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

F0

Drug Information

Launched drugs: 2
Drugs in clinical trials: 17
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

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

Ravulizumab

ALXN-1210, ALXN-1810

Approved

Alexion Pharmaceuticals Inc

Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Glomerulonephritis, IGA, Coronavirus Disease 2019 (COVID-19), Thrombotic Microangiopathies, Respiratory Distress Syndrome, Adult, Atypical Hemolytic Uremic Syndrome, Lupus Nephritis, Pneumonia, Viral, Neuromyelitis Optica, Acute Lung Injury, Amyotrophic Lateral Sclerosis

Eculizumab biosimilar (IBC GENERIUM)

Phase 3 Clinical

Ibc Generium

Hemoglobinuria, Paroxysmal, Atypical Hemolytic Uremic Syndrome

Zilucoplan

RA-101495, RA-101495-SC

Phase 3 Clinical

Ra Pharma

Myasthenia Gravis, Hemoglobinuria, Paroxysmal, Lupus Nephritis, Hemolytic-Uremic Syndrome

Pozelimab

REGN-3918

Phase 3 Clinical

Regeneron Pharmaceuticals Inc

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, Hidradenitis Suppurativa, Systemic Inflammatory Response Syndrome

BDB-001

BDB-001, BDB001, BDB 001

Phase 3 Clinical

Staidson(Beijing) Biopharmaceuticals Co Ltd

Solid tumours, Coronavirus Disease 2019 (COVID-19), Hidradenitis Suppurativa

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, Keratoconjunctivitis, Inflammation, Guillain-Barre Syndrome

Avacincaptad pegol

ARC-187, ARC-1905

Phase 3 Clinical

Archemix

Geographic Atrophy, Stargardt Disease, Macular Degeneration

Crovalimab

SKY-59, RG-6107, CH-7092230, RO-7092230, RO-7112689, RO-7112689/F01

Phase 3 Clinical

F. Hoffmann-La Roche Ltd, Chugai Pharmaceutical Co Ltd

Hemoglobinuria, Paroxysmal

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)

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