Pegulicianine
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
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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- 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
- 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]
- FDA Approved Drug Products: Lumisight (pegulicianine) for intravenous injection [Link]
- FDA News & Events for Human Drugs: FDA approves imaging drug to assist in detection of cancerous tissue following lumpectomy [Link]
- External Links
- Wikipedia
- Pegulicianine
Clinical Trials
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