Pafolacianine Explained

Tradename:

Cytalux

Dailymedid:

Pafolacianine

Pregnancy Category:

Not recommended

Routes Of Administration:

Intravenous

Atc Prefix:

V04

Atc Suffix:

CX10

Legal Us:

Rx-only

Legal Us Comment:

^[1]

Cas Number:

1628423-76-6

Pubchem:

135565623

Drugbank:

DB15413

Chemspiderid:

64880249

Unii:

F7BD3Z4X8L

Kegg:

D12249

Chembl:

4297412

Synonyms:

OTL38, OTL-0038

Iupac Name:

2--3,3-dimethyl-1-(4-sulfobutyl)-3H-indolium-5-sulfonate| C=61 | H=67 | N=9 | O=17 | S=4| SMILES = CC1(C2=C(C=CC(=C2)S(=O)(=O)[O-])[N+](=C1C=CC3=C(C(=CC=C4C(C5=C(N4CCCCS(=O)(=O)O)C=CC(=C5)S(=O)(=O)O)(C)C)CCC3)OC6=CC=C(C=C6)CC(C(=O)O)NC(=O)C7=CC=C(C=C7)NCC8=CN=C9C(=N8)C(=O)NC(=N9)N)CCCCS(=O)(=O)O)C| StdInChI = 1S/C61H67N9O17S4/c1-60(2)46-33-44(90(81,82)83)22-24-49(46)69(28-5-7-30-88(75,76)77)51(60)26-16-38-10-9-11-39(17-27-52-61(3,4)47-34-45(91(84,85)86)23-25-50(47)70(52)29-6-8-31-89(78,79)80)54(38)87-43-20-12-37(13-21-43)32-48(58(73)74)66-56(71)40-14-18-41(19-15-40)63-35-42-36-64-55-53(65-42)57(72)68-59(62)67-55/h12-27,33-34,36,48H,5-11,28-32,35H2,1-4H3,(H9-,62,63,64,66,67,68,71,72,73,74,75,76,77,78,79,80,81,82,83,84,85,86)/t48-/m0/s1| StdInChIKey = PDXNSXLPXJFETD-DYVQZXGMSA-N| density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }}

Pafolacianine, sold under the brand name Cytalux, is an optical imaging agent used in fluorescence-guided surgery.^{[2] [3] [4] [5] [6]} Pafolacianine is a fluorescent medication that binds to folate receptor (FR)-expressing cells.

The most common side effects of pafolacianine include infusion-related reactions, including nausea, vomiting, abdominal pain, flushing, dyspepsia, chest discomfort, itching and hypersensitivity.

It was approved for medical use in the United States in November 2021.^[7] The U.S. Food and Drug Administration considers it to be a first-in-class medication.^[8]

Medical uses

Pafolacianine is indicated as an adjunct for intraoperative identification of malignant lesions in people with ovarian cancer. It is also indicated to assist identifying lung cancer lesions in adults with known or suspected lung cancer.

History

Scientists from Purdue University designed and developed OTL38 and licensed it to On Target Laboratories in 2013.^{[9] [10]} The safety and effectiveness of pafolacianine was evaluated in a randomized, multi-center, open-label study of women diagnosed with ovarian cancer or with high clinical suspicion of ovarian cancer who were scheduled to undergo surgery. Of the 134 women (ages 33 to 81 years) who received a dose of pafolacianine and were evaluated under both normal and fluorescent light during surgery, 26.9% had at least one cancerous lesion detected that was not observed by standard visual or tactile inspection.

The safety and effectiveness of pafolacianine was evaluated in a randomized, multicenter, open-label study (NCT04241315) of participants with known or suspected lung cancer who were scheduled to undergo surgery. Of the 110 participants who received a dose of pafolacianine and were evaluated under both normal and fluorescent light during surgery, 24% had at least one cancerous lesion detected that was not observed by standard visual or tactile inspection.

The U.S. Food and Drug Administration (FDA) granted the application for pafolacianine orphan drug, priority review, and fast track designations.^[11] The FDA granted the approval of Cytalux to On Target Laboratories, LLC.

External links

• Web site: Pafolacianine . U.S. National Library of Medicine . Drug Information Portal .

Notes and References

1. Web site: Cytalux- pafolacianine injection injection . DailyMed . 18 December 2021.
2. FDA Approves New Imaging Drug to Help Identify Ovarian Cancer Lesions . U.S. Food and Drug Administration (FDA) . 29 November 2021 . 30 November 2021.
3. FDA approves imaging drug to help identify lung cancer lesions . U.S. Food and Drug Administration (FDA) . 16 December 2022 . 16 December 2022.
4. Web site: FDA approves pafolacianine for identifying malignant ovarian cancer lesions . U.S. Food and Drug Administration (FDA) . 1 December 2021 . 2 December 2021.
5. Predina JD, Newton AD, Connolly C, Dunbar A, Baldassari M, Deshpande C, Cantu E, Stadanlick J, Kularatne SA, Low PS, Singhal S . 6 . Identification of a Folate Receptor-Targeted Near-Infrared Molecular Contrast Agent to Localize Pulmonary Adenocarcinomas . Molecular Therapy . 26 . 2 . 390–403 . February 2018 . 29241970 . 5835020 . 10.1016/j.ymthe.2017.10.016 .
6. Lauwerends LJ, Abbasi H, Bakker Schut TC, Van Driel PB, Hardillo JA, Santos IP, Barroso EM, Koljenović S, Vahrmeijer AL, Baatenburg de Jong RJ, Puppels GJ, Keereweer S . 6 . The complementary value of intraoperative fluorescence imaging and Raman spectroscopy for cancer surgery: combining the incompatibles . European Journal of Nuclear Medicine and Molecular Imaging . 49 . 7 . 2364–2376 . June 2022 . 35102436 . 9165240 . 10.1007/s00259-022-05705-z .
7. Web site: On Target Laboratories Announces FDA Approval of Cytalux (pafolacianine) injection for Identification of Ovarian Cancer During Surgery . On Target Laboratories . PR Newswire . 29 November 2021 . 30 November 2021.
8. Advancing Health Through Innovation: New Drug Therapy Approvals 2021 . U.S. Food and Drug Administration (FDA) . 13 May 2022 . PDF . 22 January 2023 . 6 December 2022 . https://web.archive.org/web/20221206210020/https://www.fda.gov/media/155227/download . live .
9. Web site: Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors .
10. Web site: Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors .
11. Web site: Pafolacianine Orphan Drug Designations and Approvals . U.S. Food and Drug Administration (FDA) . 23 December 2014 . 30 November 2021.