Berdazimer

Identification

Summary

Berdazimer is a nitric oxide (NO)-releasing agent used to treat topical molluscum contagiosum.

Generic Name
Berdazimer
DrugBank Accession Number
DB18712
Background

Berdazimer is a polymeric substance consisting of a polysiloxane backbone (Si-O-Si bonds) with covalently bound N-diazeniumdiolate nitric oxide (NO) donors. It releases NO through exposure to proton donors like water, which will degrade the N-diazeniumdiolate entity.2 Berdazimer was previously investigated as a potential treatment for molluscum contagiosum, a viral cutaneous infection mainly affecting children, sexually active adults, and immunocompromised patients. It is one of the 5 most prevalent skin diseases in the world and the third-most common viral skin infection in children.3 Previously, the first line treatment for molluscum contagiosum was surgical excision, although it poses challenges such as repeated doctor visits, post-surgical scarring and skin discoloration, and fear and anxiety in the pediatric population.3

On Jan 05, 2024, the FDA approved berdazimer under the brand name ZELSUVMI for the treatment of adult and pediatric molluscum contagiosum, and it is the first drug to be approved for this condition. This decision is based on positive results demonstrated in 2 Phase 3 trials, B-SIMPLE 4 and B-SIMPLE 2, where reduced lesion counts were observed with once-a-day uses of berdazimer.5

Type
Small Molecule
Groups
Approved
Synonyms
  • Silsesquioxanes, 3-(2-hydroxy-1-methyl-2-nitrosohydrazinyl)propyl 3-(methylamino)propyl, polymers with silicic acid (h4sio4) tetra-et ester, hydroxy-terminated
External IDs
  • NVN-1000 free acid
  • NVN1000 free acid

Pharmacology

Indication

Berdazimer is indicated for the topical treatment of molluscum contagiosum (MC) in adults and pediatric patients 1 year of age and older.4

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofMolluscum contagiosum•••••••••••••••••• ••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

The pharmacodynamics of berdazimer are unknown.4

Mechanism of action

Although the mechanism of action in treating molluscum contagiosum is unknown, berdazimer is known to be a nitric oxide (NO)-releasing agent from the N-diazeniumdiolate nitric oxide donors.1 NO has been known to have broad-spectrum antimicrobial and antiviral activity, likely due to the S-nitrosylation of proteins and cytotoxicity to viral replication from reactive oxygen species.1,2

Absorption

Plasma hydrolyzed MAP3 (hMAP3), a structural marker for berdazimer, and nitrate levels were evaluated in n=34 subjects 2 to 12 years of age with MC. Subjects applied berdazimer once daily for two weeks to a total treatment area of 484 cm2 (mean lesion count=34), applying a mean dose of approximately 3 mL/day. No subjects had quantifiable plasma hMAP3 concentrations on day 1; two subjects had quantifiable concentrations on day 15. Mean plasma nitrate levels were similar on days 1 and 15 and remained relatively flat during the PK sampling period (baseline through 1, 3, and 6 hours post-application). There were no apparent differences in methemoglobin levels throughout the study.4

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

There are no available data on berdazimer use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of berdazimer to pregnant rats and rabbits increased malformations in the presence of severe maternal toxicity. The clinical relevance of this finding is unknown given the bioavailability of berdazimer following oral administration is significantly higher than topical application.4

The available data do not allow the calculation of relevant comparisons between the systemic exposure of berdazimer observed in animal studies and the systemic exposure expected in humans after topical use of berdazimer.4

The carcinogenic potential of berdazimer gel was assessed in a 2-year dermal mouse carcinogenicity study. No drug-related tumor findings were associated with daily topical administration of berdazimer gel to mice at doses up to 4% berdazimer gel.4

Berdazimer was mutagenic in a bacterial mutagenicity assay (Ames assay) but was not clastogenic in an in vitro chromosomal aberration assay in human peripheral blood lymphocytes or in an in vivo micronucleus assay in rats.4

There were no berdazimer-related effects on male or female fertility and early embryonic parameters in rats at oral doses up to 189 mg/kg/day.4

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
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Berdazimer sodiumORT9SID4QY1846565-00-1Not applicable

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
B23P7SM943
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Browning JC, Enloe C, Cartwright M, Hebert A, Paller AS, Hebert D, Kowalewski EK, Maeda-Chubachi T: Efficacy and Safety of Topical Nitric Oxide-Releasing Berdazimer Gel in Patients With Molluscum Contagiosum: A Phase 3 Randomized Clinical Trial. JAMA Dermatol. 2022 Aug 1;158(8):871-878. doi: 10.1001/jamadermatol.2022.2721. [Article]
  2. Ward BM, Riccio DA, Cartwright M, Maeda-Chubachi T: The Antiviral Effect of Berdazimer Sodium on Molluscum Contagiosum Virus Using a Novel In Vitro Methodology. Viruses. 2023 Nov 30;15(12):2360. doi: 10.3390/v15122360. [Article]
  3. Lacarrubba F, Micali G, Trecarichi AC, Quattrocchi E, Monfrecola G, Verzi AE: New Developing Treatments for Molluscum Contagiosum. Dermatol Ther (Heidelb). 2022 Dec;12(12):2669-2678. doi: 10.1007/s13555-022-00826-7. Epub 2022 Oct 14. [Article]
  4. FDA Approved Drug Products: ZELSUVMI (berdazimer) topical gel [Link]
  5. U.S. Food and Drug Administration Approves ZELSUVMI™ as a First-in-Class Medication for the Treatment of Molluscum Contagiosum [Link]
Wikipedia
Berdazimer_sodium

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentMolluscum Contagiosum3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US11285098No2014-02-282034-02-28US flag
US8956658No2006-05-302026-05-30US flag
US10376538No2010-08-202030-08-20US flag
US9526738No2011-09-032031-09-03US flag
US8282967No2006-05-302026-05-30US flag
US10265334No2012-07-032032-07-03US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at January 08, 2024 17:21 / Updated at January 19, 2024 13:35