18F-AV1451 material

¹⁸F-AV1451 Materials

1.  Drug Name (Generic Name, Chemical Name, English Name, Piny¶in, and rationale for custom names if any)

Generic Name: Flortaucipir F18

Chemical Name: 7-(6- fluoropyridine -3- yl )-5H- pyridino [4,3-b] indole

English Name: Flortaucipir F18

Fluorine - 18 AV1451

Pinyin: Fú tài pǔ F18

2. Drug Chemical Structure, Molecular Weight, Molecular Formula

Chemical Structure:

Molecular Weight:  303.3

Molecular Formula: C _{16 ​} H ₁₅ ^{​ 18} FN _{3 ​} O _{2 ​}

3. Rationale (Literature on the research and application of this product at §home and abroad)

Domestic: Some research teams and hospitals are actively carry₽ing out relevant research and synthesis work. For example, the nuclear medπicine department of the First Affiliated Hospital of Harbin Medical Uγniversity, led by physicist Han Wei, successfully synthesized 18F-AV1451, which has promoted thΩe application of neuro-nuclear medicine molecular imaging in Heilongjiang Province. Directo&r Zhao Yinlong of the Nuclear Medicine Department of the Se≥cond Hospital of Jilin University applied 18F-AV1451 imaging to the diagnosis of Alzheimer's diseas∑e, providing strong support for the accurate diagnosis of Alzheimer's diseasδe patients.

International: It is the first tau tracer approved by the U.S. Food" and Drug Administration. The development process involved extensive experimental research, inclu​ding animal model and human trials, to verify its specific bindiπng ability to tau protein, safety, and efficacy.

Applications

Domestic: Mainly used in the diagnosis of Alzheimer's disease. For ex→ample, Professor Fu Peng's team from the First Affiliated Hospital of÷ Harbin Medical University, in collaboration with the new molecular probe 18F-AV1451₽, successfully diagnosed Alzheimer's disease. Through PET/MR imaging, it was found t©hat patients had increased 18F-AV1451 uptake in the bilateral pari¥eto-occipital regions, left frontal lobe, bilateral hippocam'pus, and bilateral temporal lobes, and tau protein imaging was positive, pr∑oviding important evidence for the diagnosis of the€ disease.

International: Widely used in Alzheimer's disease-related researc•h and clinical diagnosis. It detects tau protein tangles in the brain through P₹ET imaging, helping doctors with early diagnosis, disease assessment, and §research on disease progression. Studies have shown that the cl¥assification accuracy of 18F-AV1451 in clinically distinguishing Alzheimer's diseaseΩ and mild cognitive impairment (MCI) is approximately 85.7%, but there• are also problems such as relatively low affinity for non-Alzheim♣er's tau lesions and off-target effects.

4 Research methods, experimental conditions, and data on whole-body i&maging or simulated clinical functional determination t≤ests of target organs in experimental animals, and imaging or functi§onal determination results at various time points of observation

I. Whole-body and delayed imaging of experimental animals

1. Materials and Methods

1.1. Experimental Animals

The experimental animals were mice, weighing approximately 20$g, provided by the Experimental Animal Center of Hangzhou Medical College. The scann♦ing location was the PET center of the Second Affiliated Hospital of Zhejiang University.< Images were acquired 45 minutes after drug injection to obtain a map of drug dis tribution in the body. The brain signal was weak, able to penetrate the blood-brain barrier, becaus↑e in healthy mice, there is almost no tau protein deposition in the brain, making it difficult fo'r the drug to remain.

5. Product Instructions

[Drug Name]

Generic Name:

Fluorine-[18F]-β-Tau Protein Injection

18F-AV1451

Chemical Name: 7-(6-fluoropyridine-3-yl)-5H-pyridino[4,3-b]indole

English Name: Flortaucipir F18

Fluorine - 18 AV1451

Pinyin: Fú tài pǔ F18

[Ingredients]

The main ingredient and its chemical name are: β-Tau prote∞in

Its structural formula is

[Properties]

This product is a yellow liquid.

[Indications]

18F-AV1451 is used for the diagnosis and differential ☆diagnosis of Alzheimer's disease (AD)

[18F-AV1451 PET/CT Brain Imaging Procedure]

Patient Appointment: The clinician must communicate and make an appointment with this center at l↔east one day in advance. The clinician or the appointment doctor of this center shoul"d inform the patient that they can eat normally on the day of the exa∞mination. If possible, they should fast for 2 hours. A♥D drugs and related drugs acting on the brain should be discontinued within 24 hours before the AV&45 scan. Patients need to arrive at the center one hour before t™he scheduled appointment time.

Medical History Collection: Brief medical history, clinical diagnosis​, informed consent form signed by participants.

Pre-examination Preparation: Instruct the patient to  drink water and use the restroom. After injection of the imaging agent and b↓efore the examination, they should not drink water or use the restroom again.

Before Injection: The drug group confirms the measurement time and dosage of each inj∑ection and reports it to the nursing group. The nursing group confirms the injection time a nd returns the residue to the drug group. The drug grouσp records the residual dosage and time.

Injection of 18F-AV1451: Only one patient can be injected at a time. The injection dose is" 10 mCi (±10%). The nursing group must strictly record the injection time.

Patient Rest: Before the examination, the subject should >be instructed to remain quiet, refrain from speaking, and maintain consciousn ess. Family members or caregivers may accompany the subject during this ‍time, but they should not talk or use electronic devices.

PET/CT Acquisition: Scanning should be performed exactly 50 minutes after injection of the ima£ging agent. Static scanning time is 20 minutes at 50 minutes post-injection. Dynamic acquisiti₽on time is 0-70 minutes. CT and PET acquisition parameters and reconstruction met™hods should be consistent with brain 18F-FDG imaging. The scanning team must strictly control ₽the injection time and scanning time, and strictly record the sc±anning time.

Image Interpretation and Analysis: Interpret image≥s promptly.

Report: Issue a report promptly.

Follow-up Arrangements: 18F-AV1451 and 18F-FDG brain imagin©g should be spaced at least 10 half-lives (or 20 hours) apart©.

This product is for use only in medical institutions with a "Radioactive Pharmaceutical Us‍e License".

[Adverse Reactions]

None have been found.

[Contraindications]

None have been found.

[Precautions]

If discoloration or cloudiness occurs, discontinue use'.

This product is for use only in medical institutions with a "Radioactive Pharmaceutical U✔se License".

[Use in Pregnant and Lactating Women]

Contraindicated in pregnant and lactating women.

[Pediatric Use]

Reduce dosage appropriately according to body weight.

[Specifications]

0.37~7.40GBq.

[Storage and Packaging]

This product is sealed in a 30ml vial and placed in a lead container.

[Expiration Date]

6 hours from the time of calibration.

[Manufacturer]

Name: Hangzhou Jirei Technology Co., Ltd.

Address: No. 319, Shenjia Road, Gongshu District, Hangzhou, Fengqi Valley Yu&nzhang Industrial Park

Postal Code: 234122

Telephone Number: 0571-87701916