NAV

Pegulicianine

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

Identification

Summary

Pegulicianine is an optical imaging agent used for fluorescence imaging to detect cancerous tissue within the resection cavity following removal of the primary specimen during lumpectomy surgery.

Generic Name
Pegulicianine
DrugBank Accession Number
DB18731
Background

Pegulicianine is an optical imaging agent indicated for fluorescence imaging in patients with breast cancer. It is used following surgical resection of the primary tumor to detect areas of remaining cancer. Pegulicianine itself is a prodrug comprising three main fragments, one of which contains a fluorescence quencher that keeps the parent molecule optically inactive.2 The in vivo enzymatic cleavage of pegulicianine results in two optically active fragments that emit a fluorescent signal that can be detected using a fluorescence imaging device.2

Pegulicianine (under the brand name Lumisight) was approved for use by the FDA in April 2024.2,3 It received Fast Track and priority review for this indication.3

Type
Small Molecule
Groups
Approved
Synonyms
Not Available
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Pharmacology

Indication

Pegulicianine is indicated for fluorescence imaging in adults with breast cancer as an adjunct for the intraoperative detection of cancerous tissue within the resection cavity following removal of the primary specimen during lumpectomy surgery.2

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Contraindications & Blackbox Warnings
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Pharmacodynamics

After completion of standard of care lumpectomy, prior to pegulicianine-guided tissue removal, 17% of patients had at least one cancer-positive margin - after pegulicianine-guided tissue removal, 15% of these patients changed to having all cancer-negative margins.2 False positive images were reported in 43% of patients and false negative images were reported in 8% of patients.2 The overall sensitivity and specificity in this trial were 49.1% and 86.5%, respectively.3

A non-randomized controlled trial of 234 female patients with breast cancer showed a marked improvement in sensitivity over standard pathology assessment of the main lumpectomy specimen (69.4% vs 38.2%, respectively).1 In this same trial, the false negative rate was 23.7% and the sensitivity was 76.3%.1

As with other contrast agents, pegulicianine carries a risk of hypersensitivity reactions, including anaphylaxis.2 Patients should be assessed for a history of hypersensitivity to contrast media and emergency resuscitation drugs, equipment, and trained personnel should always be available.2

Mechanism of action

Pegulicianine is a prodrug that is optically inactive when intact and produces a fluorescent signal after its peptide chain is cleaved by cathepsins and matrix metalloproteases (MMPs). This enzymatic cleavage results in “fragment 2” and “fragment 3”, which are optically active metabolites that emit fluorescence, as well as “fragment 1” containing the fluorescence quencher that keeps the intact molecule optically inactive.2

The levels of cathepsins and MMPs are higher in and around tumor and tumor-associated cells than normal cells, allowing for pegulicianine to selectively detect tumor and tumor-associated cells following administration.2

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Pegulicianine is a prodrug and is cleaved by matrix metalloproteinases (MMPs) and cathepsins to its active metabolites.2 Pegulicianine undergoes minimal hepatic metabolism in vitro.2

Route of elimination

The excretion pathway of pegulicianine in humans is unknown.2 Patients receiving pegulicianine exhibit chromaturia, suggesting that metabolites may be excreted renally.2

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
No interactions found.

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans

Chemical Identifiers

UNII
T6HE85WN0Q
CAS number
2230217-17-9

References

General References
  1. Hwang ES, Beitsch P, Blumencranz P, Carr D, Chagpar A, Clark L, Dekhne N, Dodge D, Dyess DL, Gold L, Grobmyer S, Hunt K, Karp S, Lesnikoski BA, Wapnir I, Smith BL: Clinical Impact of Intraoperative Margin Assessment in Breast-Conserving Surgery With a Novel Pegulicianine Fluorescence-Guided System: A Nonrandomized Controlled Trial. JAMA Surg. 2022 Jul 1;157(7):573-580. doi: 10.1001/jamasurg.2022.1075. [Article]
  2. FDA Approved Drug Products: Lumisight (pegulicianine) for intravenous injection [Link]
  3. FDA News & Events for Human Drugs: FDA approves imaging drug to assist in detection of cancerous tissue following lumpectomy [Link]
Wikipedia
Pegulicianine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

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

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 April 22, 2024 20:18 / Updated at April 24, 2024 19:06