Piflufolastat F 18 API Manufacturers

General Description:

Piflufolastat F 18, identified by CAS number 1207181-29-0, is a notable compound with significant therapeutic applications. Prostate cancer is the most common non-cutaneous malignancy affecting men in North America - despite this, an ongoing challenge in prostate cancer therapy is the difficulty in imaging the extent and location of tumor metastases and recurrences. The images generated by positron emission tomography (PET) are less detailed than those obtained via MRI or CT, but are more sensitive and can reveal cancerous tissue in any area of the body provided the tissue is expressing the appropriate target protein. Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein expressed in many tissues that plays a role in folate uptake and neurotransmitter release - it is expressed in the prostate at levels roughly 1000-fold greater than elsewhere in the body, and even higher in prostate cancer tissue. As such, it has become a desirable target for PET imaging of prostate cancer tissues. Piflufolastat F18, also called -DCFPyL, is a urea-based radiopharmaceutical that binds to PSMA and allows for the visualization of cancerous prostate tissue. It was first approved by the FDA in May 2021 under the brand name Pylarify and aims to allow for earlier and more accurate detection of suspected prostate cancer metastases or recurrences.

Indications:

This drug is primarily indicated for: Piflufolastat F18 is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer who have suspected metastases and are candidates for initial definitive therapy and for men with a suspected recurrence of prostate cancer based on elevated prostate-specific antigen (PSA) levels. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Half-life:

The half-life of Piflufolastat F 18 is an important consideration for its dosing schedule: The half-life of distribution of piflufolastat F18 is 0.17 ± 0.044 hours and its elimination half-life is 3.47 ± 0.49 hours. This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Piflufolastat F 18 from the body primarily occurs through: Piflufolastat F18 is eliminated via urinary excretion - within 8 hours of intravenous administration, approximately 50% of an administered dose is excreted in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Piflufolastat F 18 is distributed throughout the body with a volume of distribution of: Within 60 minutes of intravenous administration, piflufolastat F18 distributes to the kidneys, liver, and lungs. This metric indicates how extensively the drug permeates into body tissues.

Mechanism of Action:

Piflufolastat F 18 functions by: Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein that plays a role in dietary folate uptake and the release of neurotransmitters within the brain. While PSMA is expressed in many tissues, its expression levels in the prostate are roughly 1000-fold greater than elsewhere in the body and even higher in prostate cancer tissue. Piflufolastat F18 binds to PSMA and therefore, in combination with PET imaging, allows for the visualization of PSMA-positive lesions associated with prostate cancer. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Piflufolastat F 18 is categorized under the following therapeutic classes: Amides, Amino Acids, Amino Acids, Basic, Amino Acids, Diamino, Amino Acids, Essential, Amino Acids, Peptides, and Proteins, Diagnostic Radiopharmaceuticals, Fluorine Radioisotopes, Positron Emitting Activity, Radioactive Diagnostic Agent. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.