcripts derived from a single copy gene
Haviland D.L., Haviland J.C., Fleischer D.T., Hunt A., Wetsel R.A.,
J. Immunol. 146:362-368(1991)
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)
The MGC Project Team,
Genome Res. 14:2121-2127(2004)
Molecular analysis of human complement component C5: localization of the structural gene to chromosome 9
Wetsel R.A., Lemons R.S., Lebeau M.M., Barnum S.R., Noack D., Tack B.F.,
Biochemistry 27:1474-1482(1988)
Isolation and sequence analysis of a cDNA clone encoding the fifth complement component
Lundwall A.B., Wetsel R.A., Kristensen T., Whitehead A.S., Woods D.E., Ogden R.C., Colten H.R., Tack B.F.,
J. Biol. Chem. 260:2108-2112(1985)
Primary structural analysis of the polypeptide portion of human C5a anaphylatoxin. Polypeptide sequence determination and assignment of the oligosaccharide attachment site in C5a
Fernandez H.N., Hugli T.E.,
J. Biol. Chem. 253:6955-6964(1978)
Group B streptococci inactivate complement component C5a by enzymic cleavage at the C-terminus
Bohnsack J.F., Mollison K.W., Buko A.M., Ashworth J.C., Hill H.R.,
Biochem. J. 273:635-640(1991)
The amino terminus of the human C5a receptor is required for high affinity C5a binding and for receptor activation by C5a but not C5a analogs
DeMartino J.A., Van Riper G., Siciliano S.J., Molineaux C.J., Konteatis Z.D., Rosen H., Springer M.S.,
J. Biol. Chem. 269:14446-14450(1994)
Residues 21-30 within the extracellular N-terminal region of the C5a receptor represent a binding domain for the C5a anaphylatoxin
Chen Z., Zhang X., Gonnella N.C., Pellas T.C., Boyar W.C., Ni F.,
J. Biol. Chem. 273:10411-10419(1998)
Human plasma N-glycoproteome analysis by immunoaffinity subtraction, hydrazide chemistry, and mass spectrometry
Liu T., Qian W.-J., Gritsenko M.A., Camp D.G. II, Monroe M.E., Moore R.J., Smith R.D.,
J. Proteome Res. 4:2070-2080(2005)
Sequence-specific assignments in the 1H NMR spectrum of the human inflammatory protein C5a
Zuiderweg E.R.P., Mollison K.W., Henkin J., Carter G.W.,
Biochemistry 27:3568-3580(1988)