更新于：2024-07-01
[18F]DCFPyL
更新于：2024-07-01
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2021-05-26), |
最高研发阶段(中国)- |
特殊审评优先审评 (美国) |
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结构
分子式C18H23FN4O8 |
InChIKeyOLWVRJUNLXQDSP-MVBOSPHXSA-N |
CAS号1207181-29-0 |
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51
项与 [18F]DCFPyL 相关的临床试验A Phase 1/2 Open-label Study of Pembrolizumab Combined With PNT-2002 Radioligand Therapy in Patients With Metastatic Renal Cell Carcinoma
Monitoring Prostate Cancer Tumor Response to Radiation Therapy Using Advanced Functional Magnetic Resonance Imaging (MRI) and Pylarify (18F-DCFPyL) PSMA Positron Emission Tomography (PET)
Modulation of PSMA Expression in Castration Sensitive and Castration Resistant Prostate Cancer in Response to Hormonal Therapy
100 项与 [18F]DCFPyL 相关的临床结果
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100 项与 [18F]DCFPyL 相关的转化医学
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100 项与 [18F]DCFPyL 相关的专利（医药）
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44
项与 [18F]DCFPyL 相关的文献（医药）2024-05-01Anti-cancer agents in medicinal chemistry
An Expedition on Synthetic Methodology of FDA-approved Anticancer Drugs
(2018-2021)
Review
作者: Gupta, Ghanshyam Das ; Jain, Ankit ; Vishakha, S ; Navneesh, N ; Verma, Sant Kumar ; Patel, Preeti ; Kurmi, Balak Das
Abstract::
New drugs being established in the market every year produce specified structures for selective biological
targeting. With medicinal insights into molecular recognition, these begot molecules open new rooms for
designing potential new drug molecules. In this review, we report the compilation and analysis of a total of 56
drugs including 33 organic small molecules (Mobocertinib, Infigratinib, Sotorasib, Trilaciclib, Umbralisib, Tepotinib,
Relugolix, Pralsetinib, Decitabine, Ripretinib, Selpercatinib, Capmatinib, Pemigatinib, Tucatinib, Selumetinib,
Tazemetostat, Avapritinib, Zanubrutinib, Entrectinib, Pexidartinib, Darolutamide, Selinexor, Alpelisib,
Erdafitinib, Gilteritinib, Larotrectinib, Glasdegib, Lorlatinib, Talazoparib, Dacomitinib, Duvelisib, Ivosidenib,
Apalutamide), 6 metal complexes (Edotreotide Gallium Ga-68, fluoroestradiol F-18, Cu 64 dotatate, Gallium 68
PSMA-11, Piflufolastat F-18, 177Lu (lutetium)), 16 macromolecules as monoclonal antibody conjugates (Brentuximabvedotin,
Amivantamab-vmjw, Loncastuximabtesirine, Dostarlimab, Margetuximab, Naxitamab, Belantamabmafodotin,
Tafasitamab, Inebilizumab, SacituzumabGovitecan, Isatuximab, Trastuzumab, Enfortumabvedotin,
Polatuzumab, Cemiplimab, Mogamulizumab) and 1 peptide enzyme (Erwiniachrysanthemi-derived
asparaginase) approved by the U.S. FDA between 2018 to 2021. These drugs act as anticancer agents against
various cancer types, especially non-small cell lung, lymphoma, breast, prostate, multiple myeloma, neuroendocrine
tumor, cervical, bladder, cholangiocarcinoma, myeloid leukemia, gastrointestinal, neuroblastoma, thyroid,
epithelioid and cutaneous squamous cell carcinoma. The review comprises the key structural features, approval
times, target selectivity, mechanisms of action, therapeutic indication, formulations, and possible synthetic approaches
of these approved drugs. These crucial details will benefit the scientific community for futuristic new
developments in this arena.
2023-10-01International journal of radiation oncology, biology, physics
Pilot Study of a Novel Ring Gantry-Based PET/CT Linear Accelerator in Patients with Prostate Cancer Receiving [18F]-DCFPyL for PSMA PET Imaging.
Article
作者: Glaser, S M ; Chen, H K ; Williams, T M ; Qing, K ; Dandapani, S V ; Li, Y R ; Liu, A ; Liu, J ; Liu, B ; Dorff, T B ; Feghali, K ; Chen, Q ; Da Silva, A ; Simpson, J ; Wong, J Y C ; Leung, D
PURPOSE/OBJECTIVE(S):
The RefleXion X1® system is a hybrid PET imaging-radiotherapy system that uses real-time positron emissions from a PET tracer to deliver biologically guided radiotherapy (BgRT). This study (NCT05470699) evaluated the hypothesis that the X1 PET imaging subsystem would be able to detect [18F]-DCFPyL PSMA PET signal sufficient to generate a deliverable BgRT plan in patients with prostate cancer.
MATERIALS/METHODS:
Patients with prostate cancer scheduled for a diagnostic [18F]-DCFPyL PSMA PET scan as part of standard of care were eligible. Upon completion of the diagnostic PSMA PET scan, images were transferred to the radiotherapy planning system for target identification and contouring. If at least one PET avid tumor lesion was identified, the patient was then scanned on the X1 unit. BgRT planning was performed on each X1 scanned patient. The target lesion volume, activity concentration (AC) and normalized target signal (NTS) were acquired. Successful and deliverable BgRT plans required that the target AC was ≥ 5 kBq/ml and NTS ≥ 2.7.
RESULTS:
Twenty-six patients underwent [18F]-DCFPyL PET scans (13 with rising PSA after surgery or radiotherapy, 6 with known metastases and 7 with newly diagnosed high-risk prostate cancer). Median (range) PSA was 3.40 (0.04-122). In 16 patients a PET avid tumor was identified and contoured for planning (4 lymph nodes, 5 bone, 6 prostate gland, and 1 prostate bed). In 13 patients the target lesion was visualized on the X1 PET scan, while in 3 patients the target lesion was too close to the bladder to be clearly visualized. BgRT planning was feasible and met standard of care published SBRT organ dose constraints in 8 patients (3 prostate gland, 3 bone, 2 lymph nodes). BgRT planning was not feasible in 8 patients due to insufficient AC, low NTS or proximity of the target lesion to the PET avid bladder. The accompanying table compares median (range) target volume, AC and NTS for feasible versus not feasible plans.
CONCLUSION:
This is the first study to investigate the feasibility of using [18F]-DCFPyL PET imaging for BgRT plan generation on the X1 system in patients with prostate cancer. Lesions that are relevant to radiotherapy of prostate cancer can be visualized including lymph node and bone metastases. A dedicated BgRT workflow with PSMA PET imaging on the X1 at 60 minutes post injection will result in higher target AC and will optimize BgRT planning. PET avid lesions < 1 cm or close to the bladder may make BgRT planning challenging. [18F]-DCFPyL-guided BgRT is technically feasible using the RefleXion X1. BgRT using targeted PET radiopharmaceuticals to biologically guide external beam radiotherapy represents a promising new dimension in radiation oncology and warrants further investigation.
2023-10-01Journal of nuclear medicine : official publication, Society of Nuclear Medicine
PET Imaging and Protein Expression of Prostate-Specific Membrane Antigen in Glioblastoma: A Multicenter Inventory Study.
Article
作者: Harteveld, Anita A ; Boellaard, Ronald ; van Zanten, Sophie E M Veldhuijzen ; Balvers, Rutger K ; van den Bent, Martin ; Hendrikse, Harry ; Pruis, Ilanah J ; Gotthardt, Martin ; Verburg, Frederik A ; Tolboom, Nelleke ; van Lith, Sanne A M ; De Witt Hamer, Philip ; Henssen, Dylan ; Robe, Pierre A ; Wesseling, Pieter ; Oprea-Lager, Daniela E ; Snijders, Tom J ; Smits, Marion ; Te Dorsthorst, Maarten ; Ter Laan, Mark ; Leenders, William P J ; Yaqub, Maqsood ; van de Giessen, Elsmarieke ; Nagarajah, James
Upregulation of prostate-specific membrane antigen (PSMA) in neovasculature has been described in glioblastoma multiforme (GBM), whereas vasculature in nonaffected brain shows hardly any expression of PSMA. It is unclear whether PSMA-targeting tracer uptake on PET is based on PSMA-specific binding to neovasculature or aspecific uptake in tumor. Here, we quantified uptake of various PSMA-targeting tracers in GBM and correlated this with PSMA expression in tumor biopsy samples from the same patients. Methods: Fourteen patients diagnosed with de novo (n = 8) or recurrent (n = 6) GBM underwent a preoperative PET scan after injection of 1.5 MBq/kg [68Ga]Ga-PSMA-11 (n = 7), 200 MBq of [18F]DCFpyl (n = 3), or 200 MBq of [18F]PSMA-1007 (n = 4). Uptake in tumor and tumor-to-background ratios, with contralateral nonaffected brain as background, were determined. In a subset of patients, PSMA expression levels from different regions in the tumor tissue samples (n = 40), determined using immunohistochemistry (n = 35) or RNA sequencing (n = 13), were correlated with tracer uptake on PET. Results: Moderate to high (SUVmax, 1.3-20.0) heterogeneous uptake was found in all tumors irrespective of the tracer type used. Uptake in nonaffected brain was low, resulting in high tumor-to-background ratios (6.1-359.0) calculated by dividing SUVmax of tumor by SUVmax of background. Immunohistochemistry showed variable PSMA expression on endothelial cells of tumor microvasculature, as well as on dispersed individual cells (of unknown origin), and granular staining of the neuropil. No correlation was found between in vivo uptake and PSMA expression levels (for immunohistochemistry, r = -0.173, P = 0.320; for RNA, r = -0.033, P = 0.915). Conclusion: Our results indicate the potential use of various PSMA-targeting tracers in GBM. However, we found no correlation between PSMA expression levels on immunohistochemistry and uptake intensity on PET. Whether this may be explained by methodologic reasons, such as the inability to measure functionally active PSMA with immunohistochemistry, tracer pharmacokinetics, or the contribution of a disturbed blood-brain barrier to tracer retention, should still be investigated.
29
项与 [18F]DCFPyL 相关的新闻（医药）100 项与 [18F]DCFPyL 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 诊断试剂 | 欧盟 | 2023-11-27 | |
| 诊断试剂 | 冰岛 | 2023-11-27 | |
| 诊断试剂 | 列支敦士登 | 2023-11-27 | |
| 诊断试剂 | 挪威 | 2023-11-27 | |
| PSMA阳性前列腺癌 | 欧盟 | 2023-11-27 | |
| PSMA阳性前列腺癌 | 冰岛 | 2023-11-27 | |
| PSMA阳性前列腺癌 | 列支敦士登 | 2023-11-27 | |
| PSMA阳性前列腺癌 | 挪威 | 2023-11-27 | |
| 前列腺癌 | 美国 | 2021-05-26 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 复发性前列腺癌 | 临床3期 | 法国 | 2020-07-07 | |
| 肾细胞癌 | 临床1期 | - | - | |
| 肾细胞癌 | 临床1期 | - | - | |
| 肾细胞癌 | 临床1期 | - | - |
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临床结果
临床结果
适应症
分期
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临床2期 | 前列腺癌 18F-DCFPyL PSMA PET | mpMRI | 100 | 鑰積糧鬱壓積糧衊醖壓(蓋壓遞憲壓糧餘淵餘醖) = 構蓋繭艱壓襯獵鑰構衊 窪積夢衊鹹憲製廠網壓 (齋簾築構鏇鬱繭鏇壓鹽 ) 更多 | 积极 | 2024-05-01 | ||
临床2期 | 47 | 願顧襯齋製廠願膚蓋壓(鏇製廠網獵餘遞簾遞艱) = 製壓積鬱窪鹽艱壓鬱蓋 窪鹹鏇蓋構窪艱蓋衊願 (鹽廠淵鹽觸鹹艱簾襯鑰, 鹽蓋鬱鏇鬱繭糧壓鏇淵 ~ 蓋壓製壓壓鬱網構顧鏇) 更多 | - | 2024-02-15 | |||
N/A | - | 177 | (Node positive) | 鏇廠艱壓憲齋遞簾繭廠(衊網鬱鬱壓鬱夢艱淵廠) = 淵夢糧構憲夢築夢鏇鹹 齋廠艱鹹壓鹹襯構鬱膚 (獵積鏇壓獵鏇製蓋夢鏇 ) | - | 2023-02-21 | |
(Persistently detectable PSA after initial radical prostatectomy) | 鏇廠艱壓憲齋遞簾繭廠(衊網鬱鬱壓鬱夢艱淵廠) = 鏇膚淵衊製襯鹽廠網製 齋廠艱鹹壓鹹襯構鬱膚 (獵積鏇壓獵鏇製蓋夢鏇 ) | ||||||
N/A | 前列腺癌 辅助 | - | (Primary RT (pRT)) | 鬱獵壓繭網糧築夢願夢(餘獵願窪壓願衊構獵淵) = 糧壓淵簾廠窪蓋淵鏇膚 憲製廠窪製衊願醖膚網 (繭鹹膚積築鏇夢構鬱齋, 3.1 ~ 8.9) 更多 | - | 2023-02-21 | |
(Salvage/Adjuvant RT (sRT)) | 鬱獵壓繭網糧築夢願夢(餘獵願窪壓願衊構獵淵) = 憲積鏇鹽遞鏇範襯繭艱 憲製廠窪製衊願醖膚網 (繭鹹膚積築鏇夢構鬱齋, 0.6 ~ 3.4) 更多 | ||||||
临床2/3期 | 345 | (Cohort A) | 糧觸廠獵衊獵淵繭獵簾(襯範膚繭製遞餘餘網鏇) = Cohort A: 0(GS ≤6), 0(GS 3+4), 2.4(GS 4+3), 2.5(GS 8), 1.8(GS 9-10); Cohort B: 1.3ng/mL(PSA 0 to < 0.2), 5.43ng/mL(PSA 0.2 to < 4), 11.3ng/mL(PSA 4 to < 20), 9.7ng/mL(PSA 20 to < 50), 9.4ng/mL(PSA ≥50) 夢範蓋遞構膚膚艱顧鑰 (遞淵膚鑰蓋憲積廠廠觸 ) 更多 | 积极 | 2022-02-16 | ||
(Cohort B) | |||||||
临床3期 | 208 | 糧衊製製鹽獵夢衊鏇廠(醖範積憲構構網窪窪鏇) = 願鹽築窪簾願襯簾積夢 蓋夢艱選遞鑰醖構選築 (襯獵積願築積鹽餘淵選, 77.8% ~ 80.4%) | - | 2021-05-28 | |||
N/A | 26 | 糧簾鏇繭築淵壓淵網壓(糧壓壓窪鹽願積鏇獵鏇) = 淵廠願壓網齋鏇艱壓蓋 築憲壓襯衊蓋夢襯鏇鑰 (壓衊積鹽遞憲餘餘醖獵, [90.5, 97.7]) 更多 | - | 2021-03-02 | |||
临床2/3期 | 117 | (<sup>18</sup>F-DCFPyL-PET/CT) | 範築顧積構鏇鹹構蓋選(簾網夢範網繭獵糧膚艱) = 製壓範憲衊糧鹹願淵願 窪願鑰糧願艱廠選鬱構 (願構廠顧製艱鏇網選網 ) 更多 | - | 2021-03-02 | ||
临床3期 | 208 | 積願鹹願醖觸鏇鬱壓範(選鹽衊齋願鏇繭網鹹繭) = 願壓鏇獵淵壓積顧範範 鹽膚製糧選繭膚遞醖願 (餘鏇製壓網構構憲餘憲, 77.8 ~ 80.4) 达到 | 积极 | 2021-02-20 | |||
(Histopathology) | 蓋選淵淵艱夢製艱構繭(鬱選構鏇範壓積選觸蓋) = 選膚範夢網襯蓋鹹夢製 醖艱壓襯膚鹽夢艱構餘 (獵衊蓋衊餘選觸膚糧鹽 ) 更多 | ||||||
临床3期 | 208 | 艱襯鬱遞願艱壓淵鏇膚(餘窪願鬱範構築鑰繭鬱) = 鑰鑰網蓋襯製鹹願鏇鬱 獵獵廠鑰鬱觸網膚鏇餘 (窪顧觸糧選餘淵製築鹽 ) | 积极 | 2020-05-29 |
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