What studies have evaluated pafolacianine for identifying malignant ovarian cancer lesions?

Comment by InpharmD Researcher

Studies evaluating the use of pafolacianine for identifying malignant ovarian cancer lesions are largely limited to its phase 2 and phase 3 trials (see Tables 1 and 2). In the phase 3 trial, pafolacianine with near-infrared imaging met its primary efficacy endpoint, intraoperatively identifying at least one folate receptor-positive ovarian cancer lesion in a significant number of patients compared to white light only. However, the specificity of pafolacianine appears to be of concern, with a high rate of false positives. Pooled data suggest fluorescence-guided surgery using aminolevulinc acid may be preferred due to improved specificity and positive predictive value.

Background

Pafolacianine was discussed in an article highlighting the Food and Drug Administration (FDA) approval for use as an imaging drug to identify ovarian cancer lesions during surgery via fluorescent imaging. Pafolacianine is administered approximately one hour prior to surgery and binds to folate receptors, which are typically overexpressed in ovarian cancer. A phase 3 trial (summarized in Table 1) paved the way for its approval. [1]

Pafolacianine, under the research name OTL38, has been studied in a variety of investigational settings as an imaging tool to identify certain cancer types or to assist in surgical removals. These include but are not limited to lung cancer, laparoscopic partial nephrectomy, resection of pulmonary lesions, etc. The majority of studies describe pafolacianine as safe and effective in achieving the desired outcome, though these studies are primarily performed without a control group. These early studies also focus on sensitivity/specificity value during identification procedures or successful extraction during surgical procedures. [2], [3], [4], [5], [6]

A recently published meta-analysis evaluating fluorescence-guided surgery to detect microscopic disease in ovarian cancer found that the pooled odds ratio (OR) for a change in surgical plan based on folate receptor studies (e.g., pafolacianine) was 1.29 (95% confidence interval [CI] 1.13 to 1.44). Subgroup analyses found that folate receptor-based agents had a pooled sensitivity of 84% but varied across studies with a high degree of heterogeneity (I2= 91.2%). Similarly, aminolevulinic acid (5-ALA) also resulted in a sensitivity of 84%. The pooled specificity of 26% for folate receptor agents suggests these agents have a low ability to detect true negatives, with a high false-positive rate. In contrast, 5-ALA was found to have a much higher specificity of 96%, with a low degree of heterogeneity across studies. The pooled positive predictive values (PPV) for folate receptor agents was 0.76 compared to 0.96 with 5-ALA. Again, PPV results were highly variable across studies for pafolacianine. The authors determined that 5-ALA was the best agent with respect to sensitivity, specificity, and PPV. Studies found that fluorescence tracers using pafolacianine had an acceptable safety profile with the most common side effects including nausea, vomiting, and abdominal discomfort; no adverse events were reported for 5-ALA. [7]

References:

[1] Voelker R. Lighting the Way for Improved Detection of Ovarian Cancer. JAMA. 2022;327(1):27. doi:10.1001/jama.2021.22960
[2] Gangadharan S, Sarkaria IN, Rice D, et al. Multiinstitutional Phase 2 Clinical Trial of Intraoperative Molecular Imaging of Lung Cancer. Ann Thorac Surg. 2021;112(4):1150-1159. doi:10.1016/j.athoracsur.2020.09.037
[3] Sulek JE, Steward JE, Bahler CD, et al. Folate-targeted intraoperative fluorescence, OTL38, in robotic-assisted laparoscopic partial nephrectomy. Scand J Urol. 2021;55(4):331-336. doi:10.1080/21681805.2021.1933168
[4] Predina JD, Newton A, Corbett C, et al. Localization of Pulmonary Ground-Glass Opacities with Folate Receptor-Targeted Intraoperative Molecular Imaging. J Thorac Oncol. 2018;13(7):1028-1036. doi:10.1016/j.jtho.2018.03.023
[5] Lakomkin N, Van Gompel JJ, Post KD, Cho SS, Lee JYK, Hadjipanayis CG. Fluorescence guided surgery for pituitary adenomas. J Neurooncol. 2021;151(3):403-413. doi:10.1007/s11060-020-03420-z
[6] Randall LM, Wenham RM, Low PS, Dowdy SC, Tanyi JL. A phase II, multicenter, open-label trial of OTL38 injection for the intra-operative imaging of folate receptor-alpha positive ovarian cancer. Gynecol Oncol. 2019;155(1):63-68. doi:10.1016/j.ygyno.2019.07.010
[7] Erdemoglu E, Langstraat CL, Kumar A, et al. Fluorescence-Guided Surgery to Detect Microscopic Disease in Ovarian Cancer: A Systematic Review with Meta-Analysis. Cancers (Basel). 2025;17(3):410. Published 2025 Jan 26. doi:10.3390/cancers17030410

Literature Review

A search of the published medical literature revealed 2 studies investigating the researchable question:

What studies have evaluated pafolacianine for identifying malignant ovarian cancer lesions

Level of evidence

B - One high-quality study or multiple studies with limitations  Read more→



Please see Tables 1-2 for your response.


 

­­A Randomized Phase 3 Study of Pafolacianine Injection (OTL38) for Intraoperative Imaging of Folate Receptor Positive Ovarian Cancer

Design

Phase 3, randomized, multicenter, single-dose, open-label study

N= 109

Objective

To examine the use of pafolacianine injection as a tool for real-time detection of folate receptor-positive ovarian cancer.

Study Groups

Fluorescent and White Light (n= 134)

White light only (n= 6)

Inclusion Criteria

Adult female diagnosed with epithelial ovarian cancer or high clinical suspicion of ovarian cancer, scheduled to undergo cytoreductive surgery or laparoscopy and pre-authorized for laparotomy if cancer was detected

Exclusion Criteria

Previous exposure to pafolacianine, FR-negative ovarian cancer, planned surgical debulking via laparoscopy or robotic surgery, inoperable military disease

Methods

Patients were administered pafolacianine 0.025 mg/kg single 60-minute intravenous (IV) infusion at least one hour prior to intraoperative imaging. Patients were evaluable with normal white light assessment and palpitation to identify all suspicious lesions. After normal light assessment, patients were randomized (20:1) to either receive intraoperative near-infrared (NIR) fluorescence imaging or proceed directly to surgical removal of lesions. 

The ratio of 20:1 was used in agreement with the Food and Drug Agency (FDA) through the Special Protocol Assessment process.

Duration

March 2018 to April 2020

Outcome Measures

Primary: Proportion of patients with at least one evaluable FR-positive ovarian cancer lesion (confirmed by central pathology) detective by the use of pafolacianine with intraoperative NIR imaging, but not detected by normal white light and palpation

The primary efficacy endpoint was the prespecified threshold of 10%

Secondary: Sensitivity of pafolacianine with NIR to detect ovarian cancer, patient false positive rate, complete resection of cancer lesion

Baseline Characteristics

 

Fluorescent and white light (n= 134)

White light only (n= 6)

Age, years

60.4 62.8

Hispanic/Latino

11.2% 33.3%

White

85.1% 83.3%

Childbearing potential

Able to bear children

Post-menopausal/Sterile

 

16.4%

83.6%

 

16.7%

83.3%

 

All study participants (N= 140)

 

Histological epithelial type

Serous adenocarcinoma

Endometroid carcinoma

mucinous adenocarcinoma

Clear cell adenocarcinoma

Mixed Mullerian tumor

Undifferentiated adenocarcinoma

Mixed Clear Cell/Endometrioid adenocarcinoma

Papillary Epithelial Malignant neoplasia

Unreported 

 

82.6%

2.8%

1%

3.7%

1%

6.4%

1%

1%

1%

 

A total of 150 patients were initially enrolled. After exclusion of patients due to lack of FR-positive ovarian cancer lesion or otherwise, 109 patients comprised the full analysis set for efficacy analysis.

Results

Endpoint

Fluorescent and white light (n= 109)

p-Value

Primary efficacy endpoint (95% confidence interval [CI])

33% (0.243% to 0.427) 0.001

Sensitivity of pafolacianine with NIR to detect ovarian cancer (95% CI)

23/58 (39.7%; 0.270 to 0.534)  

Patient false positive rate

24.8% (0.176 to 0.336)  

Complete resection

62.4%  

Adverse Events

Drug-related adverse events: 45/150 (30%) of total patients

Common adverse events: Nausea (18%); vomiting (5.3%); abdominal pain (4.6%)

No serious-related adverse events or death were reported

Study Author Conclusions

This phase 3 study of pafolacianine with NIR imaging met its primary efficacy endpoint, intraoperatively identifying numerous additional cancers not otherwise identified or planned for resection. Pafolacianine with intraoperative NIR imaging may offer an important real-time adjunct to current surgical approaches by optimizing cytoreduction in ovarian cancer surgery.

InpharmD Researcher Critique

Although the number of patients randomized between groups varied greatly, the method was in agreement with the FDA as part of their special protocol. The level of false positives is concerning, potentially leading to unnecessary resection of non-cancerous tissue. Although serious safety risks were not reported, the decision of the surgeon to resect the lesions also plays a significant factor in patient outcomes. 



References:

Tanyi JL, Randall LM, Chambers SK, et al. ­­a randomized phase 3 study of pafolacianine injection (Otl38) for intraoperative imaging of folate receptor positive ovarian cancer. SSRN Journal. Published online 2021. doi:10.2139/ssrn.3955732

 

A phase II, multicenter, open-label trial of OTL38 injection for the intraoperative imaging of folate receptor-alpha positive ovarian cancer

Design

Single-arm, open-label, prospective phase II study

N= 44

Objective

To assess the safety and efficacy (sensitivity and positive predictive value (PPV)) of OTL38 (pafolacianine) for intraoperative imaging during epithelial ovarian cancer surgery

Study Groups

Intention-to-treat (ITT) population (n= 44)

modified ITT (mITT) population (n= 29)

Inclusion Criteria

Women age > 18 years, known or suspected ovarian cancer planned for cytoreductive surgery by laparotomy

Exclusion Criteria

Pregnancy, impaired renal function, impaired liver function, abnormal electrocardiogram at baseline, brain metastases

Methods

A single-dose of open-label pafolacianine was administered intravenously in participating patients at 0.025 mg/kg dose (after testing an escalation dose of 0.05 mg/kg, an interim safety review had decided that 0.025 mg/kg as the only dose is acceptable). Injection was administered in the preoperative are 2-3 hours prior to surgery.

All patients included were analyzed for safety whereas 28 patients were enrolled in the mITT population consisting of those who received the pafolacianine imaging, underwent surgery, and had at least one folate receptor alpha (FRa) + target lesion to determine sensitivity and PPV.

Duration

28 ± 4 days post-surgery

Outcome Measures

Primary: Sensitivity and PPV for FRa positive ovarian cancer by immunohistochemistry (IHC) determined by comparing with the "gold standard" of FRa status (positive or negative).

Secondary: Safety and tolerability

Baseline Characteristics

 

ITT population (n= 44)

 

Age, years

63.8  

Hispanic/Latino

0  

White

79.5%  

Body mass index (BMI), kg/m2

24.94  

Tumor stage

IC

IIC

III NOS

IIIA

IIIB

IIIC

IVA

Unknown

 

2.3%

2.3%

2.3%

0

4.5%

38.6%

22.7%

22.7%

 

Tumor histology

High grade serous

Clear cell

Endometrioid

Adenocarcinoma NOS

Other

 

61.4%

2.3%

4.5%

11.4%

18.2%

 

Results

Endpoint

mITT population (n= 29)

  Estimate (lower one-sided 95% CI) (with patient effect as random) Estimate (lower one-sided 95% CI) (without patient effect as random)

Detecting FRa plus ovarian cancer lesions

Sensitivity

Positive-predictive value

 

97.97 (87.75)

94.93 (86.13)

 

85.93 (81.19)

88.14 (83.59)

Detecting FRa plus ovarian cancer lesions

Sensitivity

Positive-predictive value

 

96.82 (86.09)

92.62 (83.35)

 

83.90 (79.40)

85.34 (80.93)

Adverse Events

Patient-reported treatment-related adverse events (TEAEs) related to drug: 18.2%

Gastrointestinal disorder (11.4%), nausea (9.1%), vomiting (6.8%), abdominal pain (2.3%)

Injury, poisoning, and procedural complications (11.4%)

Respiratory, thoracic, and mediastinal disorders (2.3%)

Eye disorders (2.3%)

Study Author Conclusions

OTL38-NIR was safe and efficacious in this phase II study regardless of folate expression levels and merits phase III evaluation.

InpharmD Researcher Critique

This was an open-label, uncontrolled study. Therefore, the results are exploratory at best to pave the way for phase III studies. 



References:

Randall LM, Wenham RM, Low PS, Dowdy SC, Tanyi JL. A phase II, multicenter, open-label trial of OTL38 injection for the intra-operative imaging of folate receptor-alpha positive ovarian cancer. Gynecol Oncol. 2019;155(1):63-68. doi:10.1016/j.ygyno.2019.07.010