Delving into the Latest Updates on Alfatide[18F] with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms

(18)F-AlF-NOTA-PRGD2, 18F-AlF-NOTAE[PEG4-c(RGDfk)]2, 18F-Alfatide II

+ [5]

Target

αvβ3

Mechanism

αvβ3 modulators(Integrin alpha-V/beta-3 modulators), PET imaging(Positron-emission tomography enhancers)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

Non-Small Cell Lung CancerSmall Cell Lung Cancer

Inactive Indication-

Originator Organization

Jiangsu Shimeikang Pharmaceutical Co. Ltd.

Active Organization

Taizhou Qirui Pharmaceutical Technology Co., Ltd.

Yantai Lannacheng Biotechnology Co., Ltd.

Jiangsu Shimeikang Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC93H146AlFN24O31

InChIKeyWUGBBIVPEQZTOB-LKQFREDSSA-K

CAS Registry-

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Gene Sequence

Sequence Code 1507071

This is a multicenter, open, non-inferiority Phase III clinical study to evaluate the efficacy of 18F-Alfatide Injection PET/CT compared with 18F-FDG PET/CT in the diagnosis of lymph node metastasis in non-small cell lung cancer.
This trial will include 428 patients with non-small cell lung cancer confirmed by imaging, histopathology and/or cytology or highly suspected by investigators, suspected lymph node metastasis and proposed radical surgery and lymph node dissection. Eligible subjects will receive 18F-Alfatide Injection PET/CT and 18F-FDG PET/CT scans within 1 week. Subjects will undergo relevant security checks before and after each scan. The subjects underwent radical surgery and lymph node dissection within 2 weeks of completing both scans, and the obtained lymph nodes were pathologically examined as the gold standard to compare the diagnostic efficacy of 18F-Alfatide versus 18F-FDG for lymph node metastasis.

Start Date01 Aug 2024

Sponsor / Collaborator

Yantai Lannacheng Biotechnology Co., Ltd.

ChiCTR2100047602 / RecruitingEarly Phase 1IIT

11C- MET and 18F-Alfatide II dual-tracer PET/MR molecular imaging in differential diagnosis of radiation-induced brain injury and glioma recurrence

Start Date17 Jun 2021

Sponsor / Collaborator-

CTR20192146 / CompletedPhase 1

一项观察氟[18F]阿法肽注射液在中国健康成年受试者体内的安全性、药代动力学特征以及生物分布的临床研究

[Translation] A clinical study to observe the safety, pharmacokinetic characteristics and biodistribution of 18F-fluoro[18F]alfatide injection in healthy Chinese adult subjects

主要目的：观察氟[18F]阿法肽注射液在中国健康成年受试者中单次注射的安全性及耐受性。次要目的：评价氟[18F]阿法肽注射液在中国健康成年受试者中单次注射的药代动力学（PK）特征；评估氟[18F]阿法肽注射液在中国健康成年受试者体内放射性分布特征及辐射暴露量。

[Translation]

Primary objective: To observe the safety and tolerability of a single injection of fluoro[18F] alpha peptide injection in healthy Chinese adult subjects. Secondary objective: To evaluate the pharmacokinetic (PK) characteristics of a single injection of fluoro[18F] alpha peptide injection in healthy Chinese adult subjects; To assess the radioactivity distribution characteristics and radiation exposure of fluoro[18F] alpha peptide injection in healthy Chinese adult subjects.

Start Date07 Nov 2019

Sponsor / Collaborator

Taizhou Qirui Pharmaceutical Technology Co., Ltd.

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100 Clinical Results associated with Alfatide[18F]

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100 Translational Medicine associated with Alfatide[18F]

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100 Patents (Medical) associated with Alfatide[18F]

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15

Literatures (Medical) associated with Alfatide[18F]

01 Sep 2024·European Journal of Nuclear Medicine and Molecular Imaging

[18F]AlF-NOTA-PCP2: a novel PET/CT tracer for enhanced PD-L1 heterogeneity imaging and comparative analysis with [18F]AlF-NOTA-WL12 in glioblastoma xenografts

Article

Author: Hu, Man ; Liu, Zhiguo ; Liu, Wei ; Chen, Yunhao ; Zhang, Yang ; Wang, Shijie ; Wang, Yong

PURPOSEThe unsatisfactory efficacy of PD-L1 antibodies in glioblastoma (GBM) is largely due to the temporal and spatial heterogeneity of PD-L1 expression. Molecular imaging can enhance understanding of the tumor immune microenvironment and guide immunotherapy. However, highly sensitive imaging agents capable of effectively visualizing PD-L1 heterogeneity are limited. This study introduces a novel PET tracer, offering improved imaging of PD-L1 heterogeneity in GBM xenografts, with a comparative analysis to [¹⁸F]AlF-NOTA-WL12.METHODS[¹⁸F]AlF-NOTA-PCP2 was synthesized with high purity and its affinity for PD-L1 was characterized using surface plasmon resonance (SPR) and cell binding assays. Its specificity for PD-L1 was evaluated both in vitro using various cell lines and in vivo with GBM xenograft models in NOD/SCID mice. PET/CT imaging was conducted to evaluate the tracer's biodistribution, pharmacokinetics, and ability to quantify tumoral spatial heterogeneity of PD-L1 expression. A focused comparative analysis between [¹⁸F]AlF-NOTA-PCP2 and [¹⁸F]AlF-NOTA-WL12 was conducted, examining binding affinity, biodistribution, pharmacokinetics, and imaging effectiveness in GBM xenografts. Additionally, human radiation dosimetry estimates compared the safety profiles of both tracers.RESULTS[¹⁸F]AlF-NOTA-PCP2 demonstrated high radiochemical purity (> 95%) and a strong affinity for PD-L1, comparable to [¹⁸F]AlF-NOTA-WL12. In vitro and in vivo studies confirmed its specificity for PD-L1, with increased uptake in PD-L1 expressing cells and tumors. Toxicological profiles indicated no significant abnormalities in serum biochemical indicators or major organ tissues. MicroPET/CT imaging showed [¹⁸F]AlF-NOTA-PCP2's effectiveness in visualizing PD-L1 expression levels and spatial heterogeneity in GBM xenografts. Comparative studies revealed [¹⁸F]AlF-NOTA-PCP2's improved pharmacokinetic properties, including higher tumor-to-blood ratios and lower nonspecific liver uptake, as well as reduced radiation exposure compared to [¹⁸F]AlF-NOTA-WL12.CONCLUSION[¹⁸F]AlF-NOTA-PCP2 distinguishes itself as an exceptionally sensitive PET/CT tracer, adept at non-invasively and accurately quantifying PD-L1 expression and its spatial heterogeneity in tumors, especially in GBM. Its favorable pharmacokinetic properties, safety profile, and high affinity for PD-L1 highlight its potential for enhancing the precision of cancer immunotherapy and guiding individualized treatment strategies. While promising, its clinical translation, especially in brain imaging, necessitates further validation in clinical trials.

07 Aug 2023·Molecular pharmaceutics

Automated Synthesis and Preclinical Evaluation of Optimized Integrin α6-Targeted Positron Emission Tomography Imaging of Pancreatic Cancer.

Article

Author: Ye, Jiacong ; Feng, Guokai ; Yu, Chunjing ; He, Huihui ; Li, Qingbo ; Lou, Kequan ; Fu, Haitian ; Chen, Liping

Integrin α6 has been considered a promising biomarker, is overexpressed in many tumors, and plays a vital role in tumor formation, recurrence, and metastasis. In this study, we identified a novel high-affinity integrin α6-targeted peptide named RD₂ (Arg-Trp-Tyr-Asp-PEG4)₂-Lys-Lys and developed a ¹⁸F-radiolabeled peptide tracer ([¹⁸F]-AlF-NOTA-RD₂) and evaluated its potential application in positron emission tomography (PET) imaging of pancreatic cancer. [¹⁸F]-AlF-NOTA-RD₂ was produced using GMP (Good Manufacturing Practice of Medical Products)-compliant automatic radiosynthesis on a single GE FASTLab2 cassette-type synthesis module. The stability of [¹⁸F]-AlF-NOTA-RD₂ was analyzed in phosphate-buffered saline (PBS) and fetal bovine serum (FBS). The cell uptake assay of the tracer was assessed using PANC-1 cells. In addition, small-animal PET imaging and biodistribution studies of [¹⁸F]-AlF-NOTA-RD₂ were performed in pancreatic cancer subcutaneous tumor-bearing mice. The PET tracer [¹⁸F]-AlF-NOTA-RD₂ was obtained with a radiochemical yield of 23.7 ± 4.7%, radiochemical purity of >99%, and molar activity of 165.7 ± 59.1 GBq/μmol. [¹⁸F]-AlF-NOTA-RD₂ exhibited good in vitro stability in PBS and FBS. LogP octanol water value for the tracer was -2.28 ± 0.05 (n = 3). The binding affinity of RD₂ to the integrin α6 protein (K_d = 0.13 ± 3.65 μM, n = 3) was significantly higher than that of the RWY (CRWYDENAC) (K_d = 6.97 ± 1.44 μM, n = 3). Small-animal PET imaging and biodistribution also revealed that [¹⁸F]-AlF-NOTA-RD₂ displayed rapid and good tumor uptake and lower liver background uptake in PANC-1 tumor-bearing mice. [¹⁸F]-AlF-NOTA-RD₂ showed significant radioactivity accumulation in tumors and was successfully blocked by NOTA-RD₂. Compared with [¹⁸F]-FDG, [¹⁸F]-AlF-NOTA-RD₂ PET imaging and biodistribution studies in PANC-1 xenograft tumor-bearing mice confirmed a good tumor-to-muscle ratio (8.69 ± 2.03 vs 1.41 ± 0.23, respectively) at 0.5 h and (2.99 ± 3.02 vs 1.43 ± 0.17, respectively) at 1 h post injection. Autoradiography of human pancreatic cancer tumor tissues further confirmed high accumulation of [¹⁸F]-AlF-NOTA-RD₂. In summary, we developed an optimized integrin α6-targeted imaging tracer and obtained high radioactivity products with a cassette-type synthesis module; moreover, the tracer exhibited good binding affinity with integrin α6 and good target specificity for PANC-1 cells in xenograft pancreatic tumor-bearing mice, demonstrating its promising application as a noninvasive PET radiotracer of integrin α6 expression in pancreatic cancer.

01 Apr 2023·Biomedical Chromatography

A novel LC–MS/MS approach to [¹⁹F]‐alfatide and alfatide for application in preclinical pharmacokinetics

Article

Author: Shao, Qing ; Ren, Kaiyue ; Qiao, Hongqun ; Yuan, Yanjuan

AbstractFor the further study of [19F]‐alfatide, the development of highly sensitive analytical methods for its determination is an urgent issue. In this paper, a method for simultaneously determining [19F]‐alfatide and alfatide using liquid chromatography/tandem mass spectrometry was created and validated. The plasma samples were pretreated using the protein precipitation method. Poroshell 120 EC‐C18 (4.6 × 50 mm, 2.7 μm, Agilent) was used for the separation of the analytes to be measured. The mobile phase, consisting of acetonitrile and water (0.1% acetic acid, 50:50, v/v), was delivered at a flow rate of 0.60 ml/min for sample analysis. Positive electrospray ionization was performed using multiple‐reaction monitoring with transitions of m/z 715.2 → 636.6 for [19F]‐alfatide, the ion pairs 700.3 → 851.5 for alfatide and the ion pairs 237.1 → 194.2 for carbamazepine (internal standard). According to the results, the method had high specificity, precision and accuracy as well as an extended linear range. The matrix effect and extraction recovery were also acceptable. The method was successfully applied to the pharmacokinetic study of [19F]‐alfatide in rats.

100 Deals associated with Alfatide[18F]

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Non-Small Cell Lung Cancer	Phase 3	CN	Yantai Lannacheng Biotechnology Co., Ltd.	01 Aug 2024
Small Cell Lung Cancer	Phase 3	CN	Jiangsu Shimeikang Pharmaceutical Co. Ltd.	10 Dec 2021
Small Cell Lung Cancer	Phase 3	CN	Taizhou Qirui Pharmaceutical Technology Co., Ltd.	10 Dec 2021

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2016	Not Applicable	Locally Advanced Lung Non-Small Cell Carcinoma	12	18F-alfatide RGD PET/CT (Responder group)	dkpyhmtlxd(exbvrfsylq) = vrrlgaqyya xgkzzzblpb (sgchrvrmvh )	Positive	20 May 2016
				18F-alfatide RGD PET/CT (Non-responder group)	dkpyhmtlxd(exbvrfsylq) = jgwffznbdr xgkzzzblpb (sgchrvrmvh )
SNMMI2015	Not Applicable	-	-	18F-alfatide II (Male phantom)	ffrgtppthw(atxkgzfehw) = rbjioetawd nlilnvvwma (vylrighcjq ) View more	-	15 May 2015
				18F-alfatide II (Female phantom)	ffrgtppthw(atxkgzfehw) = gubdglzjza nlilnvvwma (vylrighcjq ) View more