NAV

Narsoplimab

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Narsoplimab is an anti-MASP-2 antibody currently being investigated for use in transplant-associated thrombotic microangiopathies and IgA nephropathy.

Generic Name
Narsoplimab
DrugBank Accession Number
DB16418
Background

Thrombotic microangiopathies (TMA), including thrombotic thrombocytopenic purpura and atypical hemolytic uremic syndrome, are associated with injury and dysregulation of microvascular endothelium and platelets.1 Evidence increasingly points to a role for the complement system in TMA.1,2 Mannan-associated lectin-binding serine protease-2 (MASP-2) is a major effector in the complement lectin pathway.1,2 Narsoplimab (OMS721), a human IgG4λ anti-MASP-2 antibody, is under consideration as a treatment for hematopoietic stem cell transplant-associated TMA (HSCT-TMA/TA-TMA) and IgA nephropathy.3,4

Narsoplimab is under investigation in clinical trial NCT03205995 (Safety and Efficacy Study of OMS721 in Patients With Atypical Hemolytic Uremic Syndrome).

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • ANTI-MASP-2 MONOCLONAL ANTIBODY OMS721
  • IMMUNOGLOBULIN G4 (226-PROLINE), ANTI-(HUMAN MANNAN-BINDING LECTIN-ASSOCIATED SERINE PROTEASE 2) (HUMAN MONOCLONAL OMS721 .GAMMA.4-CHAIN), DISULFIDE WITH HUMAN MONOCLONAL OMS721 .LAMBDA.-CHAIN, DIMER
  • IMMUNOGLOBULIN G4-LAMBDA, ANTI-(HOMO SAPIENS MANNAN-BINDING LECTIN SERINE PROTEASE 2 (MANNOSE-BINDING PROTEIN-ASSOCIATED SERINE PROTEASE 2, EC=3.4.21.104) HUMAN MONOCLONAL ANTIBODY .GAMMA.4 HEAVY CHAIN (1-445) (HOMO SAPIENS VH (IGHV2-26*01 (94%) (IGHD)-I
  • MASP-2 antibody
  • Narsoplimab
External IDs
  • OMS-721
  • OMS00620646
  • OMS620646
  • OMS721
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Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Transplant-associated thrombotic microangiopathy (TA-TMA) has complex underlying pathophysiology but generally involves complement activation associated with endothelial injury, microthrombus development, and downstream organ dysfunction.1,2 Studies have demonstrated a role for the alternative and lectin complement pathways in TMA. Within the lectin pathway, considerable interest has fallen on the effector protein mannan-associated lectin-binding serine protease-2 (MASP-2), which cleaves C4 and C2 to form the C3 convertase C4bC2a.1 Narsoplimab, a human IgG4λ anti-MASP-2 antibody, appears effective in limiting lectin pathway-associated microvascular activation/injury in TA-TMA, presumably by directly inhibiting the formation of C4bC2a.1,2,3

TargetActionsOrganism
AMannan-binding lectin serine protease 2
antagonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

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.
Not Available
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
Not Available

Chemical Identifiers

UNII
FT24ZQQ5RP
CAS number
2108782-45-0

References

General References
  1. Elhadad S, Chapin J, Copertino D, Van Besien K, Ahamed J, Laurence J: MASP2 levels are elevated in thrombotic microangiopathies: association with microvascular endothelial cell injury and suppression by anti-MASP2 antibody narsoplimab. Clin Exp Immunol. 2021 Jan;203(1):96-104. doi: 10.1111/cei.13497. Epub 2020 Aug 5. [Article]
  2. Young JA, Pallas CR, Knovich MA: Transplant-associated thrombotic microangiopathy: theoretical considerations and a practical approach to an unrefined diagnosis. Bone Marrow Transplant. 2021 Aug;56(8):1805-1817. doi: 10.1038/s41409-021-01283-0. Epub 2021 Apr 19. [Article]
  3. Kaplon H, Reichert JM: Antibodies to watch in 2021. MAbs. 2021 Jan-Dec;13(1):1860476. doi: 10.1080/19420862.2020.1860476. [Article]
  4. Lafayette RA, Rovin BH, Reich HN, Tumlin JA, Floege J, Barratt J: Safety, Tolerability and Efficacy of Narsoplimab, a Novel MASP-2 Inhibitor for the Treatment of IgA Nephropathy. Kidney Int Rep. 2020 Aug 13;5(11):2032-2041. doi: 10.1016/j.ekir.2020.08.003. eCollection 2020 Nov. [Article]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentImmunoglobulin A Nephropathy1
3Unknown StatusTreatmentAtypical Hemolytic Uremic Syndrome(aHUS) / Thrombotic Microangiopathies1
2CompletedTreatmentThrombotic Microangiopathies1
2RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
2RecruitingTreatmentHematopoietic Stem Cell Transplantation (SCT) / Thrombotic Microangiopathies1

Pharmacoeconomics

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

Properties

State
Not Available
Experimental Properties
Not Available

Targets

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Details1. Mannan-binding lectin serine protease 2
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Serine-type endopeptidase activity
Specific Function
Serum protease that plays an important role in the activation of the complement system via mannose-binding lectin. After activation by auto-catalytic cleavage it cleaves C2 and C4, leading to their...
Gene Name
MASP2
Uniprot ID
O00187
Uniprot Name
Mannan-binding lectin serine protease 2
Molecular Weight
75701.685 Da
References
  1. Elhadad S, Chapin J, Copertino D, Van Besien K, Ahamed J, Laurence J: MASP2 levels are elevated in thrombotic microangiopathies: association with microvascular endothelial cell injury and suppression by anti-MASP2 antibody narsoplimab. Clin Exp Immunol. 2021 Jan;203(1):96-104. doi: 10.1111/cei.13497. Epub 2020 Aug 5. [Article]

Drug created at December 23, 2020 18:13 / Updated at July 18, 2023 22:58