Absorption, Distribution and Excretion
Pilifludazal F18 is primarily excreted in the urine—approximately 50% of the administered dose is excreted in the urine within 8 hours after intravenous administration. Within 60 minutes of intravenous administration, pilifludazal F18 is distributed to the kidneys (16.5% of the administered activity), liver (9.3%), and lungs (2.9%). Biological Half-Life The distribution half-life of pilifludazal F18 is 0.17 ± 0.044 hours, and the elimination half-life is 3.47 ± 0.49 hours.

Prostate cancer is the most common non-cutaneous malignancy among men in North America. Despite this, a major challenge in prostate cancer treatment remains the difficulty in imaging the extent and location of tumor metastases and recurrences. While positron emission tomography (PET) images are not as sharp as those from magnetic resonance imaging (MRI) or computed tomography (CT), they are far more sensitive, allowing PET to visualize cancerous tissue anywhere in the body as long as the tissue expresses the corresponding target protein. Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein expressed in various tissues and involved in folic acid uptake and neurotransmitter release. PSMA expression levels in the prostate are approximately 1000 times higher than in other parts of the body, and even higher in prostate cancer tissue. Therefore, PSMA has become an ideal target for PET imaging to detect prostate cancer tissue. Piflufolastat F18, also known as [F-18]-DCFPyL, is a urea-based radiopharmaceutical that binds to PSMA, enabling the imaging of prostate cancer tissue. It was first approved by the FDA in May 2021 under the brand name Pylarify, and is designed to detect suspected prostate cancer metastases or recurrences earlier and more accurately. On July 28, 2023, the EMA also approved Piflufolastat F18, marketed as PYLCLARI, for the initial staging or recurrence localization of prostate cancer. Piflufolastat f-18 is a radiodiagnostic agent. Its mechanism of action is as a positron-emitting active substance. Fluorine-18-labeled Piflufolastat is a urea-based radiotracer composed of the prostate-specific membrane antigen (PSMA) target DCFPyL and labeled with the positron-emitting isotope fluorine-18, which can be used for positron emission tomography (PET) imaging. After injection of fluorine-18-labeled Piflufolastat, it binds to PSMA expressed on the surface of tumor cells. The fluorine-18 component facilitates PET imaging of PSMA-expressing tumor cells. PSMA is a cell surface antigen abundant on the surface of prostate cancer cells and in the neovascularization of most solid tumors.

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Drug Indications
Piflufolastat F18 is indicated for FDA-approved patients with prostate cancer to be examined using positron emission tomography (PET) scans for prostate-specific membrane antigen (PSMA)-positive lesions. These patients are suspected of having metastases and meet the criteria for initial radical therapy. Additionally, Piflufolastat F18 is also indicated for FDA-approved patients suspected of having recurrent prostate cancer based on elevated PSA levels. This drug is also EMA-approved for initial staging in high-risk prostate cancer patients before initial radical therapy, and for locating recurrent lesions in patients suspected of having recurrent prostate cancer based on elevated serum PSA levels after radical therapy.
This drug is for diagnostic use only.
Pylclari is indicated for the detection of prostate-specific membrane antigen (PSMA)-positive lesions in adult prostate cancer (PCa) patients using positron emission tomography (PET) in the following clinical settings: initial staging in high-risk PCa patients before initial radical treatment; and localization of recurrent lesions in patients suspected of PCa recurrence with elevated serum PSA levels after initial radical treatment. Pylclari is suitable for use in conjunction with PET.

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Mechanism of Action
Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein that plays a role in the absorption of dietary folic acid and the release of neurotransmitters in the brain. Although PSMA is expressed in many tissues, its expression level in the prostate is approximately 1000 times higher than in other parts of the body, and its expression level is even higher in prostate cancer tissue. Piflufolastat F18 binds to PSMA; therefore, when used in conjunction with PET imaging, it can visualize PSMA-positive lesions associated with prostate cancer.

C18H2318FN4O8

441.4

441.153

1207181-29-0

1207181-29-0 (F18);1423758-00-2 (F-19);

52950901

Typically exists as solid at room temperature

1.361

6

10

13

31

663

2

C1=CC(=NC=C1C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O)[18F]

OLWVRJUNLXQDSP-MVBOSPHXSA-N

InChI=1S/C18H23FN4O8/c19-13-6-4-10(9-21-13)15(26)20-8-2-1-3-11(16(27)28)22-18(31)23-12(17(29)30)5-7-14(24)25/h4,6,9,11-12H,1-3,5,7-8H2,(H,20,26)(H,24,25)(H,27,28)(H,29,30)(H2,22,23,31)/t11-,12-/m0/s1/i19-1

(2S)-2-[[(1S)-1-carboxy-5-[(6-(18F)fluoranylpyridine-3-carbonyl)amino]pentyl]carbamoylamino]pentanedioic acid

18F-DCFPyL; Dcfpyl F-18; Pylarify; piflufolastat F-18

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)