Flotufolastat F-18 API Manufacturers
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Looking for Flotufolastat F-18 API 2639294-14-5?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Flotufolastat F-18. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Flotufolastat F-18
- Synonyms:
- 18F-rhPSMA-7.3 , Flotufolastat (18F) , Flotufolastat F 18 , rhPSMA-7.3C
- Cas Number:
- 2639294-14-5
- DrugBank number:
- DB17851
- Unique Ingredient Identifier:
- 811W19E3OL
General Description:
Flotufolastat F-18, identified by CAS number 2639294-14-5, is a notable compound with significant therapeutic applications. Flotufolastat F-18 (18F-rhPSMA-7.3) is an 18F-labeled ligand that targets the prostate-specific membrane antigen (PSMA). In patients with recurrent prostate cancer that require localized treatment, the use of 18F-labeled ligands for positron emission tomography (PET) offers accurate diagnostic imaging. Unlike 68Ga-labeled PSMA-targeting ligands, 18F-labeled compounds targeting this protein have a longer half-life and can be produced in larger batches. Flotufolastat F-18 is a diastereoisomer of 18F-rhPSMA-7, and compared to the other diastereoisomers of this compound, flotufolastat F-18 has a faster clearance from blood pool, liver, and kidney, and a high level of accumulation in tumors. In May 2023, the FDA approved the use of flotufolastat F-18 for PET of PSMA-positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. This is the first FDA-approved, PSMA-targeted imaging agent developed with proprietary radiohybrid (rh) technology. Additional studies have shown that in patients with primary prostate cancer, the use of flotufolastat F-18 shows led to low interreader variation and a good distinction between primary-tumor activity and bladder background activity.
Indications:
This drug is primarily indicated for: Flotufolastat F-18 is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Metabolism:
Flotufolastat F-18 undergoes metabolic processing primarily in: After it is injected, flotufolastat F-18 is not metabolized for up to 50 minutes. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.
Absorption:
The absorption characteristics of Flotufolastat F-18 are crucial for its therapeutic efficacy: After flotufolastat F-18 is administered intravenously, it distributes to the liver, heart blood pool and kidneys, with 15.8%, 7.4% and 3.2% of the administered activity, respectively. Flotufolastat F-18 is cleared from the blood. The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Flotufolastat F-18 is an important consideration for its dosing schedule: Not available. This determines the duration of action and helps in formulating effective dosing regimens.
Protein Binding:
Flotufolastat F-18 exhibits a strong affinity for binding with plasma proteins: Not available. This property plays a key role in the drug's pharmacokinetics and distribution within the body.
Route of Elimination:
The elimination of Flotufolastat F-18 from the body primarily occurs through: Flotufolastat F-18 is eliminated by urinary excretion. In the first 2 hours after flotufolastat F-18 is injected, approximately 7% of the administered activity is excreted in the urine. Approximately 15% is excreted 4.5 hours after flotufolastat F-18 is injected. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Flotufolastat F-18 is distributed throughout the body with a volume of distribution of: Not available. This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Flotufolastat F-18 is a critical factor in determining its safe and effective dosage: Not available. It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Flotufolastat F-18 exerts its therapeutic effects through: The relationship between the plasma concentrations of flotufolastat F-18 in patients and image interpretation has not been fully elucidated. The use of flotufolastat F-18 contributes to the overall long-term cumulative radiation exposure in patients, and long-term radiation exposure is associated with a higher risk of cancer. In addition, image interpretation errors can occur with flotufolastat F-18. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Flotufolastat F-18 functions by: Flotufolastat F-18 binds to the prostate-specific membrane antigen (PSMA) (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells. The fluorine-18 group in flotufolastat F-18 is a ß+ emitting radionuclide that can be detected using positron emission tomography (PET). Since prostate cancer cells overexpress PSMA and flotufolastat F-18 is internalized by cells, this radioactive agent can be used for the diagnostic imaging of prostate cancer patients. Compared to morphologic imaging, such as computerized tomography (CT) scans and magnetic resonance imaging (MRI), the use of PET targeting PSMA is a superior technique for the localization of recurrent disease or primary node (N) staging. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Categories:
Flotufolastat F-18 is categorized under the following therapeutic classes: 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.
Flotufolastat F-18 is a type of Cardiac stimulants
Cardiac stimulants are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of cardiac disorders. These medications are designed to enhance the functioning of the heart by stimulating its electrical impulses and increasing its contractility.
Cardiac stimulants work by targeting specific receptors in the heart, promoting the release of neurotransmitters such as norepinephrine and epinephrine. These neurotransmitters bind to adrenergic receptors, leading to an increased heart rate and force of contraction, which helps improve cardiac output.
One commonly used cardiac stimulant API is Dobutamine. Dobutamine acts primarily on beta-1 adrenergic receptors in the heart, increasing the strength of cardiac contractions while minimizing the impact on heart rate. This makes it a valuable medication in cases of acute heart failure or during cardiac stress testing.
Another well-known cardiac stimulant API is Isoproterenol. Isoproterenol acts on both beta-1 and beta-2 adrenergic receptors, resulting in increased heart rate, contractility, and relaxation of the smooth muscles in the bronchi. It is commonly used in the treatment of bradycardia, heart block, and certain types of asthma.
Cardiac stimulant APIs play a vital role in cardiovascular medicine and are often used in emergency situations or as temporary measures to improve heart function. However, it is important to note that their use requires careful monitoring and should be administered under medical supervision due to potential side effects such as increased blood pressure, arrhythmias, and myocardial ischemia.
In conclusion, cardiac stimulant APIs are a critical category of pharmaceutical ingredients used to enhance heart function. Medications like Dobutamine and Isoproterenol act on specific receptors in the heart, leading to increased contractility and heart rate. While these medications provide important therapeutic benefits, their use should be closely monitored by medical professionals due to potential side effects.
