Pegulicianine

Brand Names: Lumisight

Drug Class: General Prescription

Overview

11 DESCRIPTION LUMISIGHT (pegulicianine for injection) is an optical imaging agent for intravenous use. The chemical name of pegulicianine acetate is N-[6-(1-{2-[3,6-bis(2,3-dihydro-1H-indol-1-yl)xanthylium-9-yl]benzene-1-sulfonyl}piperidine-4-carboxamido)hexanoyl]glycylglycyl-L-arginyl-N6-(6-{2-[(1E,3E,5Z)-5-(1-ethyl-3,3-dimethyl-5-sulfonato-1,3-dihydro-2H-indol-2-ylidene)penta-1,3-dien-1-yl]-3,3...

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 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). The levels of these enzymes are higher in and around tumor and tumor-associated cells than normal cells. 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. “Fragment 2” and “fragment 3” absorb light in the visible light region with a peak absorption at 650 nm and fluoresce with a peak emission at 675 nm. 12.

Indications

  • 1 INDICATIONS AND USAGE LUMISIGHT 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. LUMISIGHT is an optical imaging agent 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. ( 1 )

Common Doses

  • 1 mg
  • 4 mL
  • 3.9 mL
  • 10 mg

Dosage

2 DOSAGE AND ADMINISTRATION Recommended dose of LUMISIGHT is 1 mg/kg by intravenous injection over 3 minutes administered 2 hours to 6 hours prior to imaging. ( 2.1 ) See Full Prescribing Information for instructions on preparation, administration, and imaging. ( 2.2 , 2.3 , 2.4 ) 2.1 Recommended Dose The recommended dose of LUMISIGHT is 1 mg/kg actual body weight by intravenous injection over 3 minutes administered 2 hours to 6 hours prior to imaging. 2.

Black Box Warning

WARNING: ANAPHYLAXIS AND OTHER SERIOUS HYPERSENSITIVITY REACTIONS Serious hypersensitivity reactions, including anaphylaxis, can occur during or following administration of LUMISIGHT. Anaphylaxis occurred in 4/726 (0.6%) of patients in clinical studies. Signs and symptoms associated with other hypersensitivity reactions included pruritus, urticaria, hypotension, lip swelling, erythema, anxiety, chest pain, cyanosis, dizziness, dyspnea, headache, hypoesthesia, hyperventilation, maculopapular rash, nausea, paresthesia, visual changes, and vomiting.

Contraindications

  • 4 CONTRAINDICATIONS LUMISIGHT is contraindicated in patients with a history of hypersensitivity reaction to pegulicianine. Reactions have included anaphylaxis [see Warning and Precautions (5.1) ] . History of hypersensitivity reaction to pegulicianine. ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS The following clinically important adverse reactions are described elsewhere in the labeling: Anaphylaxis and Other Serious Hypersensitivity Reactions [see Warnings and Precautions ( 5.1 )] Most common adverse reactions (≥1%) were hypersensitivity and chromaturia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Lumicell at 1-833-458-6387 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be...

Interactions

  • 7 DRUG INTERACTIONS Blue dyes used for SLN mapping procedures generate a fluorescent signal that interferes with the signal from LUMISIGHT when injected into the breast prior to imaging with LUMISIGHT. The potential of other dyes to interfere with LUMISIGHT imaging has not been evaluated. Avoid administration of dyes used for SLN mapping procedure before imaging the lumpectomy cavity in patients receiving LUMISIGHT.