Vilobelimab
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Identification
- Summary
Vilobelimab is an antibody directed against anti-human complement factor 5a is used to treat COVID-19 in adults for emergency use.
- Generic Name
- Vilobelimab
- DrugBank Accession Number
- DB16416
- Background
Vilobelimab is a chimeric monoclonal immunoglobulin G4 (IgG4) antibody that binds to the soluble form of human C5a with high affinity. It consists of mouse anti-human complement factor 5a (C5a) monoclonal binding sites (variable regions of heavy and light chain regions) and human gamma 4 heavy chain and light kappa chain constant regions.6 In April 2023, the FDA issued an emergency use authorization (EUA) for vilobelimab for the treatment of COVID-19 in hospitalized adults requiring mechanical ventilation or artificial life support. The drug is not yet fully approved for this condition.7
- Type
- Biotech
- Groups
- Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- C6456H9976N1716O2054S44
- Protein Average Weight
- 149000.0 Da (approximate)
- Sequences
>Vilobelimab heavy chain QVQLQQSGPQLVRPGTSVKISCKASGYSFTTFWMDWVKQRPGQGLEWIGRIDPSDSESRL DQRFKDRATLTVDKSSSTVYMQLSSPTSEDSAVYYCARGNDGYYGFAYWGQGTLVTVSSA STKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPSCPAPEFLGGPSVF LFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYR VVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKN QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGN VFSCSVMHEALHNHYTQKSLSLSLGK
>Vilobelimab light chain DIVLTQSPASLAVSLGQRATISCKASQSVDYDGDSYMKWYQQKPGQPPKLLIYAASNLQS GIPARFSGSGSGTDFTLNIHPVEEEDAATYYCQQSNEDPYTFGGGTKLEIKRTVAAPSVF IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- KEGG DRUG: Vilobelimab [Link]
- Synonyms
- IFX-1
- Vilobelimab
- External IDs
- CACP 29
- CaCP29
- IFX-1
Pharmacology
- Indication
Vilobelimab is used for emergency use to treat coronavirus disease 19 (COVID-19) in hospitalized adults when initiated within 48 hours of receiving invasive mechanical ventilation (IMV) or extracorporeal membrane oxygenation (ECMO). However, vilobelimab is not FDA-approved for this use.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Coronavirus disease 2019 (covid‑19) •••••••••••• ••••• •••••••••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Vilobelimab is believed to attenuate inflammation and associated tissue damage by binding to complement factor 5a (C5a).6 In clinical trials of patients with severe COVID-19 pneumonia requiring IMV or ECMO, vilobelimab reduced the median concentrations of C5a from the baseline plasma concentrations of 118.29 ng/mL to 14.53 ng/mL: this effect persisted up to Day 30 after the initiation of treatment. However, the direct clinical relevance of C5a plasma concentration reduction is unclear.6
- Mechanism of action
The complement system is a critical innate immune response against pathogens.4 Activation of the complement cascade results in proteolytic cleavage of the complement factor C5, generating C5a and C5b.4 C5a is a potent anaphylatoxin that binds to the C5a receptor to initiate an inflammatory cascade. The C5a/C5aR1 signalling pathway promotes enhanced vascular permeability, coagulation, proinflammatory cytokine release, and recruitment and activation of neutrophils and other myeloid cells.5,6 Ultimately, C5a also initiates neutrophil-driven tissue damage.4,5 Complement activation and high levels of C5a have been implicated in various inflammatory conditions,5 such as septic shock,4 antineutrophilic cytoplasmic antibody (ANCA) vasculitis,2 and viral infections such as avian influenza A (H7N9) virus infection and Coronavirus disease (COVID-19).1,3
The complement system can be activated through three pathways: classical, lectin, and alternative pathways. The lectin pathway is triggered by binding of either mannose-binding lectin protein (MBL) or ficolin to pathogens, such as bacterial or fungal carbohydrate structures and proteins.5 Experimental studies suggest that the SARS-CoV-2 virus nucleocapsid protein can bind to the mannan-binding lectin serine protease 2, thereby activating the downstream complement pathway and generating C5a. Because high levels of C5a have been identified in patients with severe COVID-19, C5a was suggested as a key mediator of acute respiratory distress syndrome and thrombotic microangiopathy associated with COVID-19.3 Vilobelimab is a chimeric monoclonal IgG4-kappa antibody that binds to complement factor 5a (C5a) with a dissociation constant of 9.6pM and blocks its interaction with the C5a receptor.6
Target Actions Organism UComplement C5 inhibitorHumans - Absorption
In healthy subjects who received a single intravenous infusion of vilobelimab ranging from 2 mg/kg to 4 mg/kg, the Cmax showed dose proportionality while the AUC showed greater-than-dose proportionality.6
Pre-dose plasma samples were collected in patients with severe COVID-19 pneumonia requiring IMV or ECMO. Following intravenous infusion of vilobelimab 800 mg on Days 1, 2, and 4, the pre-dose geometric mean (geometric CV%) plasma concentration of vilobelimab on Day 8 was 137.9 µg/mL (51%).6
- Volume of distribution
No information is available.
- Protein binding
No information is available.
- Metabolism
As with other monoclonal antibodies, vilobelimab is expected to undergo nonspecific degradation into small peptides and individual amino acids.
- Route of elimination
No information is available.
- Half-life
The elimination half-life of vilobelimab following a 4 mg/kg single intravenous dose in healthy subjects was 95 hours.6
- Clearance
No information is available.
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There is no information regarding the acute toxicity or overdose of vilobelimab.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Vilobelimab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Vilobelimab. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Vilobelimab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Vilobelimab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Vilobelimab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Gohibic Injection 10 mg/1mL Intravenous InflaRx GmbH 2023-04-04 Not applicable US
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
- Not Available
Chemical Identifiers
- UNII
- F5T0RF9ZJA
- CAS number
- 2250440-41-4
References
- General References
- Sun S, Zhao G, Liu C, Fan W, Zhou X, Zeng L, Guo Y, Kou Z, Yu H, Li J, Wang R, Li Y, Schneider C, Habel M, Riedemann NC, Du L, Jiang S, Guo R, Zhou Y: Treatment with anti-C5a antibody improves the outcome of H7N9 virus infection in African green monkeys. Clin Infect Dis. 2015 Feb 15;60(4):586-95. doi: 10.1093/cid/ciu887. Epub 2014 Nov 27. [Article]
- Jayne D: Complement inhibition in ANCA vasculitis. Nephrol Ther. 2019 Nov;15(6):409-412. doi: 10.1016/j.nephro.2019.04.001. Epub 2019 Oct 17. [Article]
- Vlaar APJ, de Bruin S, Busch M, Timmermans SAMEG, van Zeggeren IE, Koning R, Ter Horst L, Bulle EB, van Baarle FEHP, van de Poll MCG, Kemper EM, van der Horst ICC, Schultz MJ, Horn J, Paulus F, Bos LD, Wiersinga WJ, Witzenrath M, Rueckinger S, Pilz K, Brouwer MC, Guo RF, Heunks L, van Paassen P, Riedemann NC, van de Beek D: Anti-C5a antibody IFX-1 (vilobelimab) treatment versus best supportive care for patients with severe COVID-19 (PANAMO): an exploratory, open-label, phase 2 randomised controlled trial. Lancet Rheumatol. 2020 Dec;2(12):e764-e773. doi: 10.1016/S2665-9913(20)30341-6. Epub 2020 Sep 28. [Article]
- Bauer M, Weyland A, Marx G, Bloos F, Weber S, Weiler N, Kluge S, Diers A, Simon TP, Lautenschlager I, Grundling M, Jaschinski U, Simon P, Nierhaus A, Moerer O, Reill L, Jorres A, Guo R, Loeffler M, Reinhart K, Riedemann N: Efficacy and Safety of Vilobelimab (IFX-1), a Novel Monoclonal Anti-C5a Antibody, in Patients With Early Severe Sepsis or Septic Shock-A Randomized, Placebo-Controlled, Double-Blind, Multicenter, Phase IIa Trial (SCIENS Study). Crit Care Explor. 2021 Nov 17;3(11):e0577. doi: 10.1097/CCE.0000000000000577. eCollection 2021 Nov. [Article]
- Guo RF, Ward PA: Role of C5a in inflammatory responses. Annu Rev Immunol. 2005;23:821-52. doi: 10.1146/annurev.immunol.23.021704.115835. [Article]
- FDA EUA Drug Products: GOHIBIC (vilobelimab) injection, for intravenous use [Link]
- FDA: FDA authorizes Gohibic (vilobelimab) injection for the treatment of COVID-19 [Link]
- External Links
- 2639620
- Wikipedia
- Vilobelimab
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data3 Recruiting Treatment Pyoderma Gangrenosum 1 somestatus stop reason just information to hide 2 Completed Treatment C.Surgical Procedure; Cardiac / Systemic Inflammatory Response Syndrome (SIRS) 1 somestatus stop reason just information to hide 2 Completed Treatment Granulomatosis With Polyangiitis / Microscopic Polyangiitis (MPA) 1 somestatus stop reason just information to hide 2 Completed Treatment Hidradenitis Suppurativa (HS) 2 somestatus stop reason just information to hide 2 Completed Treatment Pyoderma Gangrenosum 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 10 mg/1mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- C5 is a precursor of C5a anaphylatoxin and C5b. Vilobelimab is an inhibitor of C5a.
- General Function
- 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
- Specific Function
- chemokine activity
- Gene Name
- C5
- Uniprot ID
- P01031
- Uniprot Name
- Complement C5
- Molecular Weight
- 188303.705 Da
References
- Vlaar APJ, de Bruin S, Busch M, Timmermans SAMEG, van Zeggeren IE, Koning R, Ter Horst L, Bulle EB, van Baarle FEHP, van de Poll MCG, Kemper EM, van der Horst ICC, Schultz MJ, Horn J, Paulus F, Bos LD, Wiersinga WJ, Witzenrath M, Rueckinger S, Pilz K, Brouwer MC, Guo RF, Heunks L, van Paassen P, Riedemann NC, van de Beek D: Anti-C5a antibody IFX-1 (vilobelimab) treatment versus best supportive care for patients with severe COVID-19 (PANAMO): an exploratory, open-label, phase 2 randomised controlled trial. Lancet Rheumatol. 2020 Dec;2(12):e764-e773. doi: 10.1016/S2665-9913(20)30341-6. Epub 2020 Sep 28. [Article]
- Riedemann NC, Habel M, Ziereisen J, Hermann M, Schneider C, Wehling C, Kirschfink M, Kentouche K, Guo R: Controlling the anaphylatoxin C5a in diseases requires a specifically targeted inhibition. Clin Immunol. 2017 Jul;180:25-32. doi: 10.1016/j.clim.2017.03.012. Epub 2017 Mar 30. [Article]
- FDA EUA Drug Products: GOHIBIC (vilobelimab) injection, for intravenous use [Link]
Drug created at December 23, 2020 18:12 / Updated at April 15, 2023 22:28