Pafolacianine
Clinical data
Trade namesCytalux
Other namesOTL38, OTL-0038
License data
Pregnancy
category
  • Not recommended
Routes of
administration		Intravenous
ATC code
Legal status
Legal status
Identifiers
  • 2-{(E)-2-[(3E)-2-(4-{2-[(4-{[(2-Amino-4-oxo-3,4-dihydro-6-pteridinyl)methyl]aminobenzoyl)amino]-2-carboxyethyl}}phenoxy)-3-{(2E)-2-[3,3-dimethyl-5-sulfo-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]ethylidene}-1-cyclohexen-1-yl]vinyl}-3,3-dimethyl-1-(4-sulfobutyl)-3H-indolium-5-sulfonate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC61H67N9O17S4
Molar mass1326.49 g·mol−1
3D model (JSmol)
  • 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
  • InChI=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
  • Key:PDXNSXLPXJFETD-DYVQZXGMSA-N

Pafolacianine, sold under the brand name Cytalux, is an optical imaging agent used in fluorescence-guided surgery.[1][2][3][4][5][6] Pafolacianine is a fluorescent medication that binds to folate receptor (FR)-expressing cells.[1]

The most common side effects of pafolacianine include infusion-related reactions, including nausea, vomiting, abdominal pain, flushing, dyspepsia, chest discomfort, itching and hypersensitivity.[2][4]

It was approved for medical use in the United States in November 2021.[2][7][6] 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.[1][2] It is also indicated to assist identifying lung cancer lesions in adults with known or suspected lung cancer.[3]

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.[2][4] 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.[2][4]

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.[3] 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.[3]

The U.S. Food and Drug Administration (FDA) granted the application for pafolacianine orphan drug, priority review, and fast track designations.[2][4][11][8] The FDA granted the approval of Cytalux to On Target Laboratories, LLC.[2][3]

Figures

Intraoperative imaging of a squamous cell carcinoma of the lung with OTL38, subsequently renamed pafolacianine. From Predina et al., 2018.[12]

References

  1. 1 2 3 4 "Cytalux- pafolacianine injection injection". DailyMed. Retrieved 18 December 2021.
  2. 1 2 3 4 5 6 7 8 "FDA Approves New Imaging Drug to Help Identify Ovarian Cancer Lesions". U.S. Food and Drug Administration (FDA) (Press release). 29 November 2021. Retrieved 30 November 2021. Public Domain This article incorporates text from this source, which is in the public domain.
  3. 1 2 3 4 5 "FDA approves imaging drug to help identify lung cancer lesions". U.S. Food and Drug Administration (FDA) (Press release). 16 December 2022. Retrieved 16 December 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  4. 1 2 3 4 5 "FDA approves pafolacianine for identifying malignant ovarian cancer lesions". U.S. Food and Drug Administration (FDA). 1 December 2021. Retrieved 2 December 2021. Public Domain This article incorporates text from this source, which is in the public domain.
  5. ↑ Predina JD, Newton AD, Connolly C, Dunbar A, Baldassari M, Deshpande C, et al. (February 2018). "Identification of a Folate Receptor-Targeted Near-Infrared Molecular Contrast Agent to Localize Pulmonary Adenocarcinomas". Molecular Therapy. 26 (2): 390–403. doi:10.1016/j.ymthe.2017.10.016. PMC 5835020. PMID 29241970.
  6. 1 2 Lauwerends LJ, Abbasi H, Bakker Schut TC, Van Driel PB, Hardillo JA, Santos IP, et al. (June 2022). "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. doi:10.1007/s00259-022-05705-z. PMC 9165240. PMID 35102436.
  7. ↑ "On Target Laboratories Announces FDA Approval of Cytalux (pafolacianine) injection for Identification of Ovarian Cancer During Surgery". On Target Laboratories. 29 November 2021. Retrieved 30 November 2021 – via PR Newswire.
  8. 1 2 Advancing Health Through Innovation: New Drug Therapy Approvals 2021 (PDF). U.S. Food and Drug Administration (FDA) (Report). 13 May 2022. Archived from the original on 6 December 2022. Retrieved 22 January 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  9. ↑ "Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors".
  10. ↑ "Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors".
  11. ↑ "Pafolacianine Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 23 December 2014. Retrieved 30 November 2021.
  12. ↑ Predina JD, Newton AD, Xia L, Corbett C, Connolly C, Shin M, et al. (March 2018). "An open label trial of folate receptor-targeted intraoperative molecular imaging to localize pulmonary squamous cell carcinomas". Oncotarget. 9 (17): 13517–13529. doi:10.18632/oncotarget.24399. PMC 5862595. PMID 29568374.
  • "Pafolacianine". Drug Information Portal. U.S. National Library of Medicine.
  • Clinical trial number NCT03180307 for "OTL38 for Intra-operative Imaging of Folate Receptor Positive Ovarian Cancer" at ClinicalTrials.gov
  • Clinical trial number NCT04241315 for "ELUCIDATE: Enabling Lung Cancer Identification Using Folate Receptor Targeting (Elucidate)" at ClinicalTrials.gov
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