Delving into the Latest Updates on 99mTc-3PRGD2 with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms

Target

αvβ3

Action

modulators

Mechanism

αvβ3 modulators(Integrin alpha-V/beta-3 modulators)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

Lung Cancer

Inactive Indication

Breast CancerEsophageal CarcinomaLymphatic Metastasis+ [1]

Originator Organization

Peking University

Active Organization

Foshan Rui Diao Pharmaceutical Co Ltd

Jiangsu Huayi Technology Co. Ltd.

Inactive Organization

RDO Pharm.

Sun Yat-Sen UniversityInstitute of Biophysics of Chinese Academy of Sciences

+ [2]

License Organization

Qingdao Baheal Medical, Inc.Beijing Giluntai Pharmaceutical Co., Ltd.

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationPriority Review (China)

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Structure/Sequence

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Sequence Code 95090

Sequence Code 565009095

The esophageal squamous cell carcinoma (ESCC) has high prevalence and mortality in China, which become a severe challenge for public health. The molecular imaging technology has been developed for visualization and precise diagnosis of the tumors. Integrin αvβ3 is a specific marker for tumor. Noninvasive visualization and quantitative analysis of integrin αvβ3 expression provide new opportunities for tumor diagnosis, identification and efficacy monitoring. The peptide containing Arg-Gly-Asp (RGD) can specifically bind to integrin αvβ3 receptor with high selectivity and affinity to achieve the detecting tumor .The SPECT/CT with 99mTc-3PRGD2 has a high specificity in the diagnosis of mediastinal lymphnode metastasis and a greater value in the decision-making of lymphnode dissection.
This study is a single-center self-controlled study, It is planned to enroll 30 patients with esophageal cancer , preliminarily confirmed by endoscopic biopsy, . After intravenous injection of 0.3 mCi/kg of 99mTC-3PRGD2, patients underwent single-photon emission computed tomography/computed tomography (SPECT/CT) examination.Subsequently, the patients received chest/abdomen enhanced CT and 18F fluorodeoxyglucose (18F-FDG) positron emission computed tomography /CT (PET/CT) for diagnosis. According to the determination of the researcher, patients who were suitable for surgery received surgery to obtain surgical pathology; For patients who were not suitable for surgery, ultrasound-guided lyphnode biop was performed .In this study, pathological specimens were obtained from gastroscopy, surgical pathology, or ultrasound-guided lymph node biopsy. The diagnostic accuracy, sensitivity , specificity and safety of SPECT/CT with 99mTc-3PRGD2 were evaluated and compared with PET-CT and enhanced CT.

Start Date01 Aug 2020

Sponsor / Collaborator

the First Affiliated Hospital of Sun Yat-Sen University

[+1]

NCT04233476

/ CompletedPhase 3

Safety and Efficacy of 99mTc-hydrazinonicotinamide-PEG4-E[PEG4-c(RGDfk)]2 (99mTc-3PRGD2) SPECT/CT for Integrin αVβ3 Imaging of Lung Cancer and Mapping Lymph Node Metastases: A Prospective Multicenter, Self-controlled, Phase 3 Trial

This is a prospective, multicenter, self-controlled phase 3 clinical trial designed to evaluate the safety and efficacy of an integrin αVβ3-targeted imaging, 99mTc-3PRGD2 SPECT/CT, for diagnosis of lung cancer and mapping the lymph node metastases. The pathological results will be considered as the gold standard and the conventional metabolic imaging by 18F-FDG PET/CT will be used for a head-to-head comparison. The primary objective of this study is to evaluate the efficacy of 99mTc-3PRGD2 SPECT/CT in mapping of lymph node metastasis according to the nodal mapping system released by the International Association for the Study of Lung Cancer in 2009 (IASLC-2009). The secondary objectives include evaluation of 99mTc-3PRGD2 SPECT/CT in detection of lung cancer and the safety of 99mTc-3PRGD2 injection in human beings.

Start Date12 Oct 2019

Sponsor / Collaborator

RDO Pharm.

[+1]

NCT03974685

/ CompletedPhase 1

Phase I Open Label Trial of Pharmacokinetics and Safety of 99mTc Niacinamide Polyethylene Glycol Bicyclic RGD Peptide (99mTc-3PRGD2) Injection in Healthy Volunteers

The study drug 99mTc-3PRGD2 of this study is a new radioactive diagnostic preparation for clinical use as a nuclear medicine molecular probe for tumor SPECT/CT imaging.
After 99mTc-3PRGD2 is injected into the body, it is specifically taken up by integrin receptor-positive tumor tissue, and tumor tissue is developed by SPECT/CT, which can be used for molecular imaging diagnosis and individualized treatment of common tumors.
The primary objectives of this study is to examine the pharmacokinetics the safety of 99mTc-3PRGD2 injection in healthy volunteers, as well as the biodistribution in the human body and to estimate the dose of internal radiation absorbed. This study provides the basis for the design of phase II clinical research programs.

Start Date12 Dec 2018

Sponsor / Collaborator

RDO Pharm.

[+2]

100 Clinical Results associated with 99mTc-3PRGD2

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100 Translational Medicine associated with 99mTc-3PRGD2

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100 Patents (Medical) associated with 99mTc-3PRGD2

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26

Literatures (Medical) associated with 99mTc-3PRGD2

01 Jan 2023·Frontiers in oncology

Direct attenuation correction for ^99mTc-3PRGD₂ chest SPECT lung cancer images using deep learning.

Article

Author: Jin, Xiaona ; Jing, Hongli ; Ba, Jiantao ; Xing, Haiqun ; Li, Fang ; Tian, Jian ; Wang, Tong

IntroductionThe attenuation correction technique of single photon emission computed tomography (SPECT) images is essential for early diagnosis, therapeutic evaluation, and pharmacokinetic studies of lung cancer. ^99mTc-3PRGD₂ is a novel radiotracer for the early diagnosis and evaluation of treatment effects of lung cancer. This study preliminary discusses the deep learning method to directly correct the attenuation of ^99mTc-3PRGD₂ chest SPECT images.MethodsRetrospective analysis was performed on 53 patients with pathological diagnosis of lung cancer who received ^99mTc-3PRGD₂ chest SPECT/CT. All patients' SPECT/CT images were reconstructed with CT attenuation correction (CT-AC) and without attenuation correction (NAC). The CT-AC image was used as the reference standard (Ground Truth) to train the attenuation correction (DL-AC) SPECT image model using deep learning. A total of 48 of 53 cases were divided randomly into the training set, the remaining 5 were divided into the testing set. Using 3D Unet neural network, the mean square error loss function (MSELoss) of 0.0001 was selected. A testing set is used to evaluate the model quality, using the SPECT image quality evaluation and quantitative analysis of lung lesions tumor-to-background (T/B).ResultsSPECT imaging quality metrics between DL-AC and CT-AC including mean absolute error (MAE), mean-square error (MSE), peak signal-to-noise ratio (PSNR), structural similarity (SSIM), normalized root mean square error (NRMSE), and normalized Mutual Information (NMI) of the testing set are 2.62 ± 0.45, 58.5 ± 14.85, 45.67 ± 2.80, 0.82 ± 0.02, 0.07 ± 0.04, and 1.58 ± 0.06, respectively. These results indicate PSNR > 42, SSIM > 0.8, and NRMSE < 0.11. Lung lesions T/B (maximum) of CT-AC and DL-AC groups are 4.36 ± 3.52 and 4.33 ± 3.09, respectively (p = 0.81). There are no significant differences between two attenuation correction methods.ConclusionOur preliminary research results indicate that using the DL-AC method to directly correct ^99mTc-3PRGD₂ chest SPECT images is highly accurate and feasible for SPECT without configuration with CT or treatment effect evaluation using multiple SPECT/CT scans.

01 Nov 2022·Thoracic Cancer

Evaluation of ^99mTc‐3PRGD₂ SPECT imaging on angiogenesis in animal models of lung cancer

Article

Author: Wang, Yufei ; Teng, Chuanhui ; Guo, Zhanlin ; Yang, Zheng ; Wu, Yongkun

AbstractBackgroundThe main purpose of the study was to evaluate the activity and selectivity of 99mTc‐3PRGD2 SPECT/CT and 18F‐FDG PET‐CT in order to detect the neovascularization of A549 cell subcutaneously transplanted tumors, and clarify the relationship among tumor vasculature, hypoxia and cell proliferation in the tumor microenvironment.MethodsWe established a subcutaneous tumor model, and used 99mTc‐3PRGD2 SPECT/CT and 18F‐FDG PET‐CT when the average tumor size reached 0.3–0.5 cm3. The mice were anesthetized and sacrificed and the tumors were completely removed for frozen section analysis. We subsequently evaluated the status of neovascularization, hypoxia, as well as cell proliferation via immunofluorescence staining (IF) by detecting CD31, pimonidazole and EdU, respectively.ResultsThere was a significant positive correlation (r = 0.88, p < 0.05) between the microvascular density (41.20 ± 18.60) and tumor to nontumor ratio (T/M), which was based on the value of 99mTc‐3PRGD2 (4.20 ± 1.33); meanwhile, no significance (r = −0.16, p > 0.05) was found between the T/M and hypoxic area (116.71 ± 9.36). Neovascular proliferation was particularly vigorous in the parenchymal region of the tumor, while the cells around the cavity were generally hypoxic. 99mTC‐3PRGD2 SPECT/CT was more specific than 18F‐FDG PET‐CT in detecting malignant tumors.ConclusionBoth 99mTC‐3PRGD2 and 18F‐FDG PET‐CT can be used for the detection of malignant tumors, but the specificity and accuracy of 99mTC‐3PRGD2 are better. The subcutaneous tumors showed a heterogeneous microenvironment as a result of neovascularization, a high proliferation rate of cancer cells as well as subsequent hypoxia, while most of the hypoxic areas appeared around the cavities of the vessels.

01 Aug 2021·Nuklearmedizin - NuclearMedicineQ4 · MEDICINE

Assessing Doxorubicin-Induced Cardiomyopathy by 99mTc-3PRGD2 Scintigraphy Targeting Integrin αvβ3 in a Rat Model

Q4 · MEDICINE

Article

Author: Sui, Shi ; Hou, Yang

AbstractThe present study evaluated interstitial alterations in doxorubicin-induced cardiomyopathy using a radiolabeled RGD peptide 99mTc-3PRGD2 specific for integrin αvβ3 that targets myofibroblasts.Cardiomyopathy was induced in 20 Sprague-Dawley rats by intraperitoneal doxorubicin injections (2.5 mg/kg/week) for up to six weeks. 99mTc-3PRGD2 scintigraphy was performed in control rats (n = 6) at baseline and three, six, and nine weeks after first doxorubicin administration (n = 6, 6, and 5 for each time point). For another three rats of 6-week modeling, cold c(RGDyK) was co-injected with 99mTc-3PRGD2 to evaluate specific radiotracer binding. Semi-quantitative parameters were acquired to compare radiotracer uptake among all groups. The biodistribution of 99mTc-3PRGD2 was evaluated by a γ-counter after scintigraphy. Haematoxylin and eosin, and Masson’s staining were used to evaluate myocardial injury and fibrosis, while western blotting and immunofluorescence co-localization were used to analyze integrin αvβ3 expression in the myocardium.The 99mTc-3PRGD2 half-life in the cardiac region (Heartt 1/2) of the 9-week model and heart radioactivity percentage (%Heart20 min, %Heart40 min and %Heart60 min) of the 6 and 9-week models were significantly increased compared to the control. Heart-to-background ratio (HBR20 min, HBR40 min and HBR60 min) increase began in the third week, continued until the sixth week, and was reversed in the ninth week, which paralleled the changing trend of cardiac integrin αvβ3 expression. The myocardial biodistribution of 99mTc-3PRGD2 was significantly correlated with integrin β3 expression.The 99mTc-3PRGD2 scintigraphy allows for non-invasive visualization of interstitial alterations during doxorubicin-induced cardiomyopathy.

1

News (Medical) associated with 99mTc-3PRGD2

11 Feb 2025

·www.echemi.com

Breakthrough in Nuclear Medicine as Novartis' Pluvicto Sales Soar to $1.39 Billion in 2024

In a remarkable development within the pharmaceutical sector, Novartis has announced that its nuclear medicine product, Pluvicto (177Lu-PSMA-617), achieved $1.39 billion in sales for the year 2024, marking a 42% increase compared to the previous year. This milestone establishes Pluvicto as the first blockbuster drug in the nuclear medicine field. Since its approval in the United States in March 2022, Pluvicto has demonstrated impressive growth. In its first year, the drug generated $271 million, which skyrocketed to $980 million in 2023, representing a staggering 261% year-over-year increase. Cumulatively, Pluvicto has contributed $2.643 billion to Novartis’ revenue, with four additional indications currently under investigation, including a Phase III trial for metastatic hormone-sensitive prostate cancer expected to conclude in 2025. Nuclear medicine is being hailed as a crucial aspect of precision diagnostics and treatment, with experts likening its impact to that of a "missile" in the hands of healthcare providers. According to Dr. Wang Tie, Chief Physician of Nuclear Medicine at Beijing Chaoyang Hospital, nuclear medicine offers unique advantages over traditional cancer therapies, including non-invasive precision diagnostics and integrated therapeutic capabilities. This allows for personalized treatment based on imaging and targeted delivery of radioactive agents to tumors. The demand for both diagnostic and therapeutic nuclear medicines has surged in recent years, revealing a significant unmet need in cancer treatment. Major pharmaceutical companies are keenly aware of the potential of this market. Besides Novartis, industry giants such as Bayer, Eli Lilly, AstraZeneca, Bristol Myers Squibb, Merck, and Johnson & Johnson are actively investing in nuclear medicine through acquisitions and partnerships. Notably, Bristol Myers Squibb made headlines in December 2023 with its $4.1 billion acquisition of RayzeBio, gaining access to a differentiated platform for alpha-emitting radiopharmaceuticals. In the domestic Chinese market, competition in nuclear medicine is intensifying. Nearly 20 companies, including Hengrui Medicine, Yuan Da Medicine, and Xiantong Medicine, are rapidly advancing their nuclear medicine portfolios. To date, 24 radioactive drugs have been approved for use, addressing various conditions including prostate cancer, coronary heart disease, neuroendocrine tumors, and Alzheimer's disease. Innovative domestic products are also emerging, with over 100 nuclear medicine candidates in clinical stages. The most advanced is 99mTc-3PRGD2, developed by Radiopharmaceuticals, which is the first domestically produced innovative nuclear medicine for tumor imaging. This drug has completed Phase III trials and is in the process of seeking market approval. Additionally, Hengrui's 177Lu-labelled octreotate injection is also in Phase III trials, targeting neuroendocrine tumors. With the nuclear medicine sector rapidly evolving, the future looks promising as companies strive to meet the growing demand for effective cancer diagnostics and treatments.

Phase 3AcquisitionDrug ApprovalRadiation Therapy

100 Deals associated with 99mTc-3PRGD2

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Lung Cancer	NDA/BLA	China	Foshan Rui Diao Pharmaceutical Co Ltd	29 Aug 2024
Lung Cancer	NDA/BLA	China	Jiangsu Huayi Technology Co. Ltd.	29 Aug 2024
Esophageal Carcinoma	Phase 1	China	Sun Yat-Sen University	18 Jul 2020
Lymphatic Metastasis	Phase 1	China	Peking University	30 Jul 2019
Lymphatic Metastasis	Phase 1	China	Chinese Academy of Sciences	30 Jul 2019
Lymphatic Metastasis	Phase 1	China	Foshan Rui Diao Pharmaceutical Co Ltd	30 Jul 2019
Breast Cancer	Phase 1	China	RDO Pharm.	12 Dec 2018
PSMA-Positive Tumor	Phase 1	China	RDO Pharm.	12 Dec 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CSCO2022	Not Applicable	Refractory Differentiated Thyroid Gland Carcinoma	30	整合素受体 99Tcm-3PRGD2 (99Tcm-3PRGD2 SPECT/CT)	(utrifhkfkx) = ageebxxnvn jkcxjrzwjx (upqmvuqsmj, 74.8 - 92.1) View more	-	21 Sep 2022
EANM2019	Not Applicable	Radiation Injuries	50	99mTc-3PRGD2 (15Gy Pulmonary Radiation-Induced Injury Group (15GyPI))	yetnhbxmup(ipyhdcdcqs) = lkmihdling pvaewzzksu (auzgxfsgde )	-	18 Sep 2019
SNMMI2017	Not Applicable	-	-	99mTc-3PRGD299m Tc-3PRGD2 (99mTc-3PRGD2 SPECT/CT)	(cudkwhqezn) = ebnfxqyjnv kmhiqaagse (jyxoxlxafi ) View more	-	24 May 2017
SNMMI2016	Not Applicable	-	-	99mTc-3P-RGD2d rgd peptides (99mTc-3P-RGD2)	qrzpvlkaqp(yqhqlyrcvl) = jdhqfhklin xdrglmzwnt (qtwbeefzey, 1.1)	-	24 May 2016
				tc99m labelled rgd peptides (Healthy volunteers)	qrzpvlkaqp(yqhqlyrcvl) = xjbbcbdtmz xdrglmzwnt (qtwbeefzey, 1.0)
SNMMI2016	Not Applicable	Lung Cancer	-	99mTc-3PRGD2 (Lung cancer patients)	(gyyzlmbden) = ydzlhzaxin unalanaxkl (ghflepkxxd ) View more	-	24 May 2016
				99mTc-3PRGD2 (Benign disease patients)	(gyyzlmbden) = pnogehdnyr unalanaxkl (ghflepkxxd ) View more
SNMMI2016	Not Applicable	Fibrosis, Liver	-	99mTc-3PRGD2 (Control rats)	hdtkgkfftu(ydscojddig) = vvwhgzmyrp bbwxnxfzwt (wgwobwukji, 0.25)	-	24 May 2016
				99mTc-3PRGD2 (Thioacetamide (TAA) injected rats)	hdtkgkfftu(ydscojddig) = fuebcxfuji bbwxnxfzwt (wgwobwukji, 0.59)
Pubmed \| Eur J Nucl Med Mol Imaging	Not Applicable	Breast Cancer Neoadjuvant HER-2-positive	-	99mTc-3PRGD2	(uttviiwheh) = zhtoqqbkov tlqkxhzmwg (adsiardksx ) View more	-	01 Aug 2015
				99mTc-3PRGD2	(uttviiwheh) = hxsflxnynw tlqkxhzmwg (adsiardksx ) View more
SNMMI2014	Not Applicable	Drug-Related Side Effects and Adverse Reactions	-	99mTc-3PRGD2 (Treatment group)	ojncleptav(jczvbnjclk) = The T/N ratios at 3 h decreased in the treatment group while they increased in the control group nojgysniem (jlxwomunmw )	-	05 Nov 2014
				99mTc-3PRGD2 (Control group)
NCT01737112 (Pubmed \| PLoS One)	Early Phase 1	Lung Cancer	44	99mTc-3PRGD2	rosbifvtfl(zkjhfxzvbv) = mjoyhskufk tfnouuwtpt (mmxupasldo ) View more	-	01 Jan 2014
				99mTc-MDP	rosbifvtfl(zkjhfxzvbv) = jstdkfwogz tfnouuwtpt (mmxupasldo ) View more

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