Pemefolacianine
| Clinical data | |
|---|---|
| Synonyms | NY-07 |
| Routes of administration | Intravenous |
| Drug class | Optical imaging agent |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Elimination half-life | 1.59–7.86 h[1] |
| Identifiers | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}} |
Pemefolacianine (research code NY-07) is an investigational near-infrared optical imaging agent for fluorescence-guided surgery that targets folate receptor alpha (FRα).[2]
Pemefolacianine was developed and first described by researchers in the Butch/Wang Research Group in the Department of Biomedical Engineering at Nanjing University, with clinical development led by Nanjing Nuoyuan Medical Devices Co., Ltd.[2][1]
Mechanism of action
Pemefolacianine is an antifolate–dye conjugate derived from pemetrexed that binds FRα.[2] FRα is frequently overexpressed across several epithelial malignancies while showing limited expression in most normal adult tissues.[3][4]
Selectivity for FRα over FRβ
In preclinical studies, pemefolacianine showed higher binding affinity for FRα than for FRβ (reported Kd 61.67 nM for FRα vs 486.9 nM for FRβ), and achieved tumor-to-background ratios around 3.2 at one hour post-administration, with sub-millimeter lesion detection in animal models.[2] These data suggest the potential to reduce false-positive fluorescence arising from FRβ-positive tumor-associated macrophages in inflammatory tissue, although head-to-head clinical comparisons are not available.[2]
Comparison to pafolacianine
Pafolacianine (brand name Cytalux) is a folic-acid–based FR-targeted near-infrared agent approved by the U.S. Food and Drug Administration for intraoperative identification of malignant lesions in ovarian cancer (2021) and for identification of lung lesions (2022).[5][6]
In the pivotal ovarian cancer trial (Study 006), sensitivity was 83% and the patient false-positive rate was 24.8%.[7] In lung surgery series, a false-positive rate of about 25.9% has been reported.[8]
In company materials, pemefolacianine is reported to remain stable under refrigerated (2–8 °C) or controlled room temperature storage; peer-reviewed or regulatory confirmation of these stability conditions has not yet been published.[1][11]
Clinical development
Phase I clinical trial (China)
According to company and industry reports, a Phase I clinical trial in healthy volunteers in China has been completed with positive results (no drug-related adverse events reported), with dose-proportional exposure and an elimination half-life of 1.59–7.86 h.[1] Additional industry coverage summarizes similar findings.[12] Public clinical registry entries may be available as trials progress.
Ongoing and planned trials
Nuoyuan Medical has announced initiation of a Phase II clinical trial in China and preparation for clinical studies in the United States; the agent has received investigational new drug (IND) clearances according to company communications.[1]
Medical uses
Pemefolacianine is being developed as an adjunct for intraoperative identification of malignant lesions in FRα-positive cancers (including ovarian and lung), used with compatible near-infrared fluorescence imaging systems.[1][2] In preclinical models, NY-07 enabled visualization of sub-millimeter lesions and discrimination of cancer from inflammation.[2]
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 "Nuoyuan Medical's Pemefolacianine Completes Phase I Trial, Advances Precision Tumor Surgery". Medpath. 2025. Retrieved October 28, 2025.
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 Li Y, Guissi N, Dong J, Singhal S, Dai B, Butch C, Cai H, Wang Y (October 2025). "Fluorescence Discrimination of Cancer from Inflammation by Selective Targeting Folate Receptor α". Chemical & Biomedical Imaging. doi:10.1021/cbmi.5c00087. Unknown parameter
|article-number=ignored (help) - ↑ Zannoni GF, Santoro A, d'Amati A, D'Alessandris N, Scaglione G, Padial Urtueta B, Valente M, Narducci N, Addante F, Spadola S, Bragantini E, Angelico G (May 2025). "Folate Receptor Alpha in Advanced Epithelial Ovarian Cancer: Diagnostic Role and Therapeutic Implications of a Clinically Validated Biomarker". International Journal of Molecular Sciences. 26 (11): 5222. doi:10.3390/ijms26115222. PMC 12154392 Check
|pmc=value (help). PMID 40508029 Check|pmid=value (help). - ↑ Porter RL, Matulonis UA (2023). "Mirvetuximab soravtansine for platinum-resistant epithelial ovarian cancer". Expert Review of Anticancer Therapy. 23 (8): 783–796. doi:10.1080/14737140.2023.2236793. PMID 37458180 Check
|pmid=value (help). - ↑ "FDA approves pafolacianine for identifying malignant ovarian cancer lesions". U.S. Food and Drug Administration. December 1, 2021.
- ↑ "FDA approves imaging drug to help identify lung lesions during surgery". U.S. Food and Drug Administration. January 3, 2022.
- ↑ Tanyi JL, Randall LM, Chambers SK, Butler KA, Winer IS, Langstraat CL, Han ES, Vahrmeijer AL, Chon HS, Morgan MA, Powell MA, Tseng JH, Lopez AS, Wenham RM (January 2023). "A Phase III Study of Pafolacianine Injection (OTL38) for Intraoperative Imaging of Folate Receptor-Positive Ovarian Cancer (Study 006)". Journal of Clinical Oncology. 41 (2): 276–284. doi:10.1200/JCO.22.00291. PMID 36070540 Check
|pmid=value (help). - ↑ Sarkaria IS, Martin LW, Rice DC, Blackmon SH, Slade HB, Singhal S (December 2023). "Pafolacianine for intraoperative molecular imaging of cancer in the lung: The ELUCIDATE trial". The Journal of Thoracic and Cardiovascular Surgery. 166 (6): e468–e478. doi:10.1016/j.jtcvs.2023.02.025. PMC 12507096 Check
|pmc=value (help). PMID 37019717 Check|pmid=value (help). - ↑ "Cytalux (pafolacianine) Prescribing Information" (PDF). accessdata.fda.gov. 2022.
- ↑ "Important Prescribing Information: Preparation, Storage, and Handling" (PDF). cytaluxhcp.com. July 29, 2025.
- ↑ "Medicilon supports Nuoyuan's pemefolacianine program". Medicilon. January 7, 2025.
- ↑ "Class I New Drug Pemefolacianine Completes Phase I Clinical Trial". Frost & Sullivan. July 28, 2025.
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